R | S | T

Product #


Product Name

Biochem/physiol Actions

Gene Symbol (ID)

Add to Cart

SML0181 S 17092 ≥98% (HPLC) S-17092 is a potent, selective inhibitor of Prolyl oligopeptidase (POP), also known as prolyl endopeptidase (PEP or PE). Ki=1.5 nM. Nootropic.

S-17092 inhibition of POP prevents breakdown and thus increases the activity of a number of neuropeptides, which is likely the basis for its nootropic activity. S 17092 has been shown to improve cognition. It improved cognitive task performance in chronic low dose MPTP-treated monkeys. S-17092 was recently used to inhibit the formation of AcSDKP from its precursor 43-mer thymosin ?4 (T?4). Ac-SDKP is involved in hemopoietic stem cell differentiation, is pro-angiogenic and antifibrogenic.
SML1111 S 24795 ≥98% (HPLC) S 24795 is a selective partial agonist for the α7-subtype of nicotinic acetylcholine receptor (nAChR). S 24795 was shown to be effective at improving learning and memory in various animal models relevant to Alzheimer’s disease and age-related memory loss, and is used in investigating the roles of α7 nAChRs in aging, learning, memory, and cognition.
SML0510 S 26948 ≥98% (HPLC) S 26948 is a selective PPARγ modulator (SPPARγM). S 26948 is as effective as rosiglitazone in reducing insulin resistance and lipid homeostasis, but does not increase body or white adipose tissue weight. S 26948 also leads to different co-activatior recruitment to PPARγ than rosiglitazone.
SML2177 S 38093-2 ≥98% (HPLC) S 38093 is an orally available compound with selective affinity toward histamine H3 receptor (human/mouse/rat H3R Ki = 0.2/1.44/8.8 μM), but not other histaminergic receptors, exhbiting both antagonist (KB = 652 nM against 300 nM (R)-α-Methylhistamine-induced GTPγS recruitment to mH3 CHO membrane; KB = 110 nM against 1 μM histamine-induced cAMP downregulation in hH3 CHO cells) and inverse agonist activity (hH3/rH3 HEK basal cAMP enhancing EC50 = 1.7/9 μM; 48% inhibition of ionomycin-induced hH3 or rH3 HEK AA reslease by 10 μM S 38093). S 38093 is reported to improve AD- and age-associated memory and cognition deficits in mice (0.1-3 mg/kg/day p.o.) and rats (0.1-10 mg/kg p.o. or i;p.), as well as display antiallodynic and antihyperalgesic efficacy in rat models of neuropathic pain in vivo.
SML2165 (S)-(+)-Dimethindene maleate ≥98% (HPLC) (S)-(+)-Dimethindene maleate is an antagonist of muscarinic M2 and histamine H1 receptors, recently used as part of part of four-component chemical cocktail shown to convert pluripotent stem cells (PSCs) into extended pluripotent stem (EPS). (S)-(+)-Dimethindene is up to 40-fold more potent than the (R)-(-) enantiomer, with pKi values of 7.78 for M2, and lower affinities for M1, M3 and M4 (7.08, 6.7 and 7.0, respectively). (S)-(+)-Dimethindene has lower affinity for H1 than (R)-(-)- Dimethindene, with pA2 values of 7.48 vs. 9.42, respectively.
M2 and H1 antagonist, part of four-component chemical cocktail shown to convert pluripotent stem cells (PSCs) into extended pluripotent stem (EPS)
SML2147 S-Equol ≥97% (HPLC) (S)-Equol is an estrogen receptor beta (ERβ) agonist, formed in some people by intestinal bacteria from the soy phytoestrogen daidzein. (S)-Equol has approximately 13-fold higher affinity for human ERβ over ERα and an EC50 value of 65nM for ERβ compared to an EC50 value of 85nM for ERα. It has been shown to have anti-inflammatory and neuroprotective activty.
S6445 S-2E ≥98% (HPLC), powder HMG-CoA reductase and acetyl-CoA carboxylase inhibitor. In the liver, S-2E is converted into its active metabolite, S-2E-CoA. S-2E-CoA noncompetitively inhibited the enzymatic activities of both 3-hydroxy-3-methylglutaryl coenzyme-A (HMG-CoA) reductase and acetyl-CoA carboxylase at K(i)=18.11 microM and K(i)=69.2 microM, respectively.
SML0638   S0859 ≥98% (HPLC) S0859 helps to prevent the depolarization-induced alkalinization (DIA) in astrocytes.
S0859 is a selective high-affinity generic inhibitor of the Na+/HCO3- sodium bicarbonate co-transporter (NBC). S0859 does not inhibit Na+-H+ exchange (NHE).
SML2291 S119-8 ≥98% (HPLC) S119-8 is an inhibitor of viral nucleoprotein of influenza A and B. It showed synergistic effects with oseltamivir.
SML1571 S14161 ≥98% (HPLC) S14161 inhibits D-cyclin transactivation by inhibition of phosphoinositide 3-kinase (PI3K) activity. S14161 is a pan-class I PI3K inhibitor. S14161 inhibited the activity of all 4 isoforms of the PI3K class I family, and unlike LY294002, had little effect on class IV enzymes mechanistic target of rapamycin (mTOR) and DNA-PKcs (DNA-dependent protein kinase, catalytic subunit), or on AKT-1, -2, or -3 or PDK1. S14161 inhibited the expression of cyclins D1, D2, and D3, leading to the arrest of cells at the G0/G1 phase, and has exhibited anti-myeloma and anti-leukemia activity with no gross toxicity.
S5944 S-15176 difumarate salt ≥98% (HPLC), solid Antioxidant and anti-ischemic agent. Also inhibits mitochondrial permeability transition, prevents the early step in apoptosis by preventing collapse of the electrochemical gradient across the mitochondrial membrane. IC50 for in vitro lipid peroxidation is 0.3 μM. IC50 for carnitine palmitoyltransferase (CPT-1) in heart homogenate is 16.8 μM. The shift from fatty acid to glucose oxidation may contribute to anti-ischemic effect.
S-15176 suppresses the mitochondrial permeability transition in response to calcium ions and inorganic phosphate and inhibits the release of cytochrome c in response to silver ions. It exhibits weak protonophoric activity.5
S5321 S15535 ≥98% (HPLC), solid Potent, orally active, partial 5-HT1A receptor agonist
S15535, a benzodioxane, is a selective but partial agonist of histamine 5-HT1A receptor. It activates presynaptic 5-HT1A receptors and suppresses the release of hippocampal 5-HT. It acts as anxiolytic agent and modulates the cholinergic and cognitive function in rodents.3,4
E8278   S1P5 C-Terminal Blocking Peptide buffered aqueous solution    
SML1948 S1QEL1.1 ≥98% (HPLC) S1QEL1.1 is a suppressor of mitochondrial respiratory complex I site IQ electron leak, suppressing superoxide and/or H2O2 production without altering oxidative phosphorylation. S1QEL1.1 had an IC50 values of 70 nM against superoxide-H2O2 production from site IQ. It decreased caspase activation in a in a cardiomyocyte cell model of ER stress and decreased ischemia-reperfusion injury in the Langendorff-perfused mouse heart model.
SML2642 S29434 ≥98% (HPLC) S29434 is a cell and blood-rain barrier penetrant, potent and selective inhibitor of quinone reductase 2 (QR2, NQO2) that inhibits production of ROS by QR2 in cells. S29434 triggers autophagy in human HepG2 cells. S29434 enhances exploring time of the unfamiliar object in mice memory test.
SML1996 S3226 ≥98% (HPLC) S3226 is a potent and selective NHE3 (NHE-3) inhibitor (IC50 = 20 nM/human NHE3, 3.6 μM/human NHE1, 80 μM/rabbit NHE2) for studying NHE3 physiological as well as pathophysiological roles in kidney and gastrointestinal disorders in vitro and in animal models in vivo.
S3226 is also known as {3-[2-(3-guanidino-2-methyl-3-oxo-propenyl)-5-methyl-phenyl]-N-isopropylidene-2-methyl-acrylamide dihydro-chloride}. S3226 is used to explore the physiological and pathophysiological functions of sodium-hydrogen exchanger 3 (NHE3) in animal models. It is a bismethacryloyl guanidine derivative.
S1825 S32826 disodium salt hydrate ≥98% (HPLC) S32826 is a potent inhibitor of autotaxin. Autotaxin is a newly discovered lyso-phospholipase D (lysoPLD). Autotaxin and lyso-phosphatidic acid (LPA) have been associated with early cancer progression and motility of cancer cells as well as with metastasis. Because of localization (adipose tissue), the enzyme might play an important role in diabetes and obesity. Autotaxin might be the only source of LPA. S32826 is the strongest inhibitor of autotaxin reported. The compound shows activity in cellular or ex vivo models.
SML0330 S3I-201 ≥97% (HPLC) S3I-201 is a cell-permeable Stat3 inhibitor that binds to the Stat3-SH2 domain, prevents Stat3 phosphorylation/activation, dimerization, and DNA-binding.
SML1554   S3QEL 2 S3QEL 2 is a selective inhibitor of superoxide production from the outer Q-binding site of mitochondrial respiratory complex site III (IIIQo) without altering oxidative phosphorylation. Site IIIQo is the primary source of mitochondrial reactive oxygen species (ROS) and has been implicated in a broad range of ROS-mediated signaling and pathology. S3QEL 2 lowered HIF-1α induction, protected against ROS-induced, JNK-mediated cell stress in pancreatic beta-cells, and decreased the oxidative stress-induced apoptosis that limits the yield of functional β-cells from intact islets.
S3QEL 2, a cell permeable substituted allopurinol, is also known as 1-(3,4-Dimethylphenyl)-N,N-dipropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine.
SML2031 S4 ≥98% (HPLC) S4 is a potent and selective inhibitor against sulfamate carbonic anhydrase (CA) subtypes CAIX & CAXII (Ki = 2, 7, 546, 5600 nM against human CA XII, IX, II, and I, respectively). S4 selectively inhibits migration upon anoxia/hypoxia-induced CAIX expression in cancer cultures (% inhibition/conc./cell line = 54%/100 μM/WRO, 65%/33 μM/MDA-MB-231), while exhibiting no inhibitory effects under normoxia or among non-CAIX-expressing cells (HCT116 & RT112). Daily intraperitoneal injection (10 mg/kg) is reported to reduce the metastatic tumor burden in lungs of mice bearing orthotopic eGFP-MDA-MB-231 tumors in vivo.
SML2181 SA4503 ≥98% (HPLC) SA4503 is a high affinity, orally active non-opioid intracellular receptor sigma-1 (σ1R) selective agonist (IC50 = 17.4 nM against 200 nM (+)-pentazocine for binding σ1R), exhibiting ~100-fold less affinity for the sigma 2 receptor subtype (σ2R) and little or no affinity toward 36 other receptors, ion channels and second messenger systems. Oral administration is reported to elicit cerebral acetylcholine (ACh) release in rat frontal cortex and hippocampus (5-20 mg/kg p.o.) and reduce immobility time in a mouse forced swimming test (Immobility time = 214.8 s without vs. 111.6 s with 1.0 mg/kg oral dosage).
JN0007   Sabeluzole ≥98% (HPLC) Sabeluzole is a benzothiazole derivative that exerts neuroprotective and cognition-enhancing (nootropic) efficacy by preventing NMDA- and glutamate-induced neurotoxicity.
SML1380 Sacubitril calcium salt ≥98% (HPLC) Sacubitril (AHU377) is a prodrug inhibitor of the membrane metallo-endopeptidase neprilysin. Sacubitril forms half of the heart failure combination drug LCZ696, along with the angiotensin-receptor blocker Valsartan. Sacubitril (AHU377) is cojnverted by esterases into the active inhibitor LBQ657, which prevents neprilysin′s degradation of atrial and brain natriuretic peptide, two blood pressure lowering peptides. The AHU377 valsartan combination drug LCZ696 showed a reduction in the risk of cardiovascular death of 20% compared to the standard ACE inhibitor enalapril, and also a 21% drop in the risk of hospitalization.
SML0025 Safinamide mesylate salt ≥98% (HPLC) Safinamide is a highly selective and reversible monoamine oxidase type B (MAO-B) inhibitor that increases neostriatal dopamine concentration. In addition, safinamide is voltage-dependent sodium and calcium channel blocker. It appears to bind to the batrachotoxin-sensitive site 2 of the voltage-sensitive sodium channels. Safinamide blocks N and L-type calcium channels and inhibits glutamate and aspartate release from synaptic terminals.
Safinamide mesylate prevents dopamine reuptake and is effective in the treatment of epilepsy and Parkinson′s disease.
human ... MAOB(4129)
SML1314 SAG dihydrochloride ≥98% (HPLC) SAG is a potent and cell-permeable smoothened (Smo) agonist that activates Hedgehog pathway and counteracts Cyclopamine inhibition of Smo.
SML0061 SAHA ≥98% (HPLC) SAHA or Vorinostat facilitates the transcription of genes that result in apoptosis, differentiation and growth arrest. It has been observed to give beneficial results in lymphoma but not in solid tumors.
Vorinostat or suberoylanilide hydroxamic acid (SAHA) is a potent, reversible pan-histone deacetylase (HDAC) inhibitor. It inhibits both class I and class II HDACs, altering gene transcription and inducing cell cycle arrest and/or apoptosis in a wide variety of transformed cells.
human ... HDAC1(3065), HDAC2(3066), HDAC3(8841), HDAC6(10013)
SML2198 sAJM589 ≥98% (HPLC) sAJM589 is a Myc inhibitor that disrupts the Myc-Max heterodimer with an IC50 value of 1.8 μM. sAJM589 was shown to suppress cellular proliferation in a variety of MYC-dependent cancer cell line including strong inhibition of Burkitt lymphoma Raji cell line growth. The mechanism of action of sAJM589 is thought to involve increased ubiquitination of Myc by inhibition of Max binding to Myc, leading to proteasome-mediated degradation.
SML2039 SAK3 ≥98% (HPLC) SAK3 is a potent and orally active spiroimidazopyridine derivative that enhances Cav3.1 and Cav3.3, but not Cav3.2, T-type voltage-gated Ca2+ channel (T-VGCC) activity (∼20% peak current increase with 0.1 nM SAK3 by whole-cell patch-clamp using human Cav3.1 or Cav3.3 transfected neuro2A; no effect up to 10 nM using Cav3.2 transfectant). Acute SAK3 oral administration (0.5 mg/kg) significantly enhances hippocampal CA1 region acetylcholine (ACh) release in naïve mice, as well as increases hippocampal ACh levels and improves memory deficits among olfactory-bulbectomized (OBX) mice. Daily SAK3 oral administration 24 hrs following hypothyroidism induction by methimazole (MMI) is efficacious against MMI-induced medial septum (MS) cholinergic neurons loss (0.5-1 mg/kg/day) and cognitive deficits (1 mg/kg/day).
S4451 Sal003 ≥98% (HPLC) Sal003 inhibits the late long-term potentiation (L-LTP) and long-term memory formation in mammalian hippocampal slices. The effect of Sal003 on L-LTP is mediated by the transcription factor, ATF4.
Sal003 is a potent and cell-permeable eIF-2a phosphatase inhibitor.
S8260 Salbutamol β2-adrenoceptor agonist
Salbutamol is a β2 adrenoceptor agonist with short acting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles and inhibits bronchoconstriction induced by adenosine-5′ -monophosphate (AMP).1 Salbutamol is particularly effective in treatment of asthma as it provides immediate relief.2
human ... ADRB2(154)
S5013 Salbutamol hemisulfate salt ≥98% β2-Adrenergic receptor agonist.
Salbutamol is a β2 adrenoceptor agonist with short acting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles and inhibits bronchoconstriction induced by adenosine-5′ -monophosphate (AMP).1 Salbutamol is particularly effective in treatment of asthma as it provides immediate relief.2
Salbutamol is a β2 adrenoceptor agonist with short acting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles and inhibits bronchoconstriction induced by adenosine-5′ -monophosphate (AMP). Salbutamol is particularly effective in treatment of asthma as it provides immediate relief. Salbutamol is one of the most popular short-acting BA (SABA). It is useful in treating the symptoms of EIB (exercise induced bronchospasm).
human ... ADRB2(154)
S8825 Salermide ≥98% (HPLC) Salermide is a novel Sirtuin 1 (Sirt1) and Sirtuin 2 (Sirt2) inhibitor (III histone deacetylases inhibitor). In vitro Salermide has a stronger inhibitory effect on Sirt2 than on Sirt1. Salermide induces massive apoptosis in tumor cells. The activity was ascribed to effect of Salermide to the reactivation of proapoptotic genes epigenetically repressed exclusively in cancer cells by Sirt1. Salermide is a stronger Sirtuin inhibitor than sirtinol (Cat. No.S7942).
UC407 Salicyl glucuronide disodium salt Phase II metabolite of aspirin.
S6444 N-Salicyloyltryptamine ≥98% (HPLC), solid N-Salicyloyltryptamine (STP) is a central nervous system depressant that inhibits the transient outward and sustained K+ current in neuroendocrine cells. This decreases the ability of neuronal cells to generate action potential.1,3 STP is has immunomodulatory effects as it inhibits the activation of ERK 1/2 and NF-κB.4
Activator of calcium-activated K+ channels; anticonvulsant and neuroprotectant.
S4526 Salinomycin from Streptomyces albus, ≥98% (HPLC) Salinomycin produced by Streptomyces albus is a carboxylic polyether ionophore with antibiotic and anti-cancer properties. It induces cell death in some types of cancer cells such as breast, lung, gastric cancer, leukemia and osteosarcoma. Salinomycin inhibits multidrug resistance protein 1 and induces apoptosis by the generation of reactive oxygen species that cause DNA damage and inactivation of Stat3. Use of salinomycin as antibiotic results in lowered spermatozoa count and motility and decreased steroidogenesis in mice.
S6201 Salinomycin, Ready Made Solution from Streptomyces albus, ≥98% (HPLC) Salinomycin is a monocarboxylic polyether antibiotic with unique tricyclic spiroketal ring systems and an unsaturated six-membered ring in the molecule. Salinomycin has antimicrobial and anticoccidial activities. It is an alkali ion carrier with affinity for cations and preference for K+ over other monovalent and divalent cations. Polyether antibiotics (also called carboxylic ionophores) facilitate bidirectional ion flux through the lipid barrier of membranes causing interference with natural ion transport systems both in prokaryotic and eukaryotic cells. Tumor cells express elevated levels of various types of K+ channels, which enhances cell proliferation. Thus, drugs acting as channel blockers inhibit cell proliferation. Being a highly selective potassium ionophore, salinomycin may interfere with potassium channels function in cancer stem cells (CSCs). Established cancer therapies may fail because they kill the bulk tumor cells, but do not eliminate CSCs. Studies indicate that Salinomycin selectively eradicates breast CSCs. Salinomycin may eliminate CSCs by inducing their differentiation. salinomycin suppresses the metastatic migration of 4T1 cells to the lungs.
SML1166 Salirasib ≥98% (HPLC) Salirasib (Farnesylthiosalicylic acid) is a RAS inhibitor that acts by dislodging the farnesylated protein from the membrane, facilitating Ras degradation. Salirasib impairs downstream signaling and suppresses growth and migration of proliferating tumor cells in in vitro and in vivo models. Salirasib (Farnesylthiosalicylic acid) has recently been shown to possess significant anti-inflammatory and anti-arthritic properties.
Salirasib (S-trans,trans-Farnesylthiosalicylic Acid /FTS) is a synthetic small molecule that has an ability to block all forms of Ras, unlike farnesyltransferase inhibitors, which fail to inhibit K-Ras and N-Ras function due to alternative membrane-binding mechanisms. Salirasib along with gemcitabine, exhibits anti-tumor activity and biomarker modulation in preclinical models of metastatic pancreatic adenocarcinoma (PDA). It is also used as a potent therapeutic for lung cancer.
S5068   Salmeterol xinafoate ≥98% (HPLC), solid β2-adrenoceptor agonist.
Salmeterol xinafoate is a β2 adrenoceptor agonist with longer lasting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles, stabilizes mast cells and regulates the release of histamine. Salmetrol is particularly effective in treatment of mild asthma, chronic obstructive pulmonary disorder.5,6
human ... ADRB2(154)
SML0070 Salsalate ≥98% (HPLC) Salsalate is a nonsteroidal anti-inflammatory drug (NSAID), a nonacetylated salicylate with no more problems of gastrointestinal bleeding than placebo. It inhibits synthesis and release of prostaglandins through the inactivation of cyclooxygenase-1 (COX-1) and COX-2. Salsalate is currently being investigated as a treatment for Type 2 diabetes with possible use to prevent the disease in people at risk. It reduces blood glucose concentrations in patients with type 2 diabetes, as well as in insulin-resistant patients without diabetes.
SML0398 Salsolinol hydrobromide ≥96% (HPLC) Salsolinol is the condensation product of acetaldehyde and dopamine. Salsolinol is a potential neurotoxin suspected to contribute to alcohol abuse. It appears that salsolinol excites the ventral tegmental area (VTA) dopamine neurons indirectly by activating μ-opioid receptors (MORs), which inhibit GABA neurons in the VTA.
SML0951   Salubrinal ≥98% (HPLC) Salubrinal is a selective Inhibitor of eIF2α (eukaryotic translation initiation factor 2 α-subunit) dephosphorylation, inhibiting global protein translation. Salubrinal is a specific inhibitor of ER Stress induced apoptosis.
Salubrinal maintains protein phosphorylation in order to offer protection against from the adverse effects of endoplasmic reticulum stress. Salubrinal prevents collagenase-mediated articular cartilage damage promoting downregulation of matrix metalloproteinase 13.
SML0045 Salvianolic acid A hydrate ≥98% (HPLC) Salvianolic acid A acts as scavengers of reactive oxygen species, reduces the adherence of leukocytes to endothelial cells, inhibits matrix metalloproteinases and inflammation. It has cardioprotective effects as it suppresses apoptosis, reduces lipid peroxidation in damaged cardiac tissue and decreases the leakage of lactic acid dehydrogenase.
Salvianolic acid A is cell protective antioxidant originally isolated from Salvia. It has been found to attenuate PDGF-induced ROS formation in hepatic stellate cells and protected against isoproterenol-induced myocardial damage in rats.
SML0048 Salvianolic acid B ≥94% (HPLC) Salvianolic acid B is a cell protective antioxidant and free radical scavenger being investigated for a variety of conditions from ischemic heart disorders to Alzheimer′s disease. Several mechanisms of action have been proposed including EGFR, PDGF and MMP-9 inhibition and inhibition of the TGF-β1/Smads and NF-κB signaling pathways. Salvianolic acid B acts as scavengers of reactive oxygen species, reduces the adherence of leukocytes to endothelial cells, inhibits matrix metalloproteinases and inflammation. It has cardioprotective effects as it reduces lipid peroxidation in damaged cardiac tissue and decreases the leakage of lactic acid dehydrogenase.
S8071 Salvinorin A ≥98% (HPLC), solid Salvinorin A is a potent, non-nitrogenous κ opioid selective receptor agonist. Salvinorin A is isolated from Salvia divinorum. Salvinorin A displays high affinity at both native (Ki=4.3 nm) and cloned (Ki=16 nm) κ -opioid receptors. Preliminary studies suggest that Salvanorin A is chemically unique among the psychtropic drugs and does not bind to any known receptor.
human ... OPRD1(4985), OPRK1(4986), OPRM1(4988)
rat ... Oprk1(29335)
SML1460   SAMS Peptide trifluoroacetate salt ≥95% (HPLC) SAMS Peptide is a synthetic substrate selective for AMP-activated protein kinase (AMPK). Its sequence is based on acetyl-CoA carboxylase, which is phosphorylated exclusively by the AMPK, but with serine (Ser)-79 replaced by alanine SAMS peptide is more specific for AMPK than acetyl-CoA carboxylase itself.
SML0214   SAMT-247 ≥98% (HPLC) SAMT-247 inhibits HIV by modifying the nucleocapsid NCp7 region of Gag in infected cells, blocking Gag processing and reducing infectivity.
SAMT-247 is a microbicide that decreases the viral infectivity and infectivity of the progeny virus in HIV-1 infections.
S9318 Sandoz 58-035 >98% (HPLC), powder Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor.
Sandoz 58-035 inhibits the accumulation of cholesteryl esters and inhibits the esterification of cholesterol by 95% in arterial smooth muscle cells in culture.1 It does not affect the triglyceride metabolism by the gut.2
human ... SOAT1(6646)
rat ... Soat1(81782)
S5890 Sanguinarine chloride hydrate ≥98% (HPLC) A natural product with antimicrobial, anti-inflammatory, and anti-oxidant properties. Has antiproliferative, pro-apoptosis effects in some cancer cell lines.
