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SML1565 A-196 ≥98% (HPLC) A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines. For full characterization details, please visit the A-196 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML1410 A-366 ≥98% (HPLC) A-366 is an SGC chemical probe for G9a/GLP, developed in collaboration with Abbvie. A-366 is a potent, selective inhibitor of the histone methyltransferase G9a. The IC50 values for G9a inhbition in enzymatic and cell based assays are 3.3 and approximately 3 μM, respectively. A-366 has little or no detectable activity against a panel of 21 other methyltransferases. For full characterization details, please visit the A-366 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML1033   A-278637 ≥98% A-278637 is a selective opener of ATP-sensitive K (KATP) channels (EC50 = 102 nM) that blocks contraction of bladder smooth muscle in both in vivo and in vitro assays. A-278637 is 15-fold more selective than nifedipine for bladder compared other smooth muscle KATP channels, and displays reduced effects on mean arterial pressure compared to other channel openers.
 
SML0595   A-286982 ≥95% (HPLC) A-286982 blocks binding of lymphocyte function-associated antigen-1 (LFA-1) with the cell adhesion molecule ICAM-1. The IC50 in a cell based assay is 35 nM.
 
SML1879 A-395N ≥98% (HPLC) New A-395N is a control probe for A-395, which is a chemical probe for polycomb protein EED. A-395 is a potent and selective chemical probe for the polycomb protein EED (embryonic ectoderm development), an essential component of Polycomb repressive complex 2 (PRC2), involved in transcriptional repression through methylation of histone H3K27. A-395N is structurally similar, but exhibits no activity in the biochemical and cellular assays, so is an ideal control compound.
 
SML1370   A-779 trifluoroacetate salt ≥98% (HPLC) A-779 (D-Ala7-Ang-(1-7)) is a potent and selective antagonist of angiotensin (1-7), an endogenous peptide that acts through activation of a non-AT1, non-AT2 receptor, Mas, and opposes the activity of angiotensin. A-779 has an IC50 of 0.3 nM for Mas with negligible affinity for either AT1R or AT2R.
 
SML0608   A-412997 dihydrochloride ≥98% (HPLC) A-412997 is a selective D4 agonist with Ki values of 12 and 7.9 nM for the rat and human receptors, and no affinity for other dopamine receptors at concentrations up to 1 mM. A-412997 improves short term memory and cognitive properties in rodent models.
 
SML0446 A-419259 trihydrochloride ≥98% (HPLC) A-419259 is a potent inhibitor of Src family kinases. IC50 values for src, lck, blk, csk, fyn and lyn range between 15 and 50 nM.
 
A9736 A-438079 hydrochloride hydrate ≥98% (HPLC) A-438079 hydrochloride hydrate is a selective P2X7 purinoceptor antagonist in both human and rat with minimal activity at 75 different G-protein-coupled receptors, enzymes, transporters, and ion channels tested.
 
SML0861   A-484954 ≥98% (HPLC) A-484954 is a potent, selective inhibitor of eukaryotic longation factor-2 kinase (eEF2K). Eukaryotic elongation factor-2, which is required for protein synthesis, is inactivated upon phosphorylation by eEF2K.
 
A0862 A-740003 ≥98% (HPLC) A-740003 is a selective P2X7 purinoceptor antagonist.
 
SML0617   A-804598 ≥98% (HPLC) A-804598 is a P2X7 selective, competitive antagonist. In competition assays, the IC50s for human, rat and mouse channels are 11, 10 and 9 nM, respectively.
 
SML0818   A-841720 ≥98% (HPLC) A-841720 is a potent, selective, non-competitive mGluR1 antagonist that displays greater than 30-fold selectivity over another Group I metabotopic glutamate receptor, mGluR5. The compound has potent analgesic properties, and can also diminish motor and cognitive activity.
 
SML0345 A 887826 ≥98% (HPLC) A-887826 is Nav1.8 channel blocker (IC50 = 11 nM) that blocks TTX-resistant sodium currents in rat dorsal root ganglion in a voltage dependent fashion. Oral administration of A-887826 to rats significantly attenuated tactile allodynia in a neuropathic pain model.
 
SML0085 A-967079 ≥98% (HPLC) A-967079 is a potent and selective antagonist of Transient Receptor Potential Anykrin 1 (TRPA1) with IC50′s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and minimal or no activity at other TRP channels or G-protein-coupled receptors, enzymes, transporters, and ion channels out of 89 tested. A-967079 blocks TRPA1 activation in human and rat cell lines and has been shown to reduce the responses of wide dynamic range (WDR) and nociceptive specific (NS) neurons to high-intensity mechanical stimulation.
 
SML1744 A-971432 ≥95% (HPLC) A-971432 is an orally bioavailable, non-clastogenic, azetidinecarboxylate compound that acts as a highly potent and selective sphingosine-1-phosphate receptor 5 agonist (IC50 = 6 nM/S1P5, 362 nM/S1P1 and >10 μM/S1P3 in a radio-ligand binding assay) without affect the activity of 129 protein kinases (IC50 >10 μM). A-971432 is shown to enhance blood-brain barrier integrity and reverse lipid accumulation and age-related cognitive decline in mice in vivo with good pharmacokinetics (t1/2  = 5.7 h; Cmax = 2,500 ng/ml; AUC = 35,000 ng.h/ml at 10 mg/kg, p.o. in CD1 mice). Likewise, oral gavage showed good plasma exposure and no sign of lymphopenia in rats (10, 30, and 100 mg/kg.
 
SML0863   A-1070722 ≥98% (HPLC) A-1070722 is a potent brain-penetrant inhibitor of glycogen synthase kinase-3 (GSK-3) α and β isoforms with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A-1070722 showed > 50-fold selectivity for GSK-3 over a panel of other kinases tested, including CDK family members. A-1070722 decreased phosphorylation of microtubule-associated protein Tau and protected rat primary cortical neurons against β amyloid and glutamate challenge.
 
SML0788   A 83-01 ≥98% (HPLC) A 83-01 is a TGFβ kinase/activin receptor-like kinase (ALK 5) inhibitor (IC50=12 nM) that prevents phosphorylation of Smad2/3 and inhibits growth induced by TGFβ. A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. Also, A 83-01 inhibits the transcriptional activity induced by TGFβ type I receptor ALK-5, activin type IB receptor ALK-4 and nodal type I receptor ALK-7. A-83-01 induces an expansion of neonatal Nkx2.5-eGFP (+) cells.
 
SML1404 A01 (Smurf1 inhibitor) ≥98% (HPLC) A01 is a high affinity selective inhibitor of E3 ubiquitin-protein ligase Smurf1 (Smad ubiquitination regulatory factor-1) that disturbs Smurf1-Smad1/5 interaction and blocks Smurf1 mediated Smad1/5 ubiquitination. A01 increases responsiveness to BMP-2 in myoblasts and osteoblasts.
 
A3111 A1120 ≥98% (HPLC), powder A1120 is a selective non-retinoid ligand for retinol-binding protein 4 (RBP4). RBP4 transports retinol from the liver to extrahepatic tissues and RBP4 lowering is reported to improve insulin sensitivity in mice. A1120 is a high affinity non-retinoid ligand for RBP4 which disrupts the interaction between RBP4 and its binding partner transthyretin (TTR). It binds to the same site as retinol and induces changes in the orientation (compared to the retinol bound form) of loops at the RBP4-TTR interaction interface.A1120 lowers RBP4 and retinol levels in a dose-dependent manner, to a similar extent as seen with fenretinide. However, unlike fenretinide (Sigma# H7779), A1120 does not have beneficial effects on insulin resistance.
 
A8736 A12B4C3 ≥98% (HPLC) A12B4C3 is a potent and specific hPNKP phosphatase inhibitor. A12B4C3 doubles the radiosensitivity of human A549 lung carcinoma and MDA-MB-231 breast adenocarcinoma cells.
 
A2846 A-134974 dihydrochloride hydrate ≥98% (HPLC), solid A-134974 is a novel and selective adenosine kinase (AK) inhibitor with IC50 = 60 pM. Systemic A-134974 (i.p.) dose dependently reduced hyperalgesia (ED50= 1 μmol/kg) and at higher doses, reduced locomotor activity (ED50 = 16 μmol/kg). Administration of A-134974 intrathecally (i.t.) was more potent (ED50= 6 nmol) at producing antihyperalgesia than delivering the compound by intracerebralventricular (ED50 = 100 nmol, i.c.v.) or intraplantar (ED50 >300 nmol) routes. In contrast, i.c.v. administration of A-134974 was more effective in reducing locomotor activity than i.t. administration (ED50 values were 1 and >100 nmol, respectively). Increasing the pretreatment time for i.t.-delivered A-134974 caused a greater reduction in locomotor activity (ED50= 10 nmol). This was due to diffusion of A-134974 (i.t.) to supraspinal sites. These data demonstrate that the novel AK inhibitor A-134974 potently reduces thermal hyperalgesia primarily through interactions with spinal sites, whereas its ability to depress locomotor activity is predominantly mediated by supraspinal sites.
 
SML0471 A22 hydrochloride ≥95% (HPLC) A22 is an inhibitor of MreB, an actin-like bacterial protein, and has been shown to act as an antiobiotic adjuvant. A22 inhibition of MreB disrupts the bacterial actin cytoskeleton, which can cause an increase in cell permeability and altered transport. A22 has been shown to have synergistic effects with several antibiotics including novobiocin and rifampin in gram negative bacteria.
 
A1980 A3 hydrochloride ≥98% (HPLC), solid Non-selective casein kinase (CK) inhibitor. A shorter alkyl chain derivative of W-7 that inhibits casein kinase I (Ki = 80 μM), casein kinase II (Ki = 5.1 μM), myosin light chain kinase (Ki = 7.4 μM), protein kinase A (Ki = 4.3 μM), protein kinase C (Ki= 47 μM), and protein kinase G (Ki = 3.8 μM).
 