Sanguinarine is a benzophenanthridine alkaloid isolated from plants belonging to the family Papaveracea. It exhibits anti-bacterial, anti-fungal, anti-inflammatory and anti-cancer properties. It induces cell cycle arrest and sensitizes cancer cells to apoptosis by activating TNF-related apoptosis inducing ligand.6,7 It inhibits STAT3, MMP-2, MMP-9, interacts with glutathione, induces generation of ROS, disrupts the microtubule assembly and causes DNA damage resulting the death of the cancer cells.6,7,8
S4572 SANT-1 ≥98% (HPLC), powder SANT-1 inhibited Sonic hedgehog signaling and induced apoptosis via Ras/NF-κB pathway in glioblastoma cells.
SANT-1 is a potent sonic hedgehog pathway (Shh) antagonist that directly inhibits by binding to the smoothened (Smo) receptor. SANT-1 inhibits wild type and oncogenic Smo with equal potency.
SML0644   SANT-2 ≥95% (HPLC) SANT-2 is a potent sonic hedgehog pathway (shh) antagonist that directly inhibits by binding to the smoothened receptor.
S8451 Saquinavir mesylate ≥98% (HPLC), powder Saquinavir is an HIV Protease Inhibitor used in antiretroviral therapy. It inhibits both HIV-1 and HIV-2 proteases. Studies have also looked at saquinavir as a possible anti-cancer agent.
SML2772 SAR405838 ≥98% (HPLC) New SAR405838 (MI-77301) is an orally available (F = 67%/mouse, 48%/rat; 10 mg/kg p.o.), highly potent and selective Mdm2 (Hdm2) inhibitor (human Mdm2 Ki = 0.88 nM; no binding at 10 μM to Bcl-2, Bcl-xL, Mcl-1, Mdmx; no inhibition against >200 receptors/enzymes) that upregulates wild-type p53 activity (EC50 = 300-600 nM; SJSA-1) by blocking Mdm2-p53 interaction and Mdm2-mediated p53 degradation with 5-10-times higher potency than MI-219 and nutlin-3a. SAR405838 inhibits cancer growth in a wild-type p53-dependent manner both in cultures (IC50 = 89 nM/RS4;11, 92 nM/SJSA-1, 200 nM/HCT-116, 270 nM/LANCaP) and in xenograft models in vivo (50-200 mg/kg single or daily p.o. dosing).
SML1574   Sarcophine ≥97% (HPLC) Sarcophine, a cembranoid from the Red Sea soft coral Sarcophyton glaucum, is an inhibitor of tumorigenesis. Sarcophine exhibits anti-tumor, chemo-preventive and antimicrobial activities. Sarcophine is a competitive cholinesterase inhibitor, noncompetitive phosphofructokinase inhibitor, and Na+, K+-ATPase inhibitor.
S5451 Sarpogrelate hydrochloride ≥98% (HPLC) Sarapogrelate hydrochloride is a potent and selective 5-HT2A receptor antagonist. It exhibits analgesic effects in numerous animal studies.
SML0783 Sauchinone ≥98% (HPLC) Sauchinone is an anti-inflammatory and antioxidant lignan isolated from Saururus chinensis a medical plant used for the treatment of fever, jaundice, oedema and inflammatory disease in oriental folk medicine. Sauchinone inhibits LPS-inducible iNOS (NOS II), TNF-α and COX-2 expression in macrophages through suppression of IKBα phosphorylation. It appears that sauchinone protects against myocardial ischemia/reperfusion injury by inhibition of p28 phosphorylation.
S7067 SB 202190 ≥98% (HPLC) SB 202190 is a highly selective, potent and cell permeable inhibitor of p38 MAP kinase. SB 202190 binds within the ATP pocket of the active kinase (Kd = 38 nM, as measured in recombinant human p38), and selectively inhibits the p38α and β isoforms.
human ... MAPK14(1432)
S7076 SB 202190 monohydrochloride hydrate ≥98% (HPLC) SB 202190 binds within the ATP pocket of p38 kinase and inhibits the p38α and β isoforms.
SB 202190 is a highly selective, potent, and cell-permeable inhibitor of p38 MAP kinase.
SB 202190 monohydrochloride hydrate mediates the phosphorylation of serine in the mutant p53 protein and modulates cell adhesion and prevents cell proliferation in breast cancer cell lines.
S8307 SB 203580 solid, ≥98% (HPLC) SB 203580 is a pyridinyl imidazole that suppresses the activation of MAPKAP kinase-2 and inhibits the phosphorylation of heat shock protein (HSP) 27 in response to IL-1, cellular stresses and bacterial endotoxin in vivo. It does not inhibit JNK or p42 MAP kinase and therefore, is useful for studying the physiological roles and targets of p38 MAPK and MAPKAP kinase-2. It has been shown to induce the activation of the serine/threonine kinase Raf-1 and has been reported to inhibit cytokine production.
human ... CYP1A2(1544), CYP2C19(1557), CYP2C9(1559), CYP2D6(1565), CYP3A4(1576), IL1B(3553), MAPK14(1432), MAPK8IP2(23542), RAF1(5894), TNF(7124)
S3313 SB-204070 hydrochloride solid, ≥97% (HPLC) SB-204070 is a highly potent and specific antagonist of 4-HT4 receptor. It inhibits cholinergic and noncholinergic transmission and blocks the contractions of proximal colon in guinea pigs and relaxation of human colon circular smooth muscle.
Selective 5-HT4 serotonin receptor antagonist.
human ... HTR4(3360)
S0693 SB 204741 >98% (HPLC) 5-HT2B serotonin receptor antagonist.
human ... DRD2(1813), DRD3(1814), DRD5(1816), HTR1E(3354), HTR2A(3356), HTR2B(3357), HTR2C(3358)
rat ... Adra1a(29412), Gabra2(29706), Htr1a(24473), Htr2b(29581), Htr3a(79246)
S7936 SB 205384 solid GABAA receptor modulator selective for the α3β2γ2 subunit combination.
SB 205384 is a selective and positive allosteric modulator of non-benzodiazepine site of the GABAA receptor.3 It affects the extrasynaptic GABAA receptors in rat cortical neurons4 and enhances the GABAergic transmission onto pro-opiomelanocortin neurons in mice.5
S180 SB-206553 hydrochloride hydrate ≥98% (HPLC), solid Potent 5-HT2B/5-HT2C serotonin receptor antagonist.
human ... HTR2B(3357), HTR2C(3358)
SML1349 SB-207266 ≥98% (HPLC) SB-207266 is a potent, selective, orally active and long-acting 5-HT4 antagonist in vivo.
S1068 SB-215505 solid, >98% (HPLC) Selective 5-HT2B serotonin receptor antagonist; 100-fold higher affinity at 2B versus 2C.
human ... HTR2B(3357)
S3442 SB 216763 >98% (HPLC) Potent, selective, cell permeable glycogen synthase kinase-3 (GSK-3) inhibitor.
SB-216763 is a small molecule that competes with ATP and potently inhibits the activity α and β isozymes of GSK-3. It acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway. It also delays preconditioning, reduces infarct size and prevents cardiac ischemia.
human ... GSK3A(2931), GSK3B(2932)
S9070 SB 220025 trihydrochloride ≥98% (HPLC), solid SB 220025 is a potent, specific inhibitor of human p38 mitogen-activated protein (MAP) kinase, with an IC50 value of 60 nM and 50- to 1000-fold selectivity. SB 220025 reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 reduced the lipopolysaccharide-induced production of TNF at an ED50 value of 7.5 mg/kg. At 30 mg/kg, SB 220025 reduced the expression of TNF and inhibited angiogenesis by ~40%. In a further study, the effects of p38/CSBP MAP kinase inhibition in angiogenesis-dependent chronic inflammatory disease was tested in murine collagen-induced arthritis and SB 220025 was able to prevent the progression of established arthritis.
S5192 SB 222200 ≥98% (HPLC), solid Non-peptide NK3 tachykinin receptor antagonist.
SB 222200 is a 2-phenyl-4-quinolinecarboxamides and a selective, reversible and competitive antagonist of human NK-3 receptor that effectively crosses the blood-brain barrier. It inhibits the NK-3 receptor-induced miosis or pupil constriction in conscious rabbits.1,2
human ... TACR2(6865), TACR3(6870)
SML0716   SB225002 ≥98% (HPLC) Blocking action of SB-225002 on CXCR2 (interleukin 8 receptor β), prevents the IL-8 induced matrix metalloproteinase-9 release from neutrophils. Matrix metalloproteinase-9 are proteolytic enzymes associated with inflammation.
SB-225002 is a potent nonpeptide inhibitor of chemokine receptor CXCR2 with an IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2 and > 150-fold selectivity over CXCR1 receptors. CXCR2 binds many different immune cell chemoattractants. SB-225002 is crucial for cancer progression and is involved in inflammatory diseases like COPD, rheumatoid arthritis, and ulcerative colitis.
S0569 SB 239063 >98% (HPLC) Potent p38 MAP kinase inhibitor. Selective for α and β. No activity against γ and δ isoforms.
S8061 SB 242084 dihydrochloride hydrate ≥98% (HPLC), powder SB 242084 is a potent and selective antagonist of 5-HT2C receptor. It increases the basal activity of dopaminergic neurons and affects the behavioral responses mediated by 5-HT2C such as mesolimbic neuron activity and food intake.3,4,5
S1194 SB-258585 dihydrochloride ≥98% (HPLC), powder 5-HT6 serotonin receptor antagonist.
SML1807 SB-258719 ≥98% (HPLC) SB-258719 is a selective and potent 5-HT7 antagonist. SB-258719 reverses the hypothermic effect of 5-CT in mice.
SML0421 SB265610 ≥98% (HPLC) SB265610 is a potent and selective CXCR2 chemokine receptor antagonist. It has a Kd = 2.5 nM, and it does not bind to CXCR1.
SML0391 SB-268262 ≥98% (HPLC) SB-268262 is a selective non-peptide antagonist at the CGRP1 receptor. SB-268262 inhibits CGRP binding, and CGRP-mediated stimulation of adenylyl cyclase activity in human neuroblastoma cells with IC50 values of 240 and 830 nM, respectively.
SML1297   SB269652 ≥98% (HPLC) SB269652 is an allosteric modulator of D2 dopamine receptors. SB269652 binds to an allosteric site that is distinct from the orthosteric bound by typical D2 antagonists and is only revealed in D2 receptor dimers. SB269652 is bitopic, binding to an orthosteric site one one partner in the dimer and the allosteric site in the other. Engagement of this secondary pocket at the extracellular end of TM2 and TM7 is a new mechanism of modulating binding of a ligand to the orthosteric site of a second protomer by a G-protein coupled receptor.
S7389 SB-269970 hydrochloride powder, ≥98% (HPLC) SB-269970 is an anti-psychotic agent that shows high affinity for 5-HT7 receptors. It may be effective in treating cognitive disabilities and schizophrenia-like deficits.4 SB-269970 desensitizes and decreases the excitatory effects of 5-HT7 receptors in rat hippocampus.5
Selective 5-HT7 serotonin receptor antagonist.
human ... HTR7(3363)
S5326 SB-271046A ≥98% (HPLC) The first potent and selective 5-HT6 antagonist. Training in cognitive tasks, as well as administration SB-271046, induces an increase in pERK1/2 and pCREB1 levels, while CREB2 levels are significantly reduced; cognition-enhancing properties of SB-271046 are attributed to the effect on pERK1/2, not pCREB1/2. SB-271046 reverses MK-801-induced, but not scopolamine-induced, learning impairments. However, with coadministration of galanthamine, both types of learning impairments were ameliorated.
S4326 SB-277011-A hydrochloride hydrate ≥98% (HPLC) SB-277011-A is a potent, selective brain-penetrant D3 dopamine receptor antagonist; 80-100x selective for D3 over D2; pKi = 7.95 for hD3 receptor.
The D3 dopamine receptor antagonist, SB-277011-A inhibits the cocaine-seeking behavior and cocaine-enhances brain stimulation reward in in rats. It decreases drug-seeking behavior and may be useful in treatment of cocaine and methamphetamine addiction.
SML1192 SB290157 trifluoroacetate salt ≥97% (HPLC) SB290157 is a selective antagonist of complement anaphylatoxin C3a receptor, a 74 amino acid proinflammatory peptide that is a potent chemotaxin for eosinophils, macrophages and mast cells, and has recently been found to be involved in nonimmunological roles in osteoblast differentiation, angiogenesis, and lipid metabolism. SB290157 is selective for C3aR over C5aR or other chemotactic GPCRs with an IC50 of 200 nM. It effectively blocks C3aR in humans, rat, guinea pig, and mouse.SB290157 was found to inhibit diet-induced obesity, metabolic dysfunction, and adipocyte signaling, in addition to inhibiting macrophage signaling.
SML0201 SB 297006 ≥98% (HPLC) SB 297006 inhibits the recruitment and migration of eosinophils in allergen models of models. It suppresses the Th2-mediated eosinophil infiltration in the airways.
SB-297006 is a potent, selective CCR-3 antagonist (IC50 = 60 nM). The compound blocked CCR3 agonist-induced calcium mobilization in CCR3 expressing cells with the following IC50 values: eotaxin, 210 nM; eotaxin-2, 90 nM and MCP4, 80 nM.
SML0207 SB 328437 ≥98% (HPLC) SB 328437 inhibits the recruitment and migration of eosinophils in allergen models of models. It suppresses the Th2-mediated eosinophil infiltration in the airways.
SB-328437 is a potent, selective CCR-3 antagonist (IC50 = 1.6 nM). The compound blockes CCR3 agonist-induced calcium mobilization in CCR3 expressing cells with the following IC50 values: eotaxin, 38 nM; eotaxin-2, 35 nM and MCP4, 20 nM.
SML1530 SB-334867 ≥98% (HPLC) Lateral hypothalamic orexin neuron activation leads to the development of morphine conditioned place preference, which is preferably blocked by SB-334867.
SB-334867 is a non-peptide selective antagonist of the orexin OX1 receptor. SB-334867 blocks orexin-A induced calcium response with a pKb of 7.23. SB-334867 blocks increases in heart rate and body temperature induced by administratin of methamphetamine, and can inhibit the development of tolerance to the analgesic properties of morphine in rodent models. SB-334867 also shows anxiolytic and sedative effects.
S0441 SB-366791 ≥98% (HPLC), powder SB-366791 might exhibit analgesic properties on bone cancer-related pain behavior.
Vanilloid receptor-1 (TRPV1) antagonist.
human ... TRPV1(7442)
SML0604   SB-399885 hydrochloride ≥98% (HPLC) SB-399885 is a potent, selective, and orally active 5-HT6 receptor antagonist with greater than 200 fold selectivity over other 5-HT receptors. SB-399885 is brain penetrant and displays antidepressant and anxiolytic activity in rodent models.
S1326 SB−3CT ≥98% (HPLC), powder SB-3CT is a potent matrix metalloproteinase MMP-2 and MMP-9 inhibitor. Matrix metalloproteinases (MMPs) are involved in a number of activities including angiogenesis and embryogenesis. In particular, gelatinases A (MMP-2) and B (MMP-9), are thought to facilitate tumor metastasis. SB-3CT exhibits a covalent mechanism based behavior in inhibition of MMP-2 and MMP-9. This inhibitor appears to have similarity to TIMP-1 and TIMP-2 in the slow-binding component of inhibition. SB-3CT has been shown to directly bind to the zinc in the catalytic site of MMP-2. SB-3CT does not affect the activities of MMP-1 (Ki = 206 μM) MMP-3 (Ki = 15 μM), or MMP-7 (Ki = 96 μM).
SML2636 Sb4 ≥98% (HPLC) Sb4 is a cell penetrant, potent bone morphogenetic protein (BMP) signaling agonist that rapidly activate BMP in human renal cells (HEK293). Sb4 activates BMP by stabilization of intracellular p-SMAD-1/5/9. Apparently activation of the BMP pathway by sb4 cannot be reversed by inhibition of Noggin or type I BMP kinase inhibitors
S2694 SB-408124 ≥98% (HPLC), solid SB 408124 is an OX1 orexin receptor antagonist.
SB-408124 blocks the orexin type 1 receptor that stimulates the production of stress hormone in hypothalamus. It blocks orexin A-induced increase in arterial pressure and elevation of heart rate in rats. SB-408124 modulates phrenic nerve activity that is important in respiration.
S3567 SB 415286 ≥98% (HPLC) Glycogen synthase kinase-3 (GSK-3) inhibitor.
SB 415286 is a small molecule inhibitor of GSK-3 in muscle and fat cells. SB 415286 induces activation of glycogen synthase and regulates the transport glucose. SB 415286 reduces the systemic inflammation induced by endotoxic shock in rat model of acute colitis. It increases the axonal growth and promotes the recovery of injured adult CNS neurons. SB 415289 is implicated in inducing chromosome instability when used as therapeutic agents.
human ... GSK3A(2931), GSK3B(2932)
S4317 SB 431542 hydrate ≥98% (HPLC), powder Potent and selective inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors.
SB-431542 inhibits the TGF-β-mediated activation of SMAD proteins, expression of collagen and fibronectin, cell proliferation and cell motility. It does not inhibit kinases that are activated in response to serum or stress such as ERK, p38 or JNK.
SML0890   SB 452533 ≥98% (HPLC) SB-452533 acts as a competitive inhibitor at the capsaicin binding site on the transient receptor potential channel TRPV1 receptor with a pKb of 7.7 versus capsaicin and pIC50 of 7.0 versus pH. At higher concentrations, SB-452533 is also active at TRPM8 with an IC50 of 571 nM. It has a high clearance rate, so is not suitable for in vivo use.
S4696 SB-505124 hydrochloride hydrate ≥98% (HPLC) SB-505124 is an inhibitor of activin receptor-like kinase (ALK) 5, also known as transforming growth factor-α type I receptor kinase, with an IC50 of 47 ± 5 nM.
SB-505124 selectively inhibits TGF-β type I receptors, activin receptor-like kinases (ALK) 4, 5 and 7. It inhibits ALK4-, 5- and 7-mediated activation of Smad2, Smad3 and MAPK pathway induced by TGF-β.1 SB-505124 inhibits the human fibroblast trans-differentiation induced by the co-culture with Esophageal squamous cell carcinoma.2
S8822 SB-525334 ≥98% (HPLC) SB-525334 blocks the activation of Smad2/3 induced by TGFβ1 in renal proximal tubule cells.4 The sensitivity of TGFβ1 is decreased by SB-525334 that benefits the pulmonary arterial hypertension condition by reversing the pulmonary arterial pressure.5 SB-525334 is reduces the tumor incidence and size of mesenchymal tumors such as uterine leiomyoma.6
SB-525334 is a potent activin receptor-like kinase (ALK5)/ type I TGFβ-receptor kinase inhibitor with IC50 = 14.3 nM.
SML0501 SB-590885 ≥98% (HPLC) SB-590885 is a potent and selective ATP competitive inhibitor of B-Raf kinase with Kd = 300 pM for B-Raf, and >1000-fold selectivity over a panel of 22 commonly studied cellular kinases
SML0571   SB-612111 hydrochloride ≥98% (HPLC) SB-612111 is a potent antagonist of the nociceptin receptor ORL-1. SB-612111 binds to ORL-1 with high affinity (Ki = 0.33 nM) but has very low affinity for classic opioid receptors. The compound SB-612111 antagonizes the anti-morphine effects of nociceptin and blocks nociceptin-induced thermal hyperalgesia.
S7326 SB 657510 ≥98% (HPLC) SB 657510 slows development of diabetes-associated atherosclerosis in mouse model of diabetes.1
SB-657510 is a selective urotensin-II (UT) receptor antagonist. Human urotensin-II (hU-II) is proposed to play a significant role in cardiorenal and metabolic disease states, including heart failure, atherosclerosis, hypertension.
S0946 SB-668875 ≥95% (HPLC), solid SB-668875 is a novel, selective peptide agonist at OX2 orexin receptors. SB-668875 possesses advantages over Orexins A and B which are equipotent at OX2 orexin receptors. The orexins can cause direct and reversible depolarisation of the postsynaptic membrane. The rank order of potencies of orexin receptor agonists to excite serotonergic DRN neurones is orexin-A = orexin-B > SB-668875-DM. In contrast, the rank order of potency of these agonists to excite noradrenergic locus coreleus (LC) neurones is orexin-A > orexin-B > SB-668875-DM.
SML0912   SB 674042 ≥98% (HPLC) SB-674042 is potent and selective OX1R antagonist. SB-674042 binds with high affinity to OX1R and mediates intracellular calcium flux in OX1R-expressing cells.
SML0853   SB 699551 dihydrochloride ≥98% (HPLC) SB 699551 dihydrochloride is also known as (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4′-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride). It is considered as a useful tool to explain the physiological roles of the 5-ht5A receptor.
SB-699551 is a 5-HT5A receptor antagonist, (pKi = 8.3) with 100-fold selectivity over other 5-HT receptor populations. SB-699551 completely blocks 5-HT-induced [35S]GTPγS membrane binding in cells expressing recombinant guinea pig 5-HT-5A.
SML1121 SB743921 hydrochloride ≥98% (HPLC) SB743921 is an inhibitor of kinesin spindle protein (KSP) with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4, and CENP-E.
SML1712 SBC-115076 ≥98% (HPLC) SBC-115076 is an inhibitor of PCSK9 (proprotein convertase subtilisin-kexin 9). PCSK9 binds to the LDL receptor, preventing it from removing LDL cholesterol from the blood. SBC-115076 was shown to inihbit PCSK9, blocking LDLR degradation in HEK293T cells expressing PCSK9 and to increase the uptake of LDL by liver cells in vitro. SBC-115076 lowered cholesterol levels in mice fed a high fat diet.
SML0012 SBE 13 hydrochloride ≥98% (HPLC) SBE13 is a cell-permeable highly potent polo-like kinase (Plk1) inhibitor that targets the inactive conformation of the kinase. SBE13 does not effect the activity of Plk2, Plk3, Aurora A kinases.
SML1054 SBI-0087702 ≥98% (HPLC) SBI-0087702 promotes the cytoplasmic localization of ATF2 in melanoma cells. SBI-0087702-induced translocation of ATF2 to the mitochondria results in increased apoptosis due to loss of mitochondrial membrane integrity. SBI-0087702 also inhibits growth and motility of melanoma cells. SBI-0087702 was shown to inhibit ATF2 phosphorylation on Thr52 by PKCε.
SML1540 SBI-0206965 ≥98% (HPLC) SBI-0206965 is a potent and selective inhibitor of the serine/threonine autophagy-initiating kinases ULK1 and ULK2 with selectivity for ULK1. SBI-0206965 has an IC50 value of 108 nM for ULK1, compared to 711nM for ULK2. Tumor cells require autophagy to remove misfolded proteins or damaged cellular organelles. SBI-0206965 was shown to suppress autophagy induced by mTOR inhibition. mTOR signaling is often hyperactive in many tumors and can drive proliferation, so mTOR inhibitors are being investigated as anticancer agents. However, mTOR inhibition also results in activation of the ULK1-dependent autophagy survival response, and most results with mTOR inhibitors have been at best cytostatic. SBI-0206965 synergizes with mTOR inhibition to induce apoptosis and cell death.
Since most of the tumor cells survive on autophagy mechanism, inhibition of autophagy inducers Unc-51 (serine/threonine-protein kinase)-like autophagy activating kinase (ULK1 and ULK2) might be useful in cancer therapy.
SML1645 SBI-0640756 ≥98% (HPLC) SBI-0640756 is a potent inhibitor of eIF4G1 that disrupts the eIF4F complex assembly independently of mTOR. SBI-0640756 potently inhibits growth of BRAF-resistant and BRAF-independent melanomas including NRAS- and NF1-mutant melanomas. SBI-0640756 exhibits low toxicity against nontransformed fibroblasts. SBI-0640756 also suppressed AKT and NF-kB signaling.
SML2791 SBI-797812 ≥98% (HPLC) New SBI-797812 is a cell penetrant and potent activator of nicotinamide phosphoribosyltransferase (NAMPT) that increases intracellular levels of NMN and NAD+ in cells. SBI-797812 blocks binding of inhibitors to NAMPT and shifts the reaction equilibrium towards NMN formation. It elevates levels of NAD+ in mice liver.
SML0858   SC-1 ≥98% (HPLC) SC-1 is a derivative of the multiple tyrosine kinase inhibitor sorafenib with no kinase-inhibition activity. SC-1 blocks STAT3 phosphorylation and activation with similar potency to sorafenib, and induces apoptosis in hepatocellular carcinoma cell lines.
SML0763   SC144 hydrochloride ≥98% (HPLC) SC144 is a potent inhibitor of glycoprotein 130 (gp130). SC144 binds to gp130 and blocks STAT3 phosphorylation, nuclear translocation and expression of STAT3 responsive genes. SC144 inhibits the growth of several tumor cell lines, independent of p53 or hormone receptor levels, and inhibits growth of ovarain tumor xenografts in mice.
S3065 SC 19220 ≥98% (HPLC), solid EP1 Prostanoid receptor antagonist
SC 19220 is a competitive antagonist of prostaglandin E receptors. It competes with PGE2 in regulating vesicourethral motility and increases the bladder capacity of rats. It inhibits the contraction of smooth muscles in response to prostaglandins E2 and F. SC 19220 also inhibits the formation of osteoclasts induced by vitamin D3, parathyroid hormone, IL-11 and IL-6.
human ... PTGER1(5731)
rat ... Ptger1(25637)
P7495 SC 22716 ≥98% (HPLC) Cell-permeable leukotriene A4 (LTA4) hydrolase inhibitor that suppresses LTB4 production. Implicated in the pathogenesis of a number of diseases including inflammatory bowel disease and psoriasis.