A2979 A-317491 sodium salt hydrate ≥98% (HPLC), powder Novel P2X3 and P2X2/3 receptor antagonist
 
A7730 A-331440 dihydrochloride ≥98% (HPLC), solid A-331440 dihydrochloride is a non-imidazole H3 histamine receptor antagonist. Presynaptic histamine H(3) receptors regulate release of histamine and other neurotransmitters, and histamine H(3) receptor antagonists enhance neurotransmitter release. A-331440 is a histamine H(3) receptor antagonist, which binds potently and selectively to both human and rat histamine H(3) receptors (K(i)=25 nM). Mice on a high-fat diet (45 kcal % lard) prior to 28-day oral b.i.d. dosing for measurement of obesity-related parameters. A-331440 administered at 0.5 mg/kg had no significant effect on weight, whereas 5 mg/kg decreased weight comparably to dexfenfluramine (10 mg/kg). A-331440 administered at 15 mg/kg reduced weight to a level comparable to mice on the low-fat diet. The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. Both data shows that the histamine H(3) receptor antagonist, A-331440, has potential as an antiobesity agent.
 
A3104 A-331440 L-tartrate hydrate ≥98% (HPLC), solid Histamine affects homeostatic mechanisms, including food and water consumption, by acting on central nervous system (CNS) receptors. Presynaptic histamine H3 receptors regulate release of histamine and other neurotransmitters, and histamine H3 receptor antagonists enhance neurotransmitter release. A-331440 [4′-[3-(3(R)-(dimethylami<WBR>no)-pyrrolidin-1-yl)-propoxy]-biphenyl-4-carbonitrile] is a histamine H3 receptor antagonist which binds potently and selectively to both human and rat histamine H3 receptors (Ki<=25 nM). Mice were stabilized on a high-fat diet (45 kcal % lard) prior to 28-day oral b.i.d. dosing for measurement of obesity-related parameters. A-331440 administered at 0.5 mg/kg had no significant effect on weight, whereas 5 mg/kg decreased weight comparably to dexfenfluramine (10 mg/kg). A-331440 administered at 15 mg/kg reduced weight to a level comparable to mice on the low-fat diet. The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. These data show that the histamine H3 receptor antagonist, A-331440, has potential as an antiobesity agent.
 
A6604 A-350619 hydrochloride ≥98% (HPLC), solid A-350619 modulates catalytic properties of soluble guanylyl cyclase; it increases Vmas from 0.1 to 14.5 μmol/min/mg and lowers Km from 300 to 50 μM. A-350619 activation of soluble guanylate cyclase depends on the presence of a heme moiety in the enzyme and synergy with nitric oxide.
 
A5861 A-61603 hydrate ≥98% (HPLC) A-61603 is an α1A agonist. In radioligand binding assays, A-61603 was at least 35-fold more potent at α1A receptors than at α1b or α1d sites. In fibroblast cells transfected with α1a receptors, A-61603 more potently stimulated phosphoinositide hydrolysis than norepinephrine, and was antagonized by prazosin. A-61603 is less potent in cells transfected with α1b or α1d receptors. It is a potent agonist at α1A receptors in rat vas deferens (200- to 300-fold more potent than norepinephrine or phenylephrine, respectively) and in isolated canine prostate strips (130- to 165-fold more potent than norepinephrine or phenylephrine, respectively). In contrast, it is only 40-fold more potent than phenylephrine at α1B sites in rat spleen and 35-fold less potent at rat aortic, α1D sites. A-61603 induces a pressor response in conscious rats at doses 50- to 100-fold lower than phenylephrine.
 
SML1731 A64 trifluoroacetate ≥98% (HPLC) A64 is a cell-permeable, ATP site-targeting pyridone thiazolidinedione compound that acts as a potent HIPK2-selective homeodomain-interacting protein kinase inhibitor (IC50 = 74 nM and 136 nM against HIPK2 and HIPK1, respectively; [ATP] = 100 μM), affecting MPF only at higher concentrations (by 35% at 5 μM; [ATP] = 10 μM) and exhibiting little potency toward CDK1 (IC50 >10 μM). A64 (1 μM) effectively prevents ER stresser tunicamycin (1 μg/mL) -induced HIPK2/JNK phosphorylation and cell death in HEK293 and primary rat motor neuron cultures. HIPK2 inhibition by A64 treatment is also efficacious in protecting rat motor neurons from death upon exogenous SOD1 G93A or TDP-43 expression. ff-target kinases revealed by kinome profiling include DYRK1A, CSNK2A2, DAPK2, DAPK1, PIM3, CSNK2A1, PIM1 (Kd = 8.8, 6.1, 6.1, 9.5, 3.7, 31, 37 nM, respectively) and DYRK1B (IC50 = 62 nM).
 
SML1213 A66 ≥98% (HPLC) A66 is a potent and highly selective inhibitor of the phosphoinositide 3-kinase (PI3K) catalytic subunit p110α with an IC50 of 32 nM and >100 fold selectivity for p110α over other class-I PI3K isoforms.
 
A8852 A-68930 hydrochloride ≥98% (HPLC), powder Selective D1 dopamine receptor agonist
 
A255 A-77636 hydrochloride hydrate ≥98% (HPLC), solid Potent, orally active D1 dopamine receptor agonist.
human ... DRD1(1812)
A3109 A-803467 ≥98% (HPLC) A-803467 blocks Nav1.8 in both half-maximal inactive and resting states with an IC50 of 8 nM and IC50 of 79 nM, respectively. A-803467 is over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7.
 
SML0266 AA 29504 ≥98% (HPLC) AA29504 is a GABAA positive modulator with a preference for extra-synaptic α4β3δ over α1β3γ2s synaptic receptors. AA29504 exhibits anxiolytic effects and reduces motor coordination in rat models.
 
SML0358 AA74-1 ≥98% (HPLC) AA74-1 is an extremely potent and selective inhibitor of the serine hydrolase acyl-peptide hydrolase (APEH) with an IC50 of 5 nM in mouse T-cell proteomes. AA74-1 potently blocked the activity of its target serine hydrolase, APEH, in mice in vivo without significantly affecting other enzymes. The APEH inhibition caused accumulation of N-acetylated proteins and stimulated cellular proliferation in T cells.

The APEH gene is deleted in some cancers, in which it has been proposed to serve as a potential tumor suppressor, and is involved in the degradation of oligomeric amyloid-beta which could make it a new target for therapy aimed at reducing neurodegeneration in Alzheimer′s disease. AA74-1 is the first selective tool for studying APEH activity.
 
SML0865   AA92593 ≥98% (HPLC) AA92593 is an opsinamide, a potent antagonist of melanopsin-mediated phototransduction with an IC50 of 665 nM in a Ca2+ flux assay in CHO cells expressing melanopsin (Opn4) and selectivity > 10 μM at 74 common biological targets. AA41612 is believed to act by competing for binding to melanopsin. AA41612 inhibited mouse pupillary light reflex and light aversion in vivo. AA92593 and similar compounds might be useful in alleviating the photophobia associated with migraine.
 
SML1761 AA-CW236 ≥98% (HPLC) AA-CW236 is a cell-permeable chloromethyl triazole (CMT) derivative that acts as a non-pseudosubstrate inhibitor against human O(6)-alkylguanine DNA methyltransferase (MGMT) by targeting MGMT active site Cys145 for covalent modification (KI = 24 nM, kinact = 0.03/min), displaying little affinity toward cysteines from other cellular proteins. AA-CW236 pretreatment (1 μM) effectively prevents MGMT from repairing DNA damage, causing significantly more upregulated O6-alkylguanine accumulation than the pseudosubstrate inhibitor Lomeguatrib (1 μM) when co-administered with the DNA-alkylating agent Temozolomide/TMZ (300 μM) in MCF-7 cells. Likewise, AA-CW236 is shown to boost TMZ toxicity in Caco-2 cultures (IC50 = 227 and 673 μM, respectively, with or without 3 μM AA-CW236 co-treatment).
 
UC432 AAMU    
A4111   2-AAPA hydrate ≥95% (HPLC) Abnormal thiol redox state (TRS) is involved in the pathogenesis of a variety of diseases, such as chronic heart disease and atherosclerosis, rheumatoid arthritis , AIDS , Parkinson disease, Alzheimer disease, etc. Thus there is a need for tools capable of regulating TRS. Glutathione reductase (GR) is a critical enzyme in the homeostasis of TRS. Thus selective GR inhibitor would be a valuable research tool in studying TRS-related processes. Carmustine (#C0400) an anticancer drug is commonly used as GR inhibitor (IC50~470 microM). 2-AAPA is novel, potent cell-penetrable GR inhibitor. The compound is quite selective. But small reduction of activity for GP and GST was observed at 0.1mM concentration of 2-AAPT.
Glutathione reductase (GR) is a critical enzyme in the homeostasis of cellular thiol redox state. 2-AAPA is potent, selective, cell-permeable GR inhibitor, a valuable research tool in studying processes related to thiol redox state. For example, it was used in a study of the relationship between thiol redox state and overall redox state. In addition to the expected decrease in GSH and increase in GSSG, 2-AAPA increased the ratios of NAD(P)H/NAD(P)+. Significant protein glutathionylation was also observed.
 
SML0089 Abacavir sulfate ≥98% (HPLC) Abacavir sulfate is a Nucleoside analog reverse transcriptase inhibitor (NRTI); guanosine analog used to treat HIV and AIDS.
 
SML1816 ABC44 ≥98% (HPLC) ABC44 is a cell-active, potent and selective inhibitor of palmitoyl-protein thioesterase 1 (PPT-1).
 
SML1466 ABH hydrochloride ≥98% (HPLC) ABH (2(S)-amino-6-boronohexanoic acid) is a highly potent and specific arginase inhibitor that inhibits the LPS-induced increases in pulmonary IL-8, neutrophils and goblet cells as well as airway fibrosis in rodent model of COPD.
 
SML1527 Abiraterone acetate ≥98% (HPLC) Abiraterone acetate is a prodrug of abiraterone, which is a potent, selective, and orally bioavailable inhibitor of CYP17A1 (CYP450c17), an enzyme that catalyzes two key serial reactions (17 alpha hydroxylase and 17,20 lyase) in androgen and estrogen biosynthesis resulting in the formation of DHEA and androstenedione, which may ultimately be metabolized into testosterone. CYP17 is the key enzyme for androgen biosynthesis in both the testes and adrenals, so its inhibition should stop the production of androgens in both places. Abiraterone acetate is used for the treatment of metastatic castration-resistant prostate cancer.
 
SML0294 ABL127 ≥98% (HPLC) ABL127 is a potent and selective inhibitor of Protein phosphatase methylesterase-1 (PME-1 or PPME-1). IC50 values were 11.1 nM and 6.4 nM in MDA-MB-231 and HEK 293T cells with no activity detected against >50 other serine hydrolases. PME-1 regulates the methylesterification state of protein phosphatase 2A (PP2A) and is implicated in cancer and neurodegeneration.
 
A236 AB-MECA solid High affinity A3 adenosine receptor agonist.
human ... ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
I145 I-AB-MECA solid Reference standard for radioiodinated I-AB-MECA, a widely used, high affinity radioligand for the A3 adenosine receptor.
human ... ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
SML0904   ABO dihydrochloride ≥98% (HPLC) ABO is a modulator of Annexin A7 (ANXA7) GTPase, a member of the annexin family of calcium/phospholipid-binding proteins. ABO can directly bind to Annexin A7 and inhibit its phosphorylation. Annexin A7 is involved in several processes especially in the process of membrane fusion and exocytosis. ABO is a GTPase, and both GTP-binding and Protein kinase C (PKC) activity are important in regulating its function to potentiate calcium-dependent membrane fusion. Annexin A7 has several other activities, not fully understood. ABO suppressed oxidized low-density lipoprotein (oxLDL)-induced phosphatidylcholine-specific phospholipase C (PC-PLC) activity, inhibiting apoptosis and promoting autophagy in vascular endothelial cells, indicating that ANXA7 is an endogenous regulator of phosphatidylcholine-specific phospholipase C (PC-PLC). ABO significantly reduced atherosclerotic plaque area and reduced lipid deposition and pro-inflammatory macrophages in apolipoprotein E-/- mice. ABO should be a valuable tool to study the complex functions of Annexin 7.
 
A8451 (−)-cis,trans-Abscisic acid    
A4906 (+)-Abscisic acid ≥98% (HPLC) Plant hormone and growth regulator that is involved in several physiological mechanisms including seed dormancy, leaf abscission, stomatal movement, and plant stress responses. Through complex interactions with several intracellular signaling systems, it can regulate the expression of hundreds of plant genes.
 
SML1487 ABT-089 dihydrochloride ≥98% (HPLC) ABT-089 (Pozanicline) is a subtype-selective neuronal nicotinic receptor partial agonist binding primarily to the α4β2 and also α6β2 subtypes. It has been investigated for alleviating symptoms of nicotine withdrawal including cognitive deficits and anxiety.
 
A6476 ABT-418 hydrochloride powder, ≥98% (HPLC) Neuronal nicotinic acetylcholine receptor agonist with cognition enhancing and anxiolytic activities.
 
A9227 ABT-491 hydrochloride ≥98% (HPLC) Highly potent, selective and orally active platelet-activating factor (PAF) receptor antagonist. Ki = 0.6 nM in human platelets.
 
A5111 ABT-724 trihydrochloride ≥98% (HPLC)    
SML0131 ABT-751 hydrochloride ≥98% (HPLC) ABT-751 is an orally bioavailable vascular disrupting agaent (VDA) with a broad spectrum of antitumor activity. It binds to the colchicine binding site on beta-tubulin and inhibits polymerization of microtubules.
 
A4980   Abz-FRK(Dnp)P-OH trifluoroacetate salt ≥95% (HPLC), film Substrate for ACE (Angiotensin Converting Enzyme). Internally quenched fluorogenic substrate for Real Time Fluorescent Assay.
 
A5855 Abz-LFK(Dnp)-OH trifluoroacetate salt ≥97% (HPLC) Abz-LFK(Dnp)-OH is an Angiotensin Converting Enzyme (ACE) fluorescent peptide substrate specific for the C domain for real time fluorescent assay (ACE, Peptidyl Dipeptidase, Kininase II, E.C. 3.4.15.1).
 
A5730 Abz-SDK(Dnp)P-OH trifluoroacetate salt ≥91% (HPLC), lyophilized powder Abz-SDK(Dnp)P-OH is an Angiotensin Converting Enzyme (ACE) fluorescent peptide substrate specific for the N domain for real time fluorescent assay (ACE, Peptidyl Dipeptidase, Kininase II, E.C. 3.4.15.1).
 
SML0787   AC 42 ≥98% (HPLC) AC-42 is a specific agonist of the muscarininc M1 receptor (pEC50 = 6.54) with little or no activity against other muscarinic receptor family members. AC-42 binds to an allosteric site adjacent to the adjacent to the orthosteric, acetylcholine binding site.
 
SML1418   AC187 trifluoroacetate salt ≥95% (HPLC) AC187 is an orally active, potent and selective amylin receptor antagonist that increases glucagon secretion, alters plasma glucose levels and increases food intake in vivo. AC187 completely blocks internalization of amylin monomers in pancreatic cells. AC187 blocks β-amyloid neurotoxicity in rats.
 
SML0625   AC253 trifluoroacetate salt ≥95% (HPLC) AC253 is an antagonist of Amylin, one of the peptides in the Calcitonin-gene related peptide (CGRP) family. In recent studies. AC253 restored memories in brain cells taken from animals used as models of Alzheimer′s disease. Application of AC253 significantly enhanced long-term potentiation (LTP) when given to 6- to 12-month-old TgCRND8 mice that normally show blunted LTP. In other studies, AC25 neutralized the depressant effects of Aβ(1-42) on hippocampal LTP without affecting baseline transmission or LTP on its own.
 
SML0129 AC-265347 ≥98% (HPLC) AC-265347 is a calcimimetic that acts as agonist to calcium-sensing receptor. It reduces serum parathyroid hormone and plasma ionizable calcium.
AC-265347 is a human calcium-sensing receptor (CaSR) allosteric agonist. AC-265347 activates CaSR signaling in cellular proliferation and phosphatidyl inositol (PI) hydrolysis assays.
 
A7980 AC-41848 hydrate ≥98% (HPLC), solid AC-41848 is a potent, cell permeable, subtype selective retinoic acid receptor RARγ agonist. AC-41848 has high selectivity (92%) for RARγ. EC50 = 5.9 μM.
 
A3609 AC-55541 ≥98% (HPLC), powder    
A0355 AC-7954 ≥98% (HPLC), solid Nonpeptide GPR14 / urotensin-UII (UII) receptor agonist that has an EC50 of 300 nM at the human UII receptor (h-UTR). AC-7954 has been shown to exist in two conformations, A and B; both conformations have a pharmacophoric distance within 0.5 Å of P5U, a potent peptidic UII agonist.
human ... UTS2R(2837)
A9605 AC-93253 iodide ≥98% (HPLC) AC-93253 is a potent, cell permeable, subtype selective RAR (RARα) agonist. EC50 = 6.3 μM. AC-93253 has high selectivity; 89% for RARα vs 67% for RARβ1, 35% for RARβ2, and 11% for RARγ.
 
A6981 Acamprosate calcium ≥98% (HPLC), powder Acamprosate calcium is a GABA γ-aminobutyric acid agonist.
 
A9354   Ac-Arg-Glu(EDANS)-Val-His-His-Gln-Lys-Leu-Val-Phe-Lys(DABCYL)-Arg-OH trifluoroacetate salt ≥95% (HPLC), powder α-Secretase substrate II, fluorogenic.
 
SML0180 Aceclidine hydrochloride ≥98% (HPLC) Aceclidine hydrochloride is a parasympathomimetic drug with weak anticholinesterase activity. It acts on cholinergic nerve-endings, lowers intraocular pressure and potent therapeutic agent for open-angle glaucoma.
Aceclidine is a non-selective muscarinic acetylcholine receptor partial agonist that is effective in reducing intraocular pressure.
 
A8861 Aceclofenac ≥98% (HPLC) Non-steroidal, anti-inflammatory drug (NSAID), with selectivity for COX-2 over COX-1.
 
SML0395 Ac-EEMQRR-NH2 trifluoroacetate salt ≥95% (HPLC) Ac-EEMQRR-NH2 is a SNAP25 N-terminal-derived peptide that inhibits the SNARE complex and possibly blocks neuronal exocytosis. Ac-EEMQRR-NH2 exhibits anti-inflammatory and anti-wrinkle activity. It is used as anti-wrinkle cosmetics ingredient.
 
A201 Acenaphthenequinone    
SML0074 Acenocoumarol ≥98% (HPLC) Acenocoumarol is a warfarin analog, an anticoagulant that inhibits Vitamin K epoxide reductase. This results in depletion of the reduced form of vitamin K (vitamin KH2), limiting the gamma-carboxylation and subsequent activation of the vitamin K-dependent coagulation factors II, VII, IX, and X and anticoagulant proteins C and S, resulting in decreased prothrombin levels and the amount of thrombin generated.
 