human ... LTA4H(4048)
PZ0106 SC-236 ≥98% (HPLC) SC-236 is a cyclooxygenase-2 (COX-2) inhibitor.
PZ0176 SC-26196 ≥98% (HPLC) SC-26196 is a Delta6 fatty acid desaturase (Delta6D) inhibitor. It specifically inhibited Delta6D activity with an IC(50) value of 100 nM. The rate-limiting step in arachidonic acid synthesis is the desaturation of dietary linoleic acid by Delta6D. SC-26196 completely prevented this conversion of linoleic acid to arachidonic acid.
PZ0138 SC-51089 hydrate ≥98% (HPLC) SC-51089 is a selective EP1 prostanoid receptor antagonist.
PZ0132 SC-51322 ≥98% (HPLC) SC-51322 is a selective EP1 prostanoid receptor antagonist.
SML0557   SC-514 ≥97% (HPLC) SC-514 is a cell-permeable, potent and selective ATP competitive inhibitor of nuclear factor kappa-B kinase-2 (IKK-2) that specifically blocks NF-?B-dependent gene expression. SC-514 exhibits anti-inflammatory properties.
SC-514 is an amino-acetamide compound. It is selective for IKKβ with an IC50 value of 3−12 μM. SC-514 also inhibits cytokines such as interleukin-6 (IL-6) and IL-8, mediated by IKKβ. IKKβ is responsible for osteoclast survival, hence its inhibition affects osteogenesis.
S2064 SC-560 ≥98% (HPLC) SC-560 (5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole) is a non-steroidal anti-inflammatory drug (NSAID). It is a lipophilic, diaryl heterocyclic compound. SC-560 acts as an effective antiviral agent against hepatitis C virus (HCV). It also has a potential to hinder prostaglandin E2 synthesis in neurons at nanomolar concentrations.
SC-560 belongs to the diaryl heterocycle class of cyclooxygenase (COX) inhibitors. It exhibits anti-tumor and anti-proliferative activities.
Selective cyclooxygenase-1 (COX-1) inhibitor, exhibiting 700-fold selectivity for COX-1 over COX-2.
human ... PTGS1(5742), PTGS2(5743)
PZ0110 SC-57461A ≥98% (HPLC) SC-57461A is an inhibitor of leukotriene A4 hydrolase.
PZ0139 SC-58125 ≥98% (HPLC) SC-58125 is a selective cyclooxygenase 2 (COX-2) inhibitor.
SML0261 SC66 ≥98% (HPLC) SC66 is an allosteric inhibitor of Akt that prevents binding of PIP3 to the PH domain. The compound prevents activation of Akt by PIP3, and also facilitates ubiquination and degradation of Akt. SC66 inhibition is maintained against a cancer relevant Akt mutation (E17K) that is resistant to the actions of PIP3K inhibitors. SC66 is active in vivo, and significantly inhibits the ability of HEK293T cells to form colonies in soft agar and tumor growth in nude mice.
SML2382 SC75741 ≥97% (HPLC) SC75741 (4SC-301; V1810) is a potent NF-kappaB (NF-κB) inhibitor (IC50 = 200 nM against 10 ng/mL TNF-α-induced NF-κB reporter gene expression in A549 cells) that impairs p65 subunit (RelA) DNA-binding activity without affecting p65 phosphorylation or nuclear translocation, nor proteasome-mediatted IκBα degradation. SC75741 induces apoptosis in multiple myeloma cultures (IC50 from 5 to 12 μM in 48 hrs; OPM2, U266, NCI-H929, RPMI-8226), but not PBMCs (89% viability post 4-hr 100 μM SC75741 treatment). NF-κB inhibition by SC75741 treatment is reported to effectively block influenza virus propagation both in cultures in vitro (1-5 μM) and in mice in vivo (5 mg/kg daily i.v. or 7.5-15 mg/kg twice a day i.p.).
SML0749   SC79 ≥97% (NMR) SC79 is an AKT activator. SC79 binds to the plecktrin homology (PH) domain of Akt that mimics the binding of PtdIns(3,4,5)P3 to induce a conformational change in Akt that enhances phosphorylation and activation. SC79 induces cytosolic Akt signaling in cell based assays, and prevents neuronal death in a mouse model of stroke.
S4063 SCH-202676 hydrobromide 98% Allosteric agonist and antagonist of G-protein coupled receptors (GPCRs).
SCH-202676 inhibits the binding of both agonists and antagonists to G protein-coupled receptors. It also inhibits human μ-, δ-, and κ-opioid, α- and β-adrenergic, muscarinic M1 and M2, and dopaminergic D1 and D2 receptors. Some reports indicates thiol modification as the mechanism of inhibition rather than allosteric modulation.
D054 R(+)-SCH-23390 hydrochloride ≥98% (HPLC), solid R(+)-SCH-23390 hydrochloride is a selective D1 dopamine receptor antagonist. It has greater binding capacity towards 5-hydroxytryptamine 2 (5-HT2) and 5-HT1C serotonin receptor subtypes in in vitro. R(+)-SCH-23390 has a half-life of about 25 minutes after administration. It is known to possess anti-stereotypic effect and cataleptogenic effect. It also has inhibitory effect on motor activity.
human ... DRD1(1812)
S4443 SCH-28080 ≥98% (HPLC), solid SCH-28080 is a potent inhibitor of gastric H+ and K+-ATPase. The novel antiulcer agents, SCH-28080 and SCH-32651 were examined for their ability to inhibit the H+K+ ATPase enzyme activity in a preparation of microsomal membranes from rabbit fundic mucosa. SCH- 28080 inhibited the isolated enzyme activity with a potency similar to omeprazole, IC50s of 2.5 and 4.0 μM respectively. SCH 32651 was less potent exhibiting an IC50 of 200.0 μM. Both compounds may therefore exert their antisecretory activity via a direct inhibition of the parietal cell H+K+ ATPase.
SML2591 SCH-39166 hydrobromide ≥98% (HPLC) SCH-39166 (ecopipam) is a high-affinity D1/D5 subtype-selective dopamine receptor antagonist (Ki = 1.2 nM/D1, 2.0 nM/D5, 980 nM/D2, 5.52 μM/D4, 80 nM/5-HT, 731 nM/α2a). SCH-39166 is widely employed both in cultures and in animal studies in vivo.
S6451 SCH-442416 ≥98% (HPLC) SCH-442416 potent and selective Adenosine A2a antagonist. SCH-442416 is >10,000-fold selective for A2a compared to other adensosine receptors.
SML1040   SCH-50911 ≥95% (HPLC) SCH-50911 is a selective, competitive, orally active GABAB receptor antagonist.
S4568 SCH 58261 ≥98% (HPLC), solid A2A adenosine receptor antagonist.
SCH 58261 reduces the levels of TNF-α, Fas-L, Bax expression and activation of JNK-MAPK pathway. It has neuroprotective effects as it reduces demyelination of the neurons. SCH 58261 increases the concentration of secretion of dopamine and elicits locomotor sensitization, an attractive option in the possible treatment of Parkinson′s disease.
SMB00323 Schisandrin C ≥98% (HPLC) Schisandrin C has anti-inflammatory effects and has been shown to reduce nitric oxide (NO) production.
SML0054 Schizandrin ≥98% (HPLC) Schizandrin is a natural product with several biological properties involved with antioxidant and anti-inflammatory activities. It reduces the formation of ROS, inhibits the mitochondrial pathway of the apoptotic process and oxidative stress. Schizandrin has been reported to have hepatoprotective, antitumor, antiviral, and antiamnesic effects, and has neuroprotective activity against glutamate induced neurotoxicity.
S1875 (−)-Scopolamine hydrobromide trihydrate ≥98% (HPLC), powder Competitive nonselective muscarinic acetylcholine antagonist. Scopolamine-induced amnesia in laboratory animals is a commonly-used model of memory deficit.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
S7882 (−)-Scopolamine N-butyl bromide ≥98% (TLC), powder Scopolamine is an anti-muscarinic and cholinolytic alkaloid that inhibits parasympathetic-cholinergic system.5 The central effects include hallucinations, disorientation, restlessness and euphoria.6 Scopolamine disturb the stimulus detection performance in rats by interfering with the reticular cholinergic pathways.7
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
S8502 (−)-Scopolamine methyl bromide ≥98% (HPLC), powder Scopolamine is an anti-muscarinic and cholinolytic alkaloid that inhibits parasympathetic-cholinergic system.7 The central effects include hallucinations, disorientation, restlessness and euphoria.8 Scopolamine disturb the stimulus detection performance in rats by interfering with the reticular cholinergic pathways.9
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
V9752   Scorpion venom from Centruroides sculpturatus    
V5251   Scorpion venom from Leiurus quinquestriatus (north Africa)    
SML1546 SCR7 pyrazine ≥98% (HPLC) SCR7 pyrazine is reported to be an inhibitor of non-homologous end joining (NHEJ) and has been shown to enhance the efficiency of CRISPR-Cas9 genome editing. The effect of SCR7 pyrazine on the efficiency and targeting precision of CRISPR applications has been shown to be cell type specific and context dependent. SCR7 pyrazine is a product of spontaneous cyclization of SCR7, first reported by Srivastava, M., et al.
SML2082   Scrambled 10Panx1 trifluoroacetate salt ≥98% (HPLC) SCPanx (10PanxSCR) corresponds to the scrambled version of the pannexin-1 (panx1) inhibitor peptide 10panx1 and serves as a negative control peptide in pannexin-1 inhibitory studies involving 10panx1 treatment both in vitro and in vivo.
S7817 Scriptaid ≥95%, solid Histone deacetylase inhibitor with lower toxicity than trichostatin A; used to enhance protein expression.
Scriptaid inhibits the cell cycle progression of ovarian cancer cells by inducing arrest in G0/G1 and/or G2/M phase. Treatment of cells with scriptaid results in loss of mitochondrial membrane potential and increased acetylation of H3 and H4 histone tails.2 Sciptaid induces expression of γ-globin in human erythroid progenitors via p38 signaling and may be a treatment option for sickle cell disease.3 It enhances the transcriptional activity and protein expression in mouse embryos. This is useful in producing cloned, inbred mouse embryos that develop normally into adulthood with regular reproductive ability.4
SML0014   Scutellarin hydrate ≥98% (HPLC) Scutellarin is a flavonoid that exhibits a number of cardio- and neuro-protective effects. Scutellarin inhibits p38 activity, ERK phosphorylation, and TGF-β expression and fibrosis in a rat myocardial infarct model. In a cerebral ischemia-reperfusion model, the compound reduced infarct volume and neurological deficits by increasing eNOS expression while inhibiting the induction of iNOS.
S7071 SD-208 ≥98% (HPLC), powder SD-208 is TGF-βR I kinase inhibitor with IC50 =49 nM based on direct enzymatic assay of TGFRI kinase (ALK5) activity with a specificity of >100-fold against TGFRII and at least 17-fold over members of a panel of related protein kinases including p38a, p38b, p38d, JNK1, EGFR, MAPKAPK2, MKK6, ERK2, PKC, PKA, PKD, CDC2, and CaMKII.
SD-208 is an inhibitor of TGF β receptor 1 kinase that is reportedly effective against human malignant gliomas. It increases the lytic activity and tumor infiltration by polyclonal natural killer cells, CD8 T cells and macrophages.1
S174 SDZ-205,557 hydrochloride solid Potent, selective 5-HT4 serotonin receptor antagonist.
human ... HTR4(3360)
SML0598 SDZ 220-581 hydrochloride ≥98% (HPLC) SDZ 220-581 is a competitive NMDA receptor antagonist that penetrates the blood brain barrier. ISDZ 220-581 selectively blocks the glutamate recognition-site of the NMDA receptor and reduces prepulse inhibition (PPI). SDZ 220-581 reduces prepulse inhibition (PPI) and has an ED50 of less than 3.2 mg/kg for protection against MES-induced seizures.
S2189 SE 175 ≥97% An organic nitrate compound that acts as an NO donor in vivo following reductive transformation of the nitrate group to nitric oxide.
SE 175 is a nitrate compound that belongs to the same class as nitroglycerine. It acts as a vasodilator and has clinical use in the treatment of angina. NO donors also confer neuroprotection and relieve neuropathic pain.
SML2054 SEA0400 ≥98% (HPLC) SEA0400 is a potent and selective inhibitor of Na+/Ca2+exchanger (NCX). SEA0400 potently inhibits Na+/Ca2+ exchanger activity in rat astrocytes, microglia, cultured neurons, and rat cardiomyocytes.
SML2613 Secnidazole ≥98% (HPLC) Secnidazole is a nitroimidazole anti-microbial selective against many anaerobic Gram-positive and Gram-negative bacteria and protozoa. It has been approved for the treatment of bacterial vaginosis. Secnidazole is a prodrug, whose nitro group is reduced by bacterial enzymes to radical anions that interfere with bacterial DNA synthesis.
S4562   β-Secretase inhibitor ≥97% (HPLC), powder β-Site amyloid precursor protein (APP) cleaving enzyme-1 (BACE1) is a β-secretase that initiates the production of amyloid protein in Alzheimer′s dieases (AD) patients. β-Secretase inhibitors decrease the generation of β amyloid and formation of amyloid plaques typical of AD.
SML0055 Securinine ≥98% (HPLC) Securinine is an alkaloid widely in traditional folk medicine. Long known as a GABAA antagonist, securinine was recently found to up-regulate p53 protein and to modulate the related family member p73 protein in a p53-dependent fashion, inducing p73 in the HCT116 p53(-) cells and down-regulating it in the p53(+) cells. Induction of proapoptotic protein p73 only in p53 cells could be used to target cancer cells preferentially. Securinine has been found to induce p53-independent, p73-dependent apoptosis in RKO colon cancer cells.
SML2663 Selamectin ≥98% (HPLC) Selamectin is a veterinary parasiticide and anthelminthic. Its mechanism of action is by activating glutamate-gated chloride channels at muscle synapses.
S0323 Sematilide monohydrochloride monohydrate ≥98% (HPLC), powder Sematilide monohydrochloride monohydrate is a class III antiarrhythmic; selective delayed rectifier K+ current (IKr) channel blocker. It inhibits rapidly activating Ik in guinea pig atrial myocytes, resulting in the prolongation of action potential duration and refractoriness; shows proarrhythmic effects and may lead to QT interval prolongation.
SML1615 SEN177 ≥98% (HPLC) SEN177 is a Glutaminyl cyclase (QPCT) inhibitor. Glutaminyl cyclase modifies N-terminal glutamine or glutamate residues to N-terminal 5-oxoproline or pyroglutamate (named QPCT). QPCT inhibits mutant huntingtin from forming aggregates, but also reduces aggregation of other aggregate-prone proteins containing polyQ or polyA repeats. SEN177 caused dose-dependent decreases in HTT aggregation by a mechanism that requires QPCT inhibition. SEN177 had in vitro activity against polyglutamine toxicity and was able to reduce aggregates in mammalian cells, primary neurons and in a Drosophila model.
SML1001 Senegenin ≥98% (HPLC) Senegenin (Tenuigenin) is a natural product from Polygala tenuifolia used in Chinese medicine with antioxidative and antiinflammatory activity. Senegenin has been studied for nootropic ability to improve cognition. In several independent studies, Tenuigenin attenuated α-synuclein-induced cytotoxicity and α-synuclein phosphorylation by down-regulating polo-like kinase 3 (PLK3) in α-synuclein cell model of Parkinson′s Disease, improved behavioral Y-maze learning by enhancing synaptic plasticity in mice, and attenuated hepatic ischemia-reperfusion induced cognitive dysfunction by increasing hippocampal N-methyl-D-aspartate (NMDA) receptor NR2B subunit expression in rats.
Senegenin is lipophilic and hydrosoluble. It is chemically represented as (2β,3β,4α,12α)-12-(Chloromethyl)-2,3-dihydroxy-27-norolean-13-ene-23,28-dioic acid. Senegenin plays a protective role against memory impairment in a dose and time dependent manner.
SML2500 Senicapoc ≥98% (HPLC) Senicapoc (ICA-17043) is an inhibitor of the calcium-activated K+ channel KCa3.1, also known as the Gardos channel, which plays a role in K+ loss and dehydration of sickled red blood cells. Senicapoc blocks calcium-induced rubidium flux in human RBCs with and IC50 of 11 nM and prevents RBC dehydration in a transgenic mouse sickle cell disease model. It has been investigated for a number of possible uses, which include antimalarial activity, idiopathic pulmonary fibrosis, glioblastoma, lung cancer, non-alcoholic liver disease, hereditary xerocytosis, suppression of microglial activation in stroke, and immune system disorders.
SML0764   Senktide trifluoroacetate salt ≥95% (HPLC) Senktide is a selective Neurokinin NK3 tachykinin receptor agonist. Neurokinins (tachykinins) are members of a family of at least three neuropeptides, substance P, neurokinin A, and neurokinin B (NKB), with each mediating their biological effects through binding to a preferred G-protein-coupled receptor termed NK1, NK2, or NK3, respectively. All three NK receptors are expressed in regions of the central nervous system that are related to emotion and cognition (i.e., amygdala and hippocampus) and have been linked to various degrees in psychiatric disorders. Neurokinin receptors, including NK3 receptors, are also expressed in the motor and sensory systems of the digestive tract.
Senktide treatment in follicular phase goats enhances the liberation of luteinizing hormone (LH) and advance the time of ovulation. Senktide has the ability to suppress gonadotropin-releasing hormone (GnRH) transcription. Treatment with senktide stimulates c-Fos and improve activator protein-1 (AP-1) activity.
SML1356 Sephin1 ≥95% (HPLC) In vivo studies using mice models show that sephin1 suppresses neurodegeneration, by preventing eIF2α (eukaryotic initiation factor 2) dephosphorylation.
Sephin1 is a selective inhibitor of a holophosphatase. It is a guanabez derivative that binds to and inhibits a regulatory subunit of the stress-induced protein phosphatase 1 (PPP1R15A), but not the constitutive PPP1R15B, and lacks α2-adrenergic activity. Phosphorylation of eIF2α, α subunit of eukaryotic translation initiation factor 2, reduces protein synthesis and prevents the accumulation of misfolded protein in the endoplasmic reticulum (ER). PPP1R15A recruits the serine/threonine-protein phosphatase PP1 to dephosphorylate eIF2α, so inhibiting PPP1R15A activity prolongs the phosphorylation of eIF2α and aids in its prevention of the accumulation of misfolded protein. In vitro Sephin1 protected cells from lethal protein misfolding and cytotoxic ER stress. In vivo sephin1 prevented two unrelated protein misfolding diseases in mice (Charchot-Marie-Tooth 1B and ALS).
SML1379 Seratrodast ≥98% (HPLC) Seratrodast is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist with anti-asthmatic activity. Seratrodast inhibits the bronchconstriction induced by leukotriene D4 (LTD4), and platelet activating factor (PAF) with a long duration of action.
human ... TBXA2R(6915)
H7752 Serotonin creatinine sulfate monohydrate powder Neurotransmitter.
Serotonin creatinine sulfate stimulates neuronal production of catecholamine.
human ... HTR3A(3359)
H9523 Serotonin hydrochloride powder Neurotransmitter.
human ... HTR3A(3359)
H4511 Serotonin hydrogen maleate powder Neurotransmitter.
human ... HTR3A(3359)
SML0888   Sertaconazole nitrate ≥98% (HPLC) Sertaconazole nitrate is an antifungal agent with anti-inflammatory and anti-itch activity. Topical administration of this drug reduces the releases of cytokines from activated T-cell enriched human lymphocytes. Sertaconazole nitrate has been used as a highly safe and effective therapeutic for treating tinea pedis interdigitalis. It is also used to treat contact hypersensitivity and irritant contact dermatitis.
Sertaconazole nitrate is an imidazole antifungal. Like other imidazole antifungals, sertaconazole blocks the synthesis of ergosterol, an essential component of the fungal cell membrane, by inhibiting the P450 enzyme 14α-demethylase that converts lanosterol to ergosterol.
S6319 Sertraline hydrochloride ≥98% (HPLC) Selective serotonin reuptake inhibitor, antidepressant.
Sertraline suppresses platelet function and exhibits antiplatelet and endothelium protective functions. It relieves depression and improves the quality of life in patients with cardiovascular disorders. It can also be prescribed to treat depression in Parkinson′s disease.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363), SLC6A4(6532)
S9314 Sesamin ≥95%, crystalline Non-competitive Δ5-desaturase inhibitor.
Sesamin can lower cholesterol effects in humans. It is involved in preventing high blood pressure and increases vitamin E levels. Sesamin exhibits anti-cancer, anti-proliferative, anti-metastatic and anti-inflammatory properties. It also exhibits pro-apoptotic and pro-autophagocytic properties. Sesamin has its effects on lipid and carbohydrate metabolism. It also has effects on hypertension and free radical scavenging.
SML2610 Seselin ≥98% (HPLC) Seselin is an anti-inflammatory, anti-parasitic and antifungal pyrancoumarin found in anise and other plants. It appears that seselin targets Jak2 to block the proinflammatory phenotype of macrophages in models of sepsis. Seselin down-regulates levels of proinflammatory factors and activity of STAT1 and p65 in models of sepsis.
S3944 SEW2871 ≥98% (HPLC), solid Novel, selective human sphingosine-1-phosphate subtype 1 (S1P1) receptor agonist.
SEW2871 is a selective agonist of spingosine-1 phosphate receptor. It exacerbates reperfusion arrhythmias by significantly prolonging the duration of ventricular tachycardia and ventricular fibrillation. SEW2871 modulates inflammatory reactions by influencing lymphocyte homing and cell migration. By the inhibition of proinflammatory molecules, SEW2871 reduces acute renal failure due to ischemia.
human ... S1PR1(1901), S1PR2(9294), S1PR3(1903), S1PR4(8698), S1PR5(53637)
S6701 SF-11 ≥98% (HPLC) Radioligand studies reveal that SF-11 also targets 5-HT2B and dopamine transporter.1
SF-11 is a potent, selective NPY Y2 receptor antagonist; brain-penetrant.
S5076 SF-22 ≥98% (HPLC) Radioligand studies reveal that SF-22 also targets 5-HT2B and 5-HT6 serotonin receptors and dopamine transporter.1
SF-22 is a potent, selective NPY Y2 receptor antagonist; highly brain-penetrant
SML0684   SF1670 ≥98% (HPLC) PTEN prevents PI3-K(phosphoinositide 3-kinase)/Akt signaling pathway, which is very essential for neuronal regeneration. Therefore, inhibition of PTEN by SF1670 may support neuronal regeneration.
SF1670 is a selective PTEN (phosphatase and tensin homolog) inhibitor with an IC50 of 2 micromolar. PTEN inhibition by SF1670 was shown to increase neutrophil activity (polarization, phagocytosis, oxidative burst, and recruitment to site of infection), thereby enhancing the inflammatory response and bacteria-killing capacity of neutopenic mice.
S5071 SFK1 ≥98% (HPLC), solid SFK1 interacts directly with yeast mitochodria. Induces cell death in low salt conditions and suppresses the ability of FK506 to inhibit cell growth in the presence of high levels of NaCl.
S8701 SFLLR-NH2 trifluoroacetate salt ≥95% (HPLC), powder SFLLR-NH2 is a PAR-1 (Protease-Activated Receptor) selective activating peptide, also known as Thrombin Receptor Activating Peptide 5 (TRAP-5). Protease-activated receptors (PARs) are present on various organs including, platelets, mast cell, gallblader, oesophagus etc, and regulate various physiological processes including human platelet aggregation, vascular contraction/relaxation, and an increase in endothelial permeability. Recent papers indicated that PAR′s are also involved in sensory processing and proliferation of astrocytes.
S6193 SG-209 solid, ≥98% (HPLC) Potassium channel activator; analog of nicorandil; nitrate-free coronary vasodilator
SG-209, a derivative of nicorandil, opens up potassium channels and leads to vasodilation. It dilates tracheal smooth muscle and increases the blood flow to the trachea in dogs.3
SML1107 SGC0946 ≥98% (HPLC) SGC0946 is a potent and selective inhibitor of Histone H3-lysine79 (H3K79) methyltransferase DOT1L with an IC50 of 0.3 nM in a radioactive enzyme assay, and over 100-fold selectivity for DOT1L over other histone methyltransferases. In cell studies, SGC0946 reduces H3K79 dimethylation with an IC50 of 2.6 nM in A431 cells and 8.8 nM in MCF10A cells. SGC0946 was found to selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro model of leukemia. For full characterization details, please visit the SGC0946 probe summary on the Structural Genomics Consortium (SGC) website.