A7111 Acepromazine maleate ≥98% (HPLC) Acepromazine is a phenothiazine antipsychotic comonly used as a veterinary drug (horses, dogs and cats). The compound is an analogue antipsychotic drug chlorpromazine (#C8138). The drug is thought to block receptors of dopamine in the brain. Recently it was discover that the compound inhibits ABCG2 transported protein, which overexpression in tumors is associated with drug resistance.
 
A3750 21-Acetoxypregnenolone    
P7568 β-Acetyl-γ-O-alkyl-L-α-phosphatidylcholine from bovine heart lecithin ≥99%, lyophilized powder Phospholipid produced by lymphocytes, platelets and endothelial cells that induces platelet aggregation and is involved in inflammation, anaphylaxis and wound repair.
 
A9471   Acetyl-Arg-Tyr-Tyr-Arg-Ile-Lys Amide >97% (HPLC), solid    
A9598   N-Acetyl-Asp-Glu-His-Asp-7-amido-4-methylcoumarin trifluoroacetate salt ≥95% (HPLC)    
A1086 N-Acetyl-Asp-Glu-Val-Asp-7-amido-4-methylcoumarin ≥97% (HPLC), powder Fluorogenic substrate for caspase 3, a protease that is rapidly activated when cells are exposed to apoptotic conditions and that cleaves poly(ADP-ribose) polymerase.
 
A0737 N-acetylcysteine amide ≥98% (HPLC) N-acetylcysteine amide is a membrane penetrating antioxidant with antiinflamatory activity through regulation of activation of NF-κB and HIF-1α as well as modulation of ROS. The compound readily crosses cell membranes, replenishes intracellular GSH, and defends the cell from oxidative stress. In contrast to DTT, AD4 is able to directly reduce intracellularl GSSG to GSH without the involvement of glutathione peroxidase. Such direct thiol exchange might have a protective effect. This compound has a potential in research and exploration for treatment of neurodegeneration, radiation exposure, and other oxidation-mediated disorders.
 
A6166 3-Acetyldeoxynivalenol from Fusarium roseum    
A1556 15-O-Acetyl-4-deoxynivalenol from Fusarium graminearum    
C001 Acetylethylcholine mustard hydrochloride >97% (GC), powder Acetylethylcholine mustard is a precursor for ethylcholine mustard aziridinium ion (AF-64A); irreversible ligand for the high affinity choline transport system; specific presynaptic long action cholinotoxin; inhibitor of choline acetyl-transferase.
 
SML1017   Acetyl fentanyl ≥98% (HPLC) Acetyl fentanyl is an impurity formed in the production process of fentany, and is a very potent μ opiod receptor agonist.
 
A1341 N-Acetyl-Glu-Ser-Met-Asp-al ≥90% (HPLC), powder In the caspase-3 precursor, procaspase-3, the ESMD amino acid sequence has been identified as a cleavage site for producing the p17 and p12 subunits of mature caspase 3; Ac-ESMD-CHO has been shown to inhibit the protease that cleaves procaspase-3 at this site. Ac-ESMD-CHO binds caspase-7 and inhibits with a Ki of approximately 1300 nM, which makes it a weaker inhibitor than other inhibitor tetrapeptide analogs.
 
P4904 β-Acetyl-γ-O-hexadecyl-L-α-phosphatidylcholine hydrate ≥98% Extracellular signaling lipid; ligand for G protein-coupled platelet activating factor (PAF) receptors. Induces inflammation by increasing vascular permeability; activates MAP kinase (MAPK) and MAP kinase kinase (MAPKK) in CHO cells.
 
A1216 N-Acetyl-Ile-Glu-Thr-Asp-al ~99% (TLC), powder Caspase 8 inhibitor; blocks the cleavage of the 32 kDa caspase 3 precursor into the p12 and p20 subunits, thus blocking the formation of active caspase 3.
 
A5720 N-Acetyl-Leu-Glu-Glu-Asp-7-amido-4-trifluoromethylcoumarin ≥90% (HPLC), powder    
A5513 N-Acetylprocainamide hydrochloride ≥99% (HPLC), powder Class III antiarrhythmic. Increases the duration of the action potential by decreasing the delayed outward potassium current, slightly decreasing the calcium current, and slightly depressing the inward rectifier potassium current. This is the active metabolite of procainamide that does not induce systemic lupus erythematosus.
 
A7191 N-Acetyl-D-sphingosine ≥97% (TLC), powder Cell-permeable, biologically active ceramide. It induces differentiation and apoptosis in cells and has been shown to activate protein phosphatases.
 
A6720 N-Acetyl-Trp-Glu-His-Asp-7-amido-4-trifluoromethylcoumarin trifluoroacetate salt ≥97% (HPLC), powder Fluorogenic substrate for caspase 1 and 5.
 
A4339   N-Acetyl-Tyr-Val-Lys(biotinyl)-Asp 2,6-dimethylbenzoyloxymethyl ketone ≥90% (HPLC), powder    
SML0357 AcH4-21 trifluoroacetate salt ≥95% (HPLC) AcH4-21 is a good substrate of Protein Arginine Methyltransferases (PRMTs).
 
SML0312 Acivicin ≥98% (HPLC) Acivicin is an antibiotic that inhibits g-glutamyl transpeptidase and transmembrane glutathione transport. Acivicin is a potent antitumor agent that induces apoptosis in human lymphoblastoid cells.
 
A9229 Ac-Lys-(Me)Leu-Val-(Me)Phe-Phe-NH2 trifluoroacetate salt ≥95% (HPLC) Amyloid β40 fibrillogenesis inhibitor
 
A8001 Aconitine ≥95% (HPLC), crystalline Neurotoxin. Activates tetrodotoxin-sensitive Na+ channels, inducing presynaptic depolarization, thus blocking the nerve action potential which, in turn, blocks the release of neurotransmitters and decreases the end plate potential at the neuromuscular junction. Aconitine also blocks norepinephrine reuptake. In the heart, aconitine induces ventricular tachycardia after intracoronary injection. In cultured ventricular myocytes, aconitine increases the duration of the action potential and induces the appearance of early after depolarization.
 
SML1569 Acotiamide dihydrochloride ≥98% (HPLC) Acotiamide is a potent, selective and reversible inhibitor of human and canine stomach-derived acetylcholinesterase (AChE). Acotiamide showed no affinity for dopamine D2 or serotonin 5-HT4 receptors but does have activity as a muscarinic antagonist. It acts as a prokinetic drug through acetylcholinesterase inhibition and muscarinic receptor antagonism, and has been used for the treatment of functional dyspepsia (FD) involving gastric motility dysfunction.
 
A2112 Ac-PGP trifluoroacetate salt hydrate ≥98% (HPLC) N-acetyl Proline-Glycine-Proline (ac-PGP) is a potent and selective neutrophil chemoattractant. It is generated enzymatically from extracellular matrix proteins such as collagen. PGP is generated from native collagen by the action of matrix metalloproteinase–8 (MMP-8) and/or MMP-9, followed by a secondary cleavage by prolyl endopeptidase (PE). N-terminal acetylation of PGP (Ac-PGP) occurs through an unknown mechanism. Both PGP and AcPGP are considered biomarkers and possible therapeutic targets for chronic obstructive pulmonary disease (COPD) and may also be markers for acute pulmonary exacerbation in Cystic Fibrosis.
 
SML0119 Acrivastine ≥98% (HPLC) Acrivastine is a second-generation antihistamine, an H1-receptor antagonist.
 
SML1393 ACT-462206 ≥98% (HPLC) ACT-462206 is a orally active, brain penetrant, potent and selective dual orexin1/2 receptor antagonist (DORA). ACT-462206 decreases wakefulness, decreases sleep latency, and increases sleep efficacy in rats and dogs.
 
A6671 Actinonin   human ... ANPEP(290), DPP4(1803), ECE1(1889), LAP3(51056)
A4669 Acycloguanosine ≥99% (HPLC), powder Antiviral agent. Phosphorylation by herpes simplex virus thymidine kinase (HSV-TK) leads to the formation of acycloguanosine triphosphate that competitively inhibits the viral DNA polymerase.
Antiviral agent. Phosphorylation by herpes simplex virus thymidine kinase (HSV-TK) leads to the formation of acycloguanosine triphosphate that competitively inhibits the viral DNA polymerase. Acycloguanosine can be used to induce apoptosis in cells transfected with HSV-TK. Inhibits replication of cytomegalovirus by a mechanism that is independent of its phosphorylation by viral or cellular thymidine kinase.
human ... HV1S(3365), NP(4860)
SML0429 Ac-YVAD-cmk ≥95% (HPLC) Ac-YVAD-cmk is a selective ireversible inhibitor of caspase-1 (interleukin-1β converting enzyme, ICE) with some activity also against caspase-4. Ac-YVAD-cmk is anti-apoptotic and has anti-inflammatory and neuroprotective effects, thought to result from its preventing caspase-1 activation of the proinflammatory cytokine, Interleukin-1β.
 
SML0928   AD-01 trifluoroacetate salt ≥95% (HPLC) AD-01 is a potent antiangiogenic peptide a FKBPL fragment, which interact with cell-surface receptor CD44. AD-01 inhibits the self-renewal capacity of CD44-positive breast cancer stem cells (BCSC).
 
A7486 Adapalene ≥98% (HPLC) Retinoic acid analogue that is a RARβ and RARγ agonist (AC50 values are 2.2, 9.3, 22 and > 1000 nM for RARβ, RARγ, RARα and RXRα receptors respectively). Inhibits proliferation and induces apoptosis in colorectal cancer cells in vitro. Displays comedolytic activity. Its unique pharmacological properties make it superior to other retinoids for the treatment of acne.
 
SML1110 Adaphostin ≥98% (HPLC) Adaphostin is a p210bcr/abl tyrosine kinase inhibitor displaying anti-proliferative activity in leukemia models, human prostate cancer cell line PC-3 and other cancer cell lines. Adaphostin is a potent inducer of myeloid cell death. Similarly to AG957, adaphostin appears to induce a degradation of WT and mutated Bcr/Abl.
 
SML0240 Adefovir ≥98% (HPLC) Adefovir is an antiviral drug that after intracellular conversion to adefovir diphosphate inhibits hepatitis B virus (HBV) DNA polymerase (reverse transcriptase).
 
A9251 Adenosine ≥99% Endogenous neurotransmitter at adenosine receptors. Cardioprotective effects may relate to activation of A1 adenosine receptors. The antiplatelet and anti−inflammatory actions of adenosine appear to be mediated via the A2 adenosine receptor. In contrast, adenosine appears to be a pro-inflammatory mediator in asthma and chronic obstructive pulmonary disease (COPD).
human ... ADA(100), ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140), ERBB2(2064), ERBB4(2066)
rat ... Adcy2(81636), Adora1(29290), Adora2a(25369), Adora3(25370)
01890 Adenosine Endogenous neurotransmitter at adenosine receptors. Cardioprotective effects may relate to activation of A1 adenosine receptors. The antiplatelet and anti−inflammatory actions of adenosine appear to be mediated via the A2 adenosine receptor. In contrast, adenosine appears to be a pro-inflammatory mediator in asthma and chronic obstructive pulmonary disease (COPD).
 
A111 Adenosine amine congener hydrate solid, ≥98% (HPLC) Potent aqueous-soluble A1 adenosine receptor agonist.
rat ... Adora1(29290)
A5285 Adenosine 5′-diphosphate monopotassium salt dihydrate bacterial, ≥95%, powder P2Y receptor agonist.
human ... HSP90AA1(3320), P2RY1(5028)
A9501 Adenosine 3′,5′-cyclic monophosphate ≥98.5% (HPLC), powder Naturally-occurring activator of cyclic-AMP-dependent protein kinase (PKA). cAMP is an important second messenger that is linked in many systems to neurotransmitter- or hormone-induced receptor stimulation. The cAMP/PKA signaling pathway has been shown to inhibit cell proliferation, induce differentiation and lead to apoptosis.
human ... OPRK1(4986)
A6885 Adenosine 3′,5′-cyclic monophosphate sodium salt monohydrate ≥98.0% (HPLC), powder Naturally-occurring activator of cyclic-AMP-dependent protein kinase (PKA). cAMP is an important second messenger that is linked in many systems to neurotransmitter- or hormone-induced receptor stimulation. The cAMP/PKA signaling pathway has been shown to inhibit cell proliferation, induce differentiation and lead to apoptosis.
 
A2224 Adenosine 3′,5′-cyclic monophosphate acetoxymethyl ester >97% (HPLC) Membrane-permeable precursor of the second messenger cyclic AMP
 
A166 Sp-Adenosine 3′,5′-cyclic monophosphorothioate triethylammonium salt hydrate ≥98% (HPLC), solid Sp-Diastereomer of adenosine 3′,5′-cyclic monophosphorothioate is a potent, membrane-permeable activator of cAMP dependent protein kinase I and II that mimics the effects of cAMP as a second messenger in numerous systems while being resistant to cyclic nucleotide phosphodiesterases; exhibits greater specificity and affinity than forskolin and cAMP analogs such as dibutyryl-cAMP.
 
A165 Rp-Adenosine 3′,5′-cyclic monophosphorothioate triethylammonium salt powder, ≥98% (HPLC) Rp-Diastereomer of adenosine-3′,5′-cyclic monophosphothioate. Specific membrane-permeable inhibitor of activation by cAMP of cAMP-dependent protein kinase I and II; resistant toward cyclic nucleotide phosphodiesterases; blocks cAMP-mediated effects in numerous systems.
 
A8016 Adenosine 5′-[β-thio]diphosphate trilithium salt ≥80% (HPLC) P2Y receptor agonist.
 
SML0998   AdipoRon ≥98% (HPLC) AdipoRon is an adiponectin agonist that binds to and activates adiponectin receptors AdipoR1 and AdipoR2, activating AMPK and PPAR-α pathways, and ameliorating insulin resistance and glucose intolerance in mice fed a high-fat diet in a manner similar to adiponectin itself. AdipoRon did not affect body weight, but did increase the expression of genes involved in fatty-acid oxidation, decreased tissue triglyceride content, and prolonged the shortened lifespan of db/db mice.
 
SML1829 ADX71743 ≥98% (HPLC) ADX71743 is a brain-penetrant, selective and potent negative allosteric modulator of metabotropic glutamate receptor 7 (mGlu7). In one study ADX71743 exhibited an anxiolytic-like profile in rat and mouse models without causing impairment of locomotor activity. In another study it induced absence epileptic seizures and lethargy.
 
SML0457 AE9C90CB ≥98% (HPLC) AE9C90CB is a muscarinic acetylcholine receptor antagonist with 20-fold selectivity for M3 receptor subtypes compared to M2. In an in vivo assay, AE9C90CB was approximately 5 times more selective for inhibiting carbachol-induced urinary bladder contraction, compared to saliva production.
 
SML1400 AEE788 ≥98% (HPLC) AEE788 is an orally available and potent dual family of human EGFR and VEGFR receptor tyrosine kinase inhibitor that exhibits potent antitumor and antiangiogenic activity.
 
SML0264 AEG 3482 ≥98% (HPLC) AEG3284 is a compound that binds to HSP90, leading to heat shock factor 1 (HSF1) dependent expression of HSP70, an endogenous inhibitor of JNK activity. Treatment of PC12 cells with AEF3284 blocks JNK dependent apoptosis.
 
SML1556   AEM1 ≥98% (HPLC) AEM1 is a potent inhibitor of deregulated Nrf2 transcriptional activity. AEM1 broadly decreases the expression of NRF2 controlled genes and sensitizes A549 cells to various chemotherapeutic agents.
 
SML0706   2-AEMP trifluoroacetate salt ≥97% (NMR) 2-AEMP is a competitive GABAC antagonist with a rapid onset of, and release from inhibition.
 
A1612 AF-353 hydrochloride ≥98% (HPLC), powder AF-353 is a potent antagonist of P2X3 homotrimers and P2X2/3 heterotrimers with a pIC50 range of 7.3 - 8.5. The compound does not affect other P2X family members at 300-fold excess concentrations. AF-353 significantly reversed pain behavior in a rat model of bone cancer pain.
 
SML0435 AF-DX 116 ≥98% (HPLC) AF-DX 116 is a selective M2 muscarinic acetylcholine receptor antagonist.
 
SML0620   AF-DX 384 Free Base ≥98% (HPLC) AF-DX 384 Free Base is a potent muscarinic M2/M4 receptor selective antagonist (pKi values are 8.22, 8.00, 7.51, 7.18 and 6.27 at human M2, M4, M1, M3 and M5 receptors respectively).
 
A6636 Aflatoxin B1 from Aspergillus flavus from Aspergillus flavus Green Alternative Aflatoxin B1 is a carcinogenic compound produced by Aspergillus flavus, a common soil fungus, that induces transversion of G to T at codon 249 of the p53 tumor suppressor gene. Aflatoxin B1 is a food contaminant and a hepatocarcinogen. Aflatoxin is biotransformed to genotoxic intermediates by P450 Phase I enzymes, mainly CYP3A4 via aflatoxin B1 3-hydroxylation. Detoxification depends on Phase II enzymes, such as Glutathione S-Transferase and AFB(1)-aldehyde reductase (AFAR). Aflatoxin B1 is a CYP1A2, CYP2A6, CYP2D6, and CYP3A family substrate.
 
A9887 Aflatoxin B2 Hepatocarcinogen. Food contaminant produced by Aspergillus flavus, a common soil fungus.
 
A0138 Aflatoxin G1 from Aspergillus flavus Hepatocarcinogen. Food contaminant produced by Aspergillus flavus, a common soil fungus.
 
A0263 Aflatoxin G2 Hepatocarcinogen. Food contaminant produced by Aspergillus flavus, a common soil fungus.
 
A6428 Aflatoxin M1 from Aspergillus flavus Hepatocarcinogen.
 
A6655   Aflatoxin B1−BSA Conjugate from Aspergillus flavus    
A6412   Aflatoxin M1–BSA Conjugate    
A9441   Aflatoxin B + G mixture dry concentrate    
SML1578   Aftin-4 ≥98% (HPLC) Aftin-4, an amyloid forty-two inducer, activates γ-secretase, promoting the generation of amyloid-β-1-42 (Aβ1-42) from amyloid-β protein precursor. Aftin-4 increased Aβ-1-42, but not Aβ-1-40 in mouse hipppocampus, accompanied by learning deficits and mitochondrial ultrastructural changes similar to those found in the brains of patients with AD. Aftin-4 can thus be used to induce a rapid, acute Alzheimer′s disease-like toxicity in the rodent brain.
 
A9486 AG-09/1 ≥98% (HPLC) AG-09/1 is a selective formyl peptide receptor 1 (FPR1) agonist; it activates chemotaxis in human neutrophils. Formyl peptide recetors (FPRs) are GPCRs mainly expressed in phagocytic leukocytes but with lower expression in many other cell types. Formyl peptides, act as Alarmins and are released from bacteria and damaged mitochondria, serving as chemoattractants for phagocyte recruitment to sites of inflammation, resulting in immune response. Because the endogenous ligands for FPRs are peptides and arachadonic acid metabolites, there are few small molecule tools for these receptors. A recent HTS of commercially available libraries yielded several FPR-1 selective agonists, of which AG-091 was the most potent. AG-091 induced intracellular calcium flux in FPR-1- but not FPR-2-expressing cells. It also caused chemotaxis and intracellular calcium flux in human leukocytes. AG-091 is a valuable tool for studying FPR1 function in immune and other disease states.
 