SGC0649 is the negative control for the active probe, SGC0946. To request a sample of the negative control from the SGC, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML2343 SGC3027 ≥98 mg/mL (HPLC) SGC3027 is a selective and cell-active inhibitor of protein arginine N-methyltransferase (PRMT7) It is a pro-drug of the active component, SGC8158, which is produced in the cell by reductases. SGC8158 was shown to inhibit PRMT7 with an IC50 value < 2.5 nM for methylation of H2B (23-37) and greater than 40-fold selectivity over other histone methyltransferases and non-epigenetic targets. SGC3027 inhibited the methylation of HSP70 In cellular assays using C2C12 cells with an IC50 value of 1.3 microM. The closely related SGC3027N is significantly less active in the cellular assay, and is a control compound for cellular studies.
SML2342 SGC3027N ≥98% (HPLC) Control probe for PRMT7 inhibitor SGC3027
SGC3027N is the control probe for the PRMT7 inhibitor SGC3027
SML1242 SGC707 ≥98% (HPLC) SGC707 is a potent allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). SGC707 has an IC50 value of 50 nM and >100-fold selectivity over other methyltransferases and non-epigenetic targets. SGC707 binds to PRMT3 with KD of 50 nM (ITC), and inhibits histone methylation in cells with an IC50 value below 1 μM. For full characterization details, please visit the SGC707 probe summary on the Structural Genomics Consortium (SGC) website.