PZ0268 AG-17724 ≥98% (HPLC) AG-17724 is a potent peptidyl-prolyl isomerase (PPIase) Pin1 inhibitor.
 
A1487 AG-205 ≥98% (HPLC) AG-205 is a Pgrmc1 (progesterone receptor membrane component 1) inhibitor. AG-205 alters the spectroscopic properties of the Pgrmc1-heme complex. AG-205 inhibits cancer cell viability and cancer cell progression. acting preferentially on Pgrmc1-expressing cells.
 
SML0895   AGI-6780 ≥98% (HPLC) AGI-6780 is a selective inhibitor of IDH2/R140Q a tumor-associated mutant of isocitrate dehydrogenase IDH2. Several human cancers have somatic point mutations in the genes encoding isocitrate dehydrogenases 1 and 2 (IDH1 and IDH2), confering a gain-of-function in cancer cells in which the mutant enzymes produce the oncometabolite (R)-2-hydroxyglutarate, [(R)-2HG]. (R)-2HG inhibits histone- and DNA-modifying enzymes, resulting in altered gene expression, histone and DNA hypermethylation, and inducing a block in cellular differentiation that promotes tumorigenesis. AGI-6780 reduced (R)-2HG levels in cell lines overexpressing IDH2/R140Q with an EC50 of 20 nM, and induced differentiation of TF-1 erythroleukemia and primary human acute myelogenous leukemia cells in vitro. AGI-6780 binds allosterically at the dimer interface of IDH2. AGI-6780 shows good selectivity against other dehydrogenases, including the closely related IDH1-WT or R132H mutant enzymes.
 
A9219   Agitoxin-2 from scorpion venom recombinant, expressed in E. coli, ≥98% (SDS-PAGE), lyophilized powder Potent Shaker K+ channel blocker . Useful as a probe for Kv channels.
 
A8231 AGK2 ≥97% (HPLC), powder AGK2 is a SIRT2 inhibitor. AGK2 rescues dopamine neurons from α-synuclein toxicity in Parkinson′s disease models. IC50 for SIRT2 = 3.5 uM. AGK2 is >15-fold more selective for SIRT2 than SIRT1 and SIRT3. AGK2 may be the most selective SIRT2 inhibitor available.
 
A1362 Agomelatine ≥98% (HPLC) Agomelatine is an extremely potent agonist at both melatonin receptors (MT1 and MT2), with additional antagonism at 5HT2C. It is a novel antidepressant with many desired in vivo properties, including neuroprotection and neurogenesis in depression-sensitive brain areas. Agomelatine′s efficacy appears to be due to both melatonergic and serotonergic properties. In neurogenesis assays, both in vitro and in vivo, the compound effects were differentially affected by antagonists for MT1/MT2 and 5HT2C, demonstrating actions through all three receptors.
 
A3477 AH 11110 >98% (HPLC), solid α1B-adrenoceptor ligand
 
A9102 AH13205 ≥98% (HPLC), oil AH13205 is a selective, low potency agonist for the EP2 receptor. AH13205 has been shown to compete with Prostaglandin E2 (PGE2) for binding, resulting in the displacement of PGE2 binding.
 
A8227 AH23848 hemicalcium salt ≥90% (HPLC), powder EP4 prostanoid receptor antagonist with TP blocking activity.
 
A1221 AH6809 ≥98%, crystalline solid or supercooled liquid DP/EP prostanoid receptor antagonist; has the highest affinity for DP receptors, but also acts as a weak antagonist at murine EP1 and EP2 prostanoid receptors.
 
SML0009 AI-1 ≥98% (HPLC) AI-1 promotes Nrf2 activation via the covalent modification of Kelch-like ECH-associated protein 1 (Keap1), a negative regulator of Nrf2. Biochemical studies indicate that an aromatic chloride present within the AI-1 molecule undergoes a nucleophilic aromatic substitution reaction with cysteine thiols of Keap1.
 
SML0300 Aib-1 trifluoroacetate salt ≥98% (HPLC) Aib-1 is an inhibitor of β-Amyloid oligomerization. Aib-1 is an endomorphin analog more stable to enzymatic degradation and incorporating the β-breaker 2 aminoisobutyric acid. It interacted with Aβ and markedly inhibited the formation of toxic oligomer and fibril growth using in vitro assays, prevented Aβ toxicity in neuronal PC12 cells, and increased longevity in a fly model of Alzheimer′s disease. Aib-1 activity is thought to be due to multi-mode interactions including aromatic, hydrophobic, and polar contacts with Aβ.
 
A9978 AICAR ≥98% (HPLC), powder AICAR is a cell permeable activator of AMP-activated protein kinase (AMPK), a metabolic master regulator that is activated in times of reduced energy availability (high cellular AMP:ATP ratios) and serves to inhibit anabolic processes. In vivo, pharmacologic activation of AMPK with AICAR mimics exercise and triggers insulin-independent glucose uptake by skeletal muscle.
 
A7479 5-AIQ hydrochloride ≥97% (HPLC), solid 5-AIQ hydrochloride is an inhibitor of poly (ADP-ribose) polymerase-1 (PARP-1).
 
SML1344 AK-1 ≥98% (HPLC) AK-1 is a cell permeable, potent and specific SIRT2 inhibitor that induced proteasomal degradation of the Snail transcription factor.
 
SML0152 AK-7 ≥98% (HPLC) AK-7 is a brain penetrant selective SIRT2 inhibitor. No inhibition of SIRT1 or SIRT3 detected.
Selective SIRT2 Inhibitor
 
SML1822 Akebia saponin D ≥98% (HPLC) Akebia saponin D (ASD) is a bioactive triterpenoid saponin isolated from the rhizome of Dipsacus asper Wall that is used as an anti-osteoporosis drug. Akebia saponin D exhibits therapeutic effects in number of disease models including cancer, Alzheimer′s disease, cardiovascular disease, and bone fractures. Akebia saponin D protects against nonalcoholic fatty liver disease (NAFLD) liver damage in mice model of NAFLD. ASD decreases hepatic steatosis and heptocyte apoptosis through autophagy modulation. Akebia saponin D prevents oleic acid induced lipid droplets accumulation and increases autophagic flux BRL cells.
 
A6730 Akt1/2 kinase inhibitor ≥98% (HPLC) Isozyme selective Akt1/2 kinase inhibitor. In in vitro kinase assays, Akt1/2 kinase inhibitor shows IC50 = 58 nM, 210 nM, and 2.12 mM for Akt1, Akt2, and Akt3, respectively, The inhibition appears to be pleckstrin homology (PH) domain-dependent and the Akt1/2 kinase inhibitor has no inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 μM.
 
A3846 AL-8810 ≥98% (HPLC), solid AL-8810 is a novel prostaglandin F analog; selective FP prostanoid receptor antagonist.
human ... PTGFR(5737)
SML1374 Alamandine trifluoroacetate salt ≥98% (HPLC) Alamandine is an endogenous heptapeptide that can be formed from angiotensin A by angiotensin converting enzyme-2 or directly from angiotensin-(1–7) by decarboxylation of its aspartate residue. Alamandine′s activity is similar to Ang-(1–7) rather than that of angiotensin II or angiotensin A. However, Alamandine acts at a different receptor, the Mas-related receptor, MrgD. Alamandine causes vasodilation, and has antifibrosis and antihypertensive activity.
 
A4665 Alamethicin from Trichoderma viride ≥98% (HPLC) Alamethicin is a monovalent cation ionophore that can mimic nerve action potential across artificial membranes. Alamethicin has also been used to study membrane interactions of antimicrobial peptides.
 
A5361   Alamethicin, Ready Made Solution from Trichoderma viride 5 mg/mL in DMSO, sterile; 0.2 μm filtered Alamethicin is a 20-amino acid channel-forming peptide antibiotic isolated from the fungus Trichoderma viride. Alamethicin consists of several isoforms, for which structural information has been published. Alamethicin forms voltage-dependent channels across lipid bilayer membranes. The Alamethicin channel is built by a bundle of helical monomers forming a water filled transmembrane pore. The conductivity level of the channel is determined by the number of associated helical monomers (3-12), which generates a non aligned supermolecular structure with an aqueous core through which ions can cross lipid membranes. Alamethicin catalyzes the exchange of protons for monovalent cations with little difference in affinities and has the ability to transport cations through biological and artificial lipid membranes. Alamethicin can be used for the permeabilization of mitochondria without affecting the outer or inner membranes.
 
SML0415 Alantolactone ≥98% (HPLC) Alantolactone is a sesquiterpene lactone disrupts the Cripto-1/ActRII complexes, resulting in an induction of activin/SMAD3 signaling. Alantolactone inhibits proliferation in cancer cells with no affect on normal cells.
 
A3227 Ala-Tyr-Pro-Gly-Lys-Phe-NH2 trifluoroacetate salt ≥98% (HPLC), solid AYPGK is a ligand for the PAR4 receptor; binding results in activation of PAR4. AYPGK stimulates platelet aggregation in vitro (EC50 =15 μM) via PAR4. In human platelets treated with the PAR4 agonist, AYPGKF stimulates the production of thromboxane, a potent agent for platelet-aggregation. Additionally, AYPGKF mediates the thrombin-induced release of endostatin from rat platelets.
 
SML1590 Alcaftadine ≥98% (HPLC) Alcaftadine is a potent inverse agonist at H1, H2 and H4 histamine receptors. Alcaftadine is antiallergic agent that exhibit anti-inflammatory and mast cell stabilizing effects.
 