XY1 is the negative control for the active probe, SGC707. To request a sample of the negative control from the SGC, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML2340 SGC8158 ≥98% (HPLC) New SGC8158 isthe active component produced by cell reductases from the prodrug, SGC3027, a selective and cell-active inhibitor of protein arginine N-methyltransferase (PRMT7). SGC8158 was shown to inhibit PRMT7 with an IC50 value < 2.5 nM for methylation of H2B (23-37) and greater than 40-fold selectivity over other histone methyltransferases and non-epigenetic targets. SGC3027 inhibited the methylation of HSP70 In cellular assays using C2C12 cells with an IC50 value of 1.3 microM. The closely related SGC3027N is significantly less active in the cellular assay, and is a control compound for cellular studies.
SML2219 SGC-AAK1-1 ≥98% (HPLC) SGC-AAK1-1 is an ATP-competitive kinase inhibitor against AP2-associated protein kinase 1/AAK1 and BMP-2-inducible protein kinase/BIKE/BMP2K (Ki = 9.1 & 17 nM, respectively, by ATP site fluorescent tracer displacement assay; AAK1 IC50 = 270 nM by coupled enzyme assay). SGC-AAK1-1 downregulates cellular AP2M1 Thr156 phosphorylation level in a dose-dependent manner (ECmax ∼12.5 μM) without detectable cytotoxicity. Selectivity profiling identifies only 5 additional kinases among a panel of ∼400 with >50% inhibition by 1 μM SGC-AAK1-1 (KD = 72 nM/RIOK1, 290 nM/RIOK3, 260 nM/PIP5K1C, 880 nM/CDKL1, 960 nM/MYLK2 by DiscoverX KINOMEscan). SGC-AAK1-1N is a structure analog and the recommended negative control (IC50 = 11 μM by AAK1 activity assay; KD = 8.8 μM/AAK1 & >10 μM/BIKE vs. KD = 26 nM/AAK1 & 930 nM/BIKE with SGC-AAK1-1 by DiscoverX). For characterization details of SGC-AAK1-1, please visit the SGC-AAK1-1 probe summary on the Structural Genomics Consortium (SGC) website.

SGC-AAK1-1N is the negative control for the active probe, SGC-AAK1-1. SGC-AAK1-1N is available from Sigma. To learn more about and purchase SGC-AAK1-1N, click here.

To learn about other SGC chemical probes, visit sigma.com/sgc
SML2220 SGC-AAK1-1N ≥98% (HPLC) SGC-AAK1-1N is a structure analog of and the recommended negative control for SGC-AAK1-1 (AAK1 IC50 = 11 μM and 270 nM, respectively, by coupled enzyme assay; KD = 8.8 μM/AAK1 & >10 μM/BIKE with SGC-AAK1-1N vs. KD = 26 nM/AAK1 & 930 nM/BIKE with SGC-AAK1-1). For characterization details of the active probe, SGC-AAK1-1, please visit the SGC-AAK1-1 probe summary on the Structural Genomics Consortium (SGC) website.

SGC-AAK1-1, the active probe, is available from Sigma. To learn more about and purchase SGC-AAK1-1, click here.

To learn about other SGC chemical probes, visit sigma.com/sgc
SML2834 SGC-CAMKK2-1 ≥98% (HPLC) New SGC-CAMKK2-1 (YL-36) is a potent and selective CaM kinase kinase (CaMKK) inhibitor (CAMKK2 IC50 = 30 nM) that inhibits C4-2 cellular AMPK phosphorylation (IC50 = 1.6 μM) with selective affinity toward CAMKK1/2 over other kinases (404-kinase panel kinome-wide Discoverx screen).
SML2835 SGC-CAMKK2-1N ≥98% (HPLC) New SGC-CAMKK2-1N is an inactive analog of and negative control for the potent and selective CaM kinase kinase (CaMKK) inhibitor SGC-CAMKK2-1 (YL-36). SGC-CAMKK2-1N inhibits CaMKK2 with an IC50 of 27 μM in cell-free assays (IC50 = 30 nM by SGC-CAMKK2-1) and shows no cellular potency.
SML1133 SGC-CBP30 ≥98% (HPLC) SGC-CBP30 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.021 and 0.038 μM, respectively). SGC-CBP30 has little activity against other bromodomains at concentrations up to 1 mM. For full characterization details, please visit the SGC-CBP30 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SGC-CBP30 might serve as a therapeutic agent in treating cancer. In ankylosing spondylitis and psoriatic arthritis condition, SGC-CBP30 is found to decrease immune cell production of T helper cell 17 and other pro-inflammatory cytokines.
SML2202 SGC-GAK-1 ≥98% (HPLC) SGC-GAK-1 (CA93) is an ATP-competitive cyclin G-associated kinase (GAK) inhibitor (Ki = 3.1 nM by ATP site fluorescent tracer displacement assay; KD = 4.5 nM by ITC) that effectively inhibits Dengue viral entry and packaging in cultures (IC50 = 920 nM) without detectable cytotoxicity. SGC-GAK-1 exhibits much reduced affinity toward only 4 other kinases among a panel of ∼400 (KD = 1.9 nM/GAK vs. 110 nM/RIPK2, 190 nM/ADCK3, 520 nM/NLK, 980 nM/AVCR1 by ligand competitive binding assay; IC50 = 110 nM/GAK vs. 360 nM/RIPK2 by cellular target engagement assay). SGC-GAK-1N (CA71) is a structure analog and the recommended negative control (GAK KD = 7.1 μM by ligand competitive binding assay; GAK & RIPK2 IC50 >50 μM by cellular target engagement assay). For characterization details of SGC-GAK-1, please visit the SGC-GAK-1 probe summary on the Structural Genomics Consortium (SGC) website.