SML1480   Alclometasone dipropionate ≥98% (HPLC) Alclometasone dipropionate is a glucocorticoid receptor agonist that mimics the metabolic, anti-inflammatory, immunosuppressive, antipruritic, and vasoconstrictive effects of natural glucocorticoids.
 
SML0462 Alda-1 ≥98% (HPLC) Alda-1 is an ALDH2 agonist; cell-permeable activator of both the wild-type ALDH2*1 and the asian E487K mutant ALDH2*2 forms of mitochondrial aldehyde dehydrogenase 2. ALDH2 is the oxidative enzyme, which removes the ethanol metabolite acetaldehyde and other aliphatic aldehydes. Also. ALDH2 is involved in bioconversion of vasodilator nitroglycerin to nitric oxide. Alda-1 increases acetaldehyde oxidation by ALDH2*1 (wild type) and ALDH2*2 9 Asian variant) approximately 1.5- and 6-fold, respectively. It appears that Alda-1 stimulates acetaldehyde oxidation by ALDH2 by improving NAD binding, but does not improve the nitroglycerin binding affinity of the Asian variant.
 
SML0317 Aldi-2 ≥95% (HPLC) Aldi-2 is a potent and specific covalent inhibitor of aldehyde dehydrogenases. Apparently, Aldi-2 undergoes an enzyme-mediated β-elimination which generates a vinyl-ketone intermediate that covalently modifies the active site cysteine.
 
A9477 Aldosterone ≥95% (HPLC) Biologically active aldosterone isomer; a mineralocorticoid produced by the adrenal cortex that induces urinary excretion of K+ and renal reabsorption of Na+.
human ... SERPINA6(866)
rat ... Ar(24208), Nr3c2(25672)
A4978 Alendronate sodium trihydrate ≥97% (NMR), powder Alendronate sodium trihydrate is a bone resorption inhibitor; farnesyl diphosphate synthase inhibitor (IC50 = 460 nM); CD45 protein tyrosine phosphatase inhibitor.
 
A8986 Alexidine dihydrochloride ≥95% (HPLC) Alexidine dihydrochloride is a potent and selective PTPMT1 (Protein Tyrosine Phosphatase Localized to the Mitochondrion 1) inhibitor. Alexidine increases insulin secretion by isolated rat pancreatic islets.
 
A0232 Alfuzosin hydrochloride ≥98% (HPLC), solid Alfuzosin hydrochloride is an alpha-adrenergic blocker used to treat benign prostatic hyperplasia (BPH). It works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate.
 
SML0381 ALLO-1 ≥98% (HPLC) ALLO-1 is a Smoothened (Smo) antagonist that inhibits both wild-type and mutant Smo, including D473H SMO mutant. ALLO-1 binds to a different domain of Smo than other known Smo ligands.
 
A8476 17-(Allylamino)-17-demethoxygeldanamycin ≥98% (HPLC), solid Potent inhibitor of heat shock protein 90 (Hsp90). 17-AAG is a less toxic analog than geldanamycin. It induces apoptosis and displays antitumor effects. 17-AAG inhibits the activity of oncogenic proteins such as N-ras, Ki-ras, c-Akt, and p185erB2.
 
SML0337 S-Allyl-L-cysteine ≥98% (HPLC) S-allyl-L-cysteine is a sulfur containing amino acid found in garlic with antioxidant, anti-cancer, antihepatotoxic, neuroprotective and neurotrophic activity. S-allyl-L-cysteine has potent activity in several animal models of ischemic injury and Alzhemer′s disease.
 
A114 (+)-N-Allylnormetazocine hydrochloride ≥98% (HPLC) Selective σ1 receptor agonist.
human ... OPRS1(10280)
S168 N-Allyl-(±)-SKF-38393 hydrobromide solid, ≥98% (HPLC) N-Allyl-(±)-SKF-38393 hydrobromide is a selective agonist of D1/D5 dopamine receptors. It mimics the physiological action of dopamine and enhances cognition, memory and learning. It decreases the age-related decline in long-term potentiation of mouse hippocampus. SKF-38393 increases the D1-mediated locomotion in rats.
human ... DRD1(1812)
SML1484 Allyphenyline oxalate ≥98% (HPLC) Allyphenyline is a potent α2C-adrenoceptor/serotonin 5-HT1A receptor agonist and α2A-adrenoceptor antagonist that exhibits anxiolytic effect and antidepressant activity. Allyphenyline attenuates opioid and alcohol withdrawal symptoms including hyperlocomotion and anxiety.
 
SML1210   Almotriptan malate ≥98% (HPLC) Almotriptan is a serotonin 5HT-1B/1D-receptor agonist used to treat migraine. Almotriptan has low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors while affinity for 5-HT receptors other than 5-HT(1B/1D) is substantially lower. Affinity for 5-HT(7) and 5-HT(1A) receptors was approximately 40 and 60 times lower than that for 5-HT(1B/1D) receptors, respectively.
 
SML0346 Alosetron hydrochloride ≥98% (HPLC) Alosetron is a potent and highly selective antagonist of serotonin 5-HT3 receptors, nonselective cation channels found predominantly in the enteric nervous system of the gastrointestinal tract. These receptors are involved in the regulation of visceral pain, colonic transit and GI secretions that can contribute to the pathophysiology of irritable bowel syndrome (IBS). Alosetron is used clinically for treatment of women with severe diarrhea-predominant IBS.
 
A1862 Alpidem ≥98% (HPLC), powder Alpidem is a potent antagonist of peripheral benzodiazepine receptor (PBR) that is located on the outer mitochondrial membrane and interacts with the mitochondrial permeability transition (MPT) pore. Alpidem is an anxiolytic drug from the imidazopyridine family. Alpidem acts selectively on the α3 receptor subtype and to a lesser extent at the α1 subtype (Kd of 0.33nM and 1.67nM respectively), of the benzodiazepine receptor.
 
A8800 Alprazolam Alprazolam binds the GABAA receptor at the benzodiazepine site, which is different than the ligand-binding site at which GABA binds. Alprazolam has been shown to be an anxiolytic (anti-anxiety agent) as well as having anticonvulsant, muscle relaxant and antidepressant activity.
 
A4847   Alsterpaullone ≥98% (HPLC), powder Potent and selective inhibitor of GSK-3β and CDK5/p25; potent inhibitor of CDK1/cyclin B (IC50 = 0.035 μM).
rat ... Gsk3b(84027)
A8106 Altanserin hydrochloride hydrate ≥98% (HPLC), solid Altanserin hydrochloride hydrate is a specific 5-HT2/serotonergic antagonist.
 
A1312 Alternariol from Alternaria sp. ~96%    
A3171 Alternariol monomethyl ether from Alternaria alternata (tenuis)    
SML0318 Alvameline tartrate ≥97% (HPLC) Alvameline (Lu 25-109) is a muscarinic M1 receptor agonist and M2/M3 receptor antagonist that was under investigation for the treatment of Alzheimer′s disease. Alvameline (Lu 25-109) improved cognitive function following traumatic brain injury (TBI) in rats, but failed to show significant positive results in clinical trials.
 
SML1347 Alvimopan ≥98% (HPLC) Alvimopan is a gastroprokinetic peripheral mu-opioid receptor antagonist. As a drug, Alvimopan is given to patients undergoing bowel surgery to protect the bowel from the effects of opioid medications that are used to treat pain, blocking the undesirable GI side-effects of the opioid agonists without affecting analgesia or causing withdrawal. Alvimopan does not cross the blood-brain barrier, competitively binding to gastrointestinal tract mu-opioid receptors.
 
A5475 ALX-1393 >98% (HPLC), powder GlyT-2 glycine transporter inhibitor.
 
SML0897 ALX 5407 hydrochloride ≥98% (HPLC) ALX-5407 hydrochloride (NFPS hydrochloride) is a selective irreversible inhibitor of the glycine transporter GlyT1 with IC50 values of 3 nM for GlyT1 compared to 100 μM for GlyT2. ALX-5407 hydrochloride showed no activity at the inhibitory glycine receptor or glycine site of the NMDA receptor (IC50 > 100 mM).
 
BM0029   AM095 ≥98% (HPLC) AM095 is a potent and selective, orally bioavailable antagonist of lysophosphatidic acid receptor1 (LPA1). AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 and human A2058 melanoma cells. LPA1 has been shown to be involved in neuropathic pain. AM095 inhibition of LPA1 after spinal cord injury resulted in reduced demyelination and improvement in locomotor recovery.
 
A6478 (R,S)-AM1241 ≥98% (HPLC), solid Selective CB2 cannabinoid receptor agonist
 
A6226 AM251 >98% (HPLC), solid AM251 is a CB1 cannabinoid receptor antagonist.
mouse ... Cnr1(12801), Cnr2(12802)
rat ... Cnr1(25248)
A0980 AM281 ≥98% (HPLC) Potent and selective CB1 cannabinoid receptor antagonist/inverse agonist
rat ... Cnr1(25248)
SML1804 AM4113 ≥98% (HPLC) AM4113 is a Cannabinoid CB-1 neutral antagonist. AM4113 reduced reward and reinstatement of drug-seeking behavior, reducing cue-induced reinstatement in monkeys trained to self-administer cocaine.
 
A8843 AM580 ≥98% (HPLC)   human ... RARA(5914), RARB(5915)
SML0327 AM630 ≥90% (HPLC) AM630 is a selective CB2 cannabinoid antagonist/inverse agonist (Ki = 31.2 nM) with > 150-fold selectivity over CB1 receptors.
 
A1987 AM6545 ≥98% (HPLC) AM6545 is a peripheral CB1 cannabinoid receptor antagonist and appetite suppressant.
 
A1304 β-Amanitin from Amanita phalloides ~90% (HPLC) Toxic constituent of the mushroom, Amanita phalloides, inhibits eukaryotic RNA polymerase II and III, but not RNA polymerase I or bacterial RNA polymerase. Inhibits mammalian protein synthesis.
 
A8100   β-Amanitin–poly-L-lysine bound ≥85% Toxic constituent of the mushroom, Amanita phalloides, inhibits eukaryotic RNA polymerase II and III, but not RNA polymerase I or bacterial RNA polymerase. Inhibits mammalian protein synthesis.
 
A1260 Amantadine hydrochloride Dopamine releaser used to treat Parkinsonism and drug-induced extrapyramidal reactions.
 
A5602 AMD3100 octahydrochloride hydrate ≥97% (NMR), solid AMD3100 is a highly specific chemokine receptor CXCR4 antagonist.
 
SML1433   AMD3465 ≥98% (HPLC) AMD3465 is a highly selective chemokine receptor CXCR4 antagonist with antiviral and anticancer activity. The chemokine receptor CXCR4 is expressed on a wide variety of leukocytes and is the predominant receptor for stromal cell-derived factor-1 (SDF1, CXCL12) in addition to acting as a co-receptor for HIV entry into cells. AMD3465 blocks surface binding of CXCL12 (SDF-1α). AMD3465 is an antagonist of SDF-1 ligand binding (K(i) of 41.7+/-1.2 nM). AMD3465 was found to halt the progression of an agressive childhood blood cancer, T-cell acute lymphoblastic leukemia (T-ALL), within two weeks of starting treatment in an animal model.
 
SML0751   AMG-548 dihydrochloride ≥98% (HPLC) AMG-548 is a potent, selective inhbitor of p38α. The Ki values for each p38 isoform are 0.5, 3.6, 2600 and 4100 nM for p38α, p38β, p38γ and p38δ respectively. AMG-548 inhibits LPS-induiced TNFα production in whole blood assay. AMG-548 has also been shown to inhibit Wnt signaling by direcly inhibing Casein kinase 1 isoforms δ and ε.
 
A2731 AMG 9810 ≥98% (HPLC), powder AMG 9810 is a potent, non-vanilloid, antagonist of the TRPV1 receptor. IC50 = 17 nM.
 
A9232 AMI-1 sodium salt hydrate ≥98% (HPLC) Protein arginine N-methyltransferases (PRMTs) are involved in post-translational modification implicated in protein trafficking, signal transduction, and transcriptional regulation. AMI-1 does not inhibit lysine methyltransferase activity and does not interact with S-adenosylmethionine (AdoMet), unlike most methyltransferase inhibitors which compete for the AdoMet binding site. AMI-1 can modulate nuclear receptor-regulated transcription from estrogen and androgen response elements; and is a HIV-1 reverse transcriptase inhibitor. AMI-1 is a potent antagonist of NADPH-oxidase-derived superoxide production, but acts as a direct antioxidant rather than indirectly through methyltransferase inhibition.
 
A5922 Amifostine trihydrate ≥97% (TLC), powder Radioprotective agent. Selectively protects normal tissues from the damaging effects of anti-neoplastic radiation therapy. Selectivity is due to preferential uptake by normal tissues and subsequent metabolic activation to 2-(3-aminopropyl)aminoethanethiol.
 
A7410 Amiloride hydrochloride hydrate ≥98% (TLC), powder Selective T-type calcium channel blocker and blocker of epithelial sodium channel. Selective inhibitor of urokinase plasminogen activator (uPA).
human ... ABP1(26), ACCN1(40), ACCN2(41), PLAU(5328), SCNN1A(6337), SCNN1B(6338), SCNN1D(6339), SCNN1G(6340), SLC9A1(6548), TNF(7124)
mouse ... Abp1(76507), Accn1(11418), Accn2(11419), Plau(18792), Scnn1a(20276), Scnn1b(20277), Scnn1d(140501), Scnn1g(20278), Slc9a1(20544)
rat ... Abp1(65029), Accn1(25364), Accn2(79123), Plau(25619), Scnn1a(25122), Scnn1b(24767), Scnn1g(24768), Slc9a1(24782)
A9400 7-Aminoactinomycin D ~97% (HPLC), powder    
SML0628   8-Aminoadenosine ≥98% (HPLC) 8-Aminoadenosine, a ribose nucleoside, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine also inhibits transcription and polyadenylation. 8-Aminoadenosine potently inhibits varies breast cancer cell lines proliferation and activates cell death independent of p53. 8-NH2-Ado is highly cytotoxic to other cancer cell lines.
 
A0788 3-Aminobenzamide ≥99% (TLC) 3-Aminobenzamide is an inhibitor of poly (ADP-ribose) polymerase (PARP).
mouse ... Parp1(11545)
A3940 1-Aminobenzotriazole Green Alternative Suicide inhibitor of cytochrome P450 and chloroperoxidase.
human ... CYP1A2(1544)
A138 Aminobenztropine solid High affinity muscarinic ligand that has been used for affinity purification of muscarinic cholinergic receptors.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
T1694 (E)-4-Amino-2-butenoic acid    
A9345   N-(4-Amino-2-chlorophenyl)phthalimide Anticonvulsant
 
A0779 p-Aminoclonidine hydrochloride solid α2-adrenoceptor agonist.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
A6355 3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione hydrochloride powder, ≥98% (HPLC) 3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione is extracellular signal-regulated kinase (ERK) docking domain inhibitor. Inhibits ERK binding rather then ERK activity at the ATP domain. IC50 = 25 μM in HeLa, A549, and SUM-159 tumor cells. Currently, no specific inhibitors of the ERK proteins exist. Preferentially binds to ERK2 with a Kd of ~5 μM and prevents its interaction with protein substrates. Shown to block ERK-mediated phosphorylation of ribosomal S6 kinase-1 (RSK-1) and ternary complex factor Elk-1, but exhibits little effect on ERK1/2 phosphorylation by MEK1/2.
 
A5879 2-(2-Aminoethyl)isothiourea dihydrobromide Inhibits constitutive and inducible NOS.
human ... NOS1(4842), NOS2(4843), NOS2B(201288), NOS2C(645740), NOS3(4846)
A9657 DL-Aminoglutethimide DL-Aminoglutethimide is a derivative of the sedative glutethimide. Originally introduced as an anticonvulsant, it was found to cause adrenal insufficiency. Blocks adrenal steroidogenesis by inhibiting the enzymatic conversion of cholesterol to pregnenolone. It also blocks the peripheral conversion (aromatization) of androgenic precursors to estrogens. The D-isomer is 30 times more potent at inhibiting aromatase activity, whereas the L-isomer is more potent at inhibiting cholesterol side-chain cleavage (steroidogenesis).
human ... CYP17A1(1586), CYP19A1(1588)
rat ... Cyp19a1(25147)
A7009 Aminoguanidine hemisulfate salt ≥98% Inhibits both constitutive and inducible nitric oxide synthetase
human ... NOS1(4842), NOS2(4843), NOS2B(201288), NOS2C(645740), NOS3(4846)
SML1856 8-Aminoguanine ≥95% (HPLC) New 8-Aminoguanine, a guanine derivative, is an orally available and highly efficacious potassium-sparing diuretic/natriuretic that increased sodium excretion by 17.2-fold and decrease potassium excretion by 71.0%. 8-Aminoguanine increases glucose excretion by 12.1-fold. Also, 8-Aminoguanine suppressed deoxycorticosterone/salt-induced hypertension.
 
A3281 N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide hydrochloride A calmodulin antagonist; inhibits Ca2+/calmodulin activated phosphodiesterase and myosin light chain kinase.
human ... CAMK2A(815), CAMK2B(816)
SML0657   N-(6-Aminohexyl)-1-naphthalenesulfonamide hydrochloride ≥98% (HPLC) N-(6-Aminohexyl)-1-naphthalenesulfonamide (W-5) is a cell permeable calmodulin antagonist that binds directly to the enzyme.
 
M5560 (S)-2-Amino-2-methyl-4-phosphonobutyric acid hydrochloride synthetic, solid Selective mGluR4,6,7 metabotropic glutamate receptor antagonist.
human ... GRM4(2914), GRM6(2916), GRM7(2917)
A4330 4′-Aminomethyltrioxsalen hydrochloride 4′-Aminomethyltrioxsalen hydrochloride is used to inactivate DNA and RNA viruses, including HIV-1, by nucleic acid cross-linking followed by UV irradiation.
 
SML1062   6-Aminophenanthridine ≥98% (HPLC) 6-Aminophenanthridine selectively inhibits protein folding activity of the ribosome (PFAR). Apparently 6-Aminophenanthridine interacts with the ribosome domain V rRNA and the protein substrate. 6-Aminophenanthridine is an antiprion compound that promotes mammalian prion clearance.
 
A202 N6-2-(4-Aminophenyl)ethyladenosine >95% Potent, non-selective A3 adenosine receptor agonist.
human ... ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
A5352 L-(+)-2-Amino-6-phosphonohexanoic acid ≥98% (HPLC), solid L-(+)-2-Amino-6-phosphonohexanoic acid (L-AP6) is an excitatory glutamate analogue that is able to depolarize L-quisqualic acid (QUIS)-sensitized CA1 rat hippocampal neurons.
 
A1755 Aminophylline ≥98%, powder Non-selective phosphodiesterase (PDE) inhibitor. Antiepileptic drug
 
A1784 Aminopterin powder Folic acid antagonist. Aminopterin is actively transported into cells by the folate transporter. In the cell, it is converted to a high molecular weight polyglutamate metabolite by folylpolyglutamate synthase that, in turn, binds to dihydrofolate reductase