SGC-GAK-1N is the negative control for the active probe, SGC-GAK-1. SGC-GAK-1N is available from Sigma. To learn more about and purchase SGC-GAK-1N, click here.

To learn about other SGC chemical probes, visit sigma.com/sgc
SML2203 SGC-GAK-1N ≥98% (HPLC) SGC-GAK-1N (CA71) is a structure analog of and the recommended negative control for the ATP-competitive cyclin G-associated kinase (GAK) inhibitor SGC-GAK-1 (CA93) (GAK KD = 1.9 nM/SGC-GAK-1 vs. 7.1 μM/SGC-GAK-1N by ligand competitive binding assay; GAK IC50 = 110 nM/SGC-GAK-1 vs. >50 μM/SGC-GAK-1N by cellular target engagement assay; Dengue viral entry and packaging IC50 = 920 nM/SGC-GAK-1 vs. >10 μM/SGC-GAK-1N). For characterization details of the active probe, SGC-GAK-1, please visit the SGC-GAK-1 probe summary on the Structural Genomics Consortium (SGC) website.

SGC-GAK-1, the active probe, is available from Sigma. To learn more about and purchase SGC-GAK-1, click here.

To learn about other SGC chemical probes, visit sigma.com/sgc
SML2440 SGC-iMLLT ≥98% (HPLC) SGC-iMLLT (Chemical Probe 92) is a cell penetrant, potent and selective inhibitor of YEATS domain MLLT1/3 histone interaction. SGC-iMLLT downregulates MYC and DDN genes, while increases CD86 in MV4;11 AML cells.
SML1358 SGI-1027 ≥98% (HPLC) SGI-1027 is a DNA methyltransferase (DNMT) inhibitor with IC50 values of 6-13 μM for DNMT3B, DNMT3A and DNMT1. SGI-1027 directly inhibits DNMT activity by competing with the cofactor, S-adenosylmethionine (SAM) in the methylation reaction. SGI-1027 treatment of cancer cell lines induced degradation of DNMT1, but not DNMT3A or DNMT3B, and in RKO cells caused re-expression of the silenced tumor supressor genes p16, MLH1 and TIMP3.
SML1459   SHA 68 ≥98% (HPLC) SHA 68 is a potent and selective neuropeptide S receptor antagonist that exhibits anxiogenic effects.
SML0562 Shiga Toxin 1, B subunit recombinant, expressed in E. coli, ≥95% (SDS-PAGE) The Shiga toxins are a family of related protein toxins secreted by certain types of bacteria. Shiga toxin (Stx) is produced by Shigella dysenteriae, whereas the Shiga-like toxins, Stx1 and Stx2, with a few known isoforms, are secreted by specific strains of Escherichia coli named Shiga-toxin-producing E. coli (STEC) such as E. coli O157:H7, which causes bloody diarrhea and hemorrhagic colitis in humans, sometimes resulting in fatal systemic complications.

Stx1 is identical to Stx, while the Stx2 isoforms share less sequence similarity with Stx (~60%) and are immunologically distinct. In spite of the differences in their amino acid sequence, all Stx isoforms share the same overall toxin structure and mechanism of action.

Shiga toxins consist of two polypeptides: An A chain and a B chain non-covalently associated with an apparent stoichiometry of one A and five B chains, to form the holotoxin. The catalytic A subunit has a RNA N-glycosidase activity that inhibits eukaryotic protein synthesis. The B subunits form a pentamer that recognizes and binds to the functional cell-surface receptor globotriaosylceramide [Gb3; Gala(1-4)-Galb(1-4)-Glcb1-ceramide]. Gb3 is overexpressed in membranes of numerous tumor cells, therefore STxB binding to Gb3 receptors may be useful for cell-specific vectorization, labeling and imaging purposes.
SML0655 Shiga toxin 1, B subunit, HIS-tagged recombinant, expressed in E. coli, ≥95% (SDS-PAGE) The Shiga toxins are a family of related protein toxins secreted by certain types of bacteria. Shiga toxin (Stx) is produced by Shigella dysenteriae; whereas, the Shiga-like toxins, Stx1 and Stx2, with a few known isoforms, are secreted by specific strains of Escherichia coli named Shiga-toxin-producing E. coli (STEC), such as E. coli O157:H7, which causes bloody diarrhea and hemorrhagic colitis in humans, sometimes resulting in fatal systemic complications.

Stx1 is identical to Stx, while the Stx2 isoforms share less sequence similarity with Stx (∼60%) and are immunologically distinct. In spite of the differences in their amino acid sequence, all Stx isoforms share the same overall toxin structure and mechanism of action.

Shiga toxins consists of two polypeptides. An A chain and a B chain non-covalently associate with an apparent stoichiometry of one A and five B chains to form the holotoxin. The catalytic A subunit has
RNA N-glycosidase activity that inhibits eukaryotic protein synthesis. The B subunits form a pentamer, which recognizes and binds to the functional cell-surface receptor globotriaosylceramide [Gb3; Gala(1-4)-Galb(1-4)-Glcb1-ceramide]. Gb3 is overexpressed in membranes of numerous tumor cells, therefore STxB binding to Gb3 receptors may be useful for cell-specific vectorization, labeling, and imaging purposes.
SML2699 SHMT inhibitor Hit 1 ≥98% (HPLC) SHMT inhibitor Hit 1 is a potent and specific inhibitor of serine hydroxymethyltransferase (SHMT). SHMT inhibitor Hit 1 potently inhibits SHMT1 and SHMT2 in rat liver homogenate.
SML1762 SI-2 ≥98% (HPLC) SI-2 targets the receptor-interacting domain (RID) of steroid receptor coactivators (SRCs) and suppresses cellular transcriptional activity (Effec. conc. >/= 5 nM in cell-based SRC-1, SRC-2, and SRC-3 reporter assays) by downregulating SRCs protein, but not transcript level (Effec. conc. >/= 12.5 nM against SRC-3, >/= 25 nM against SRC-1 and SCR-2 in MDA-MB-468 culture). SI-2 is cytotoxic to breast cancer cultures (IC50 = 1.5 nM/BT-474, 3.4 nM/MDA-MB-468, 22 nM/MCF-7), but not to normal hepatocytes even at 500 nM concentration. SI-2 is reported to be orally available in mice and, when administered intraperitoneally (2 mg/kg b.i.d.), effectively suppress MDA-MB-468-derived tumor expansion in mice in vivowith good pharmacokinetics (Cmax = 30 μM, tmax = 0.25 h, t1/2 = 1.0 h; 20 mg/kg i.p.) and no apparent adverse effects to the animals.
S9186 SIB 1757 ≥99% (HPLC), crystalline SIB 1757 is a highly selective mGluR5 metabotropic glutamate receptor antagonist. It non-competitively inhibits glutamate-induced increase in Ca2+ at human metabotropic glutamate receptor 1 (hmGluR1).1 Inhibition of mGlu5 receptor renders protection to neurons2 against methamphetamine-induced oxidative damage.3
human ... GRM1(2911), GRM5(2915)
S9311 SIB 1893 >99%, solid SIB 1893 non-competitively inhibits glutamate-induced increase in Ca2+ at human metabotropic glutamate receptor 1 (hmGluR1).1 It also acts as a positive allosteric modulator of hmGluR4.2
Selective and noncompetitive mGlu5 metabotropic glutamate receptor antagonist.
human ... GRM1(2911), GRM5(2915)
S9944 Sibutramine hydrochloride monohydrate ≥98% (HPLC), solid Sibutramine is a serotonin and noradrenaline reuptake inhibitor (SNRI). It is an antiobesity drug, which decreases calorie intake and increases energy expanditure. Sibutramine antagonizes MPTP-induced dopamine depletion in mouse brain.
human ... SLC6A2(6530), SLC6A3(6531), SLC6A4(6532)
SML1518 SID 3712249 ≥95% (HPLC) SID 3712249 (MiR-544 Inhibitor 1) is an inhibitor of the biogenesis of microRNA-544 (miR-544). MiR-544 represses expression of mTOR, promoting tumor cell survival in a hypoxic environment. Inhibition of miR-544 processing with MiR-544 Inhibitor 1 caused apoptosis in triple negative breast cancer cells in response to hypoxic stress, sensitized their response to 5-fluorouracil, and blocked their growth after transplantion into immunodeficient mice. SID 3712249 (MiR-544 Inhibitor 1) is believed to bind directly to the precursor miRNA, blocking production of the mature microRNA and resulting in decreased miR-544, HIF-1α, and ATM transcripts. MiR-544 Inhibitor 1 was as selective and 25-fold more potent than a 2′-O-methyl RNA antagomir.
S1323 SID7969543 ≥98% (HPLC), solid SID7969543 is a SF-1 (or NR5A1) inhibitor. The Steroidogenic Factor 1 (SF-1, also known as NR5A1) is a transcription factor belonging to the nuclear receptor superfamily. It plays a central role in sex determination and the formation of steroidogenic tissues during development, and is involved in endocrine function throughout life. It has also been reported to have a potential role in obesity. It has also been observed that an increased concentration of SF-1 causes adrenocortical cell proliferation and cancer.
S3451 SID 852843 ≥98% (HPLC) SID 852843 is an inhibitor of West Nile Virus NS2B-NS3 proteinase. Flaviviruses, such as West Nile and Dengue, are a threat to humans from both public health and bioterrorism perspectives. The NS3 proteinase is essential for flaviviral maturation. Inhibitors of NS3 are sought for treatment and prophylactic therapeutics. The NIH molecular library was screened for activity against West Nile Virus NS3, resulting in the discovery of SID 852843. This compound inhibits the NS3 proteinase of West Nile, but not of Dengue type 2 virus. SID 852843 is a reversible, allosteric inhibitor of the formation of the functional conformation of the NS3 proteinase. This is the first flaviviral proteinase inhibitor with the potential to lead to a drug. Aprotinin is an efficient inhibitor of NS3, but it is not selective and has low penetration into cells, limiting its potential for therapeutic use.
SML2142 Silodosin ≥98% (HPLC) Silodosin is a selective alpha 1-adrenoceptor antagonist with high affinity for the ?1A adrenergic receptor, used clinically for the treatment of benign prostatic hyperplasia (BPH).
S6196 Simvastatin ≥97% (HPLC), solid Simvastatin is a specific inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early step in cholesterol biosynthesis. It is used in the treatment of hypercholesterolemia, as it reduces levels of low-density lipoproteins and triglycerides, and raises high-density lipoprotein levels. Simvastatin is a lactone that is readily hydrolyzed in vivo to the corresponding β-hydroxyacid, and can be activated prior to use with NaOH in EtOH treatment. It is a synthetic analog of lovastatin (Cat. No. M2147).
Simvastatin is a specific inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early step in cholesterol biosynthesis. It is used in the treatment of hypercholesterolemia, as it reduces levels of low-density lipoproteins cholesterol and triglycerides, and raises high-density lipoprotein levels. Simvastatin is a lactone that is readily hydrolyzed in vivo to the corresponding β-hydroxyacid and can be activated prior to use with NaOH in EtOH treatment. It may also have beneficial effects on endothelial function, inflammation, smooth muscle cell function, vascular wall function, hemostasis and LDL oxidation.
human ... HMGCR(3156)
rat ... Hmgcr(25675)
S8559 Sinefungin 95% (HPLC), powder Sinefungin blocks the methylation of bases in DNA and RNA, such as 5-methylcytosine or N6-methyladenosine, suggesting a role in gene expression. In addition, sinefugin is involved in physiological processes such as aging and carcinogenesis.
Sinefungin blocks the methylation of bases in DNA and RNA, such as 5-methylcytosine or N6-methyladenosine, suggesting a role in gene expression. In addition, sinefugin is involved in physiological processes such as aging and carcinogenesis.
Methylation inhibition by sinefugin is often accompanied by an altered rate of cytosine deamination that is coupled to transition mutation in the DNA. Sinefugin inhibits Epstein-Barr viral activity and this inhibition is related to the change in DNA methylation and gene expression. It can cause a rate change in several restriction DNA endonuclease activities, including Mme I, which is not connected to the inhibition of the methytransferase activity.
SML1787 Sinensetin ≥98% (HPLC) Sinensetin is a citris flavonoid with anti-inflammatory and anti-proliferative activity. It has also been shown to enhance adipogenesis and lipolysis.
SML1002 Sinomenine hydrochloride ≥98% (HPLC) Sinomenine is a herbal medicine used to treat inflammatory diseases like rheumatoid arthritis. Sinomenine had anti-inflammatory effects in several animal models of inflammation, and inhibits mast cell degranulation and histamine release. Additionally, Sinomenine potentiates renewal of human embryonic stem cells.
SML0976   Siramesine fumarate salt ≥98% (HPLC) Siramesine is a blood-brain barrier penetrant, selective and potent sigma-2 receptor agonist, which exhibits potent and very long-lasting anxiolytic effects in rodents. Also, siramesine is a lysosome-destabilizing agent that causes lysosomal cell death in varies immortalized and cancer cell lines.
Siramesine or Lu 28-179 (1′-[4-[1-(4-fluorophenyl)-1H-indol-3-yl]-1-butyl]-spiro[isobenzofuran-1(3H),4′-piperidine]) is considered as a drug for depression and anxiety. This lysosomotropic agent stimulates mitochondrial membrane potential (MMP) reduction and the production of ROS (reactive oxygen species).
S7942 Sirtinol ≥95% (HPLC) Sirtinol inhibits yeast Sir2p transcriptional silencing activity in vivo, yeast Sir2p and human SIRT2 deacetylase activity in vitro. It inhibits the physiological regulators of platelet aggregation such as thrombin and collagen, attenuates intracellular Ca2+ release and formation thromboxane B2. It may increase levels of cAMP by inhibition of cAMP phosphodiesterase and inhibit the aggregation of platelets.2 Sirtinol reduces inflammatory responses of human dermal microvascular endothelial cells to TNF-α and IL-1β.3
Sirtinol inhibits yeast Sir2p transcriptional silencing activity in vivo, yeast Sir2p, and human SIRT2 deacetylase activity in vitro.
human ... SIRT1(23411), SIRT2(22933)
S0447 SIS3 ≥98% (HPLC), powder SIS3 is a novel specific inhibitor of TGF-β1/ALK-5 phosphorylation of Smad3
Sugar insensitive 3 (SIS3) promotes drug-induced apoptosis and hinders the function of adenosine triphosphate (ATP)-binding cassette (ABC) transporter (ABCB1) and ABCG2. It resensitizes ABCB1 and ABCG2 overexpressed in cancerous cells, which contributes to chemotherapeutics.
SML2744 Sitafloxacin sesquihydrate ≥98% (HPLC) Sitafloxacin (DU-6859 or DU-6859a) is an orally active, fourth generation fluoroquinolone that exhibits broad-spectrum antibiotic activity against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, via dual inhibitory activity against bacterial DNA gyrase and topoisomerase IV (IC50 = 1.16 and 1.88 μg/mL against S. pneumoniae gyrA/B and parC/E, respectively). Sitafloxacin is active against methicillin-resistant staphylococci, Streptococcus pneumoniae and other streptococci with reduced susceptibility to levofloxacin and other quinolones and enterococci. Sitafloxacin also exhibits activity against clinical isolates of Klebsiella pneumoniae, Enterobacter cloacae, Pseudomonas aeruginosa as well as some activity against quinolone-resistant strains and Acinetobacter baumannii. Sitafloxacin in vitro activity against anaerobes is comparable to imipenem and metronidazole.
SML1542 Sitamaquine tosylate ≥98% (HPLC) Sitamaquine is also known as WR-6026. It is used in the treatment of visceral leishmaniasis.
Sitamaquine is an orally active 8-aminoquinoline analog that exhibit antiplasmodial and antileishmanial activities. Sitamaquine accumulates in Leishmania parasites. Sitamaquine potently inhibits respiratory chain complex II (succinate dehydrogenase), which leads to an apoptosis-like death of Leishmania parasites.
PZ0203 Sitaxentan sodium salt ≥98% (HPLC) Sitaxentan (Sitaxsentan) is a potent and selective endothelin ET(A) receptor antagonist once used in the treatment of pulmonary arterial hypertension (PAH), but removed from the market because of hepatotoxicity. It is over 6000-fold selective for the the ETA receptor subtype with an IC50 of 1 nM for ETA versus an IC50 of 9800 nM for ETB.
Sitaxsentan prevents shunt mediated elevation of pulmonary vascular resistance (PVR). Sitaxsentan effectively inhibits basolateral Na+-taurocholate cotransporting polypeptide (NTCP), organic anion-transporting polypeptides (OATPs) and bile salt export pump (BSEP).
human ... EDNRA(1909), EDNRB(1910)
S7198 Sivelestat sodium salt hydrate ≥98% (HPLC), solid Sivelestat is a competitive human neutrophil elastase (HNE) inhibitor (IC50 = 44 nM, Ki = 0.2 μM). It also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse (IC50 = 19 to 49 nM). However, it does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM. In in-vivo studies, it suppressed lung hemorrhage in hamster (ID50 = 82 μg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase.
SML2087 SJ000291942 ≥98% (HPLC) SJ000291942 is an activator of Bone Morphogenetic Protein (BMP) signaling with an EC50 value < 1 μM. Bone Morphogenetic Proteins (BMPs) are a group of growth factors and cytokines were originally discovered by their ability to induce the formation of bone and cartilage, but are now considered to constitute a group of pivotal morphogenetic signals, orchestrating tissue architecture throughout the body. SJ000291942 was shown to ventralize zebrafish embryos, activate SMAD1/5/8 phosphorylation, and induce the differentiation of C2C12 myoblasts to osteoblasts in manner consistent with BMP4 activation.
S7451 SJ-172550 ≥95% (HPLC) SJ-17255 is a MDMX inhibitor. Similarly to MDM2, MDMX regulates p53. But in contrast to MDM2, MDMX appears to directly regulate p53 transcription. SJ-172550 is a first small-molecule inhibitor of MDMX with a low micromolar binding constant. It appears that SJ-172550 is binding to the p53-binding pocket of MDMX, thus liberating p53 to induce apoptosis.
SML2344   SJB3-019A ≥98% (HPLC) potent USP1 inhibitor that induces ID1 degradation, upregulation of p21 and cytoxicity in K562 and other leukemic cell lines
SML2336 Sk052-145-2 ≥97% (HPLC) Sk052-145-2 is a potent and selective inhibitor of bacterial Lipoprotein signal peptidase (Lsp). Sk052-145-2 potently inhibits growth of E. Coli in a presence of polymyxin B nonapeptide (PMBN).
SML2248 SK-216 ≥98% (HPLC) SK-216 is an orally active potent and selective inhibitor of Plasminogen activator inhibitor-1 (PAI-1) that inhibits tumor progression and angiogenesis. SK-216 inhibits migration and tube formation of cultured human umbilical vein endothelial cells induced by various angiogenic factors. SK-116 prevents a formation of gastro-intestinal polyps in Min mice.
SML2460 SK33 ≥98% (HPLC) SK33, a trifluoromethylated enobosarm analog, is a cell and brain penetrant, tissue selective and highly potent anti-androgen that reduces androgen receptor (AR) transcriptional activity. SK33 induces cell cycle arrest at G1 phase. It exhibits increased efficacy against acquired anti-androgen resistance prostate cancer cells.
SML1966   SK609 hydrochloride ≥98% (HPLC) SK609 (ES609) is a Dopamine D3 receptor (D3R) selective agonist with a bias towards the G-protein-dependent pathway rather than recruiting β-arrestin-2 and an EC50 value of 113.9 nM for activation of ERK1/2 phosphorylation. SK609 has been shown to reverse akinesia and reduce L-dopa-induced dyskinesia in a hemiparkinsonian rat model of Parkinson′s desease. It does not induce desensitization of D3R.
S5576 SKA-31 ≥98% (HPLC) SKA-31 is an activator of KCa2 and KCa3.1 calcium-activated potassium channels. Its EC50 is almost identical at 2-3 μM for all KCa2 subtypes, and about 10-fold lower (260 nM) at KCa3.1 channels. It has significant blood-pressure reducing activity in experimentally hypertensive mice, suggesting potassium channel activation as a therapeutic target for hypertension.
SKA31 is an activator of KCa2 and KCa3.1 Potassium Channels, Potentiates the EDHF Response and Lowers Blood Pressure.
SML2206 SKA-121 ≥98% (HPLC) SKA-121 is a KCa3.1 (IKCa1, IK1, KCa4, SKCa4, SK4) subtype-selective small conductance Ca2+-activated K+ channel (SK channel) positive-gating modulator (EC50 = 109 nM/KCa3.1 vs. 8.7 μM/KCa2.1, 6.8 μM/KCa2.2, 4.4 μM/KCa2.3) with 200- to 400-fold selectivity over CaV1.2 as well as representative KVs (KV1.3, KV2.1, KV3.1, and KV11.1) and NaV (NaV1.2, NaV1.4, NaV1.5, and NaV1.7) channels. When applied in vivo, SKA-121 significantly lowers mean arterial blood pressure in wild-type, but not KCa3.1(-/-), normotensive and hypertensive mice (100 mg/kg i.p.). SKA-121 is a more potent and selective KCa3.1 activator than SKA-31 (EC50 = 260 nM/KCa3.1, 2.9 μM/KCa2.1, 1.9 μM/KCa2.2, 2.9 μM/KCa2.3).
S101 (R)-(+)-SKF-38393 hydrochloride ≥98% (HPLC), solid D1 dopamine receptor agonist; active enantiomer of (±)-SKF-38393.
D047 (±)-SKF-38393 hydrochloride crystalline, ≥98% (HPLC) (±)-SKF-38393 is a D1 dopamine receptor agonist. It is known to promote the production of glutamate in the hippocampus.
human ... DRD1(1812)
S102 S-(−)-SKF-38393 hydrochloride solid D1 dopamine receptor agonist; less active enantiomer of (±)-SKF-38393.
S2941 SKF-75670 hydrobromide >98% (HPLC), solid Atypical D1 dopamine receptor agonist. Displays antagonist activity in vitro and agonist activity in vivo.
SKF-75670 is a selective dopamine D1 receptor agonist but with lower efficacy. It also acts as cocaine antagonist and alters the behavioral effects of cocaine in squirrel monkeys.
human ... DRD1(1812)
S179 R(+)-SKF-81297 hydrobromide ≥98% (HPLC), solid SKF-81297 administration in spontaneously hypertensive rats (SHR) induces an increase in expression of proto-oncogene c-fos mRNA leading to biphasic effect on locomotion. It favors the turnover of phosphoinositide and adenylyl cyclase. SKF-81297 is involved in the stimulation of neurons, in particular the postsynaptic striatal neurons.
S178 (R)-SKF-82957 hydrobromide solid Selective D1 dopamine receptor agonist.
SML0513 SKF83822 hydrobromide SKF83822 is a dopamine receptor agonist that only activates the D1 monomers and stimulates adenylate cyclase, but not PI hydrolysis.
S2816 SKF-83959 hydrobromide ≥98% (HPLC), solid D1 dopamine receptor agonist. Displays antagonist activity in vitro and agonist activity in vivo.
SKF-83959 is an atypical agonist of D1 dopamine receptor and an allosteric modulator of σ-1 receptor on in brain and liver tissues. It has neuroprotective and anti-parkinsonian effects through selective activation of phosphoinositol-linked D1 receptor and promotes migration of cultures astrocytes by ERK1/2 activation. In in vitro studies SKF-83959 exhibits antagonist activity against dopamine D1 receptors coupled to adenylyl cyclase.
human ... DRD1(1812)
S0193 SKF-86002 ≥98% (HPLC), solid p38 MAP kinase inhibitor.
human ... IL1B(3553), TNF(7124)
rat ... Alox5(25290)
S3316 SKF-89145 hydrobromide >98% (HPLC), solid D1 dopamine receptor agonist.
S9066 SKF-89976A >98% (HPLC), solid GABA transporter type 1 (GAT-1) inhibitor that crosses the blood brain barrier.
SKF-89976A contains a cyclic amino acid with lipophilic moiety that enables the compound to cross the blood-brain barrier.1,2 It decreases the excitotoxic swelling of chick retina cells by blocking the glutamate-induced GABA release.3
human ... SLC6A1(6529), SLC6A11(6538), SLC6A12(6539)
rat ... Slc6a1(79212), Slc6a12(50676)
S7809 SKF-96365 ≥98% (HPLC), solid SKF-96365 with an alkylated imidazole ring is a selective inhibitor of receptor-mediated Ca2+ entry and voltage-gated Ca2+ entry . SKF-96365 mediated depolarization of smooth cardiac muscle membrane and had no impact on the acetylcholine (ACh)-induced depolarization. It is an inhibitor for SOCE (store-operated calcium entry). It also inhibits Homer1 protein expression. SKF-96365 elicits protective functionality in 1-methyl-4-phenylpyridinium(MPP) mediated cytotoxicity.
S8326 SKI 5C ≥98% (HPLC) SKI 5C is a selective Sphingosine Kinase 1 (SPHK1) inhibitor.
S5696 SKI II ≥98% (HPLC), solid Sphingosine kinase (SK) plays a pivotal role in regulating tumor growth and SK can act as an oncogene. Expression of SK RNA is significantly elevated in a variety of solid tumors, compared with normal tissue from the same patient. A number of novel inhibitors of human SK were identified, and several representative compounds were characterized in detail. These compounds demonstrated activity at sub- to micromolar concentrations, making them more potent than any other reported SK inhibitor, and were selective toward SK compared with a panel of human lipid and protein kinases. Kinetic studies revealed that the compounds were not competitive inhibitors of the ATP-binding site of SK. 4-[4-(4-chloro-phenyl)-thiazol-2-ylamino]-phenol (SKI-II) inhibitor is orally bioavailable, detected in the blood for at least 8 h, and showed a significant inhibition of tumor growth in mice with IC50 = 0.5 μM; SKI II does not act at ATP-binding site. Displays no inhibition of ERK2, PI 3-kinase, or PKCa at concentrations up to 60 μM.SKI II induces apoptosis and inhibits proliferation in several other tumor cell lines in vitro (IC50 = 0.9-4.6 μM).
SML1164 SKLB1002 ≥98% (HPLC) SKLB1002 is a cell permeable and potent VEGFR2 inhibitor that potently inhibits HUVEC cells proliferation, migration, invasion, and tube formation. It appears that SKLB1002 inhibits VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including extracellular signal regulated kinase, focal adhesion kinase, and Src. SKLB1002 inhibits angiogenesis.
SML1675   SKY Peptide trifluoroacetate salt ≥98% (HPLC) SKY Peptide is a non-cytotoxic and stable nonapeptide modeled after human neutrophil peptide 1 (HNP1, a-defensin) β strand 2 CCL5-binding mode to optimally complete against HNP1 for CCL5 interaction (EC50 ~ 0.1 μg/mL against 10 μg/mL HNP1 and 1 μg/mL CCL5 heteromer formation on HUVECs) without affecting CCL5 and cell surface CCR5 interaction. SKY Peptide is shown to inhibit HNP1-CCL5 heteromer-dependent classical monocytes adhesion both in cultures in vitro (EC50 <1 μg/mL; 10 μg/mL HNP1 and 1 μg/mL CCL5 over HUVEC monolayer) and in mice in vivo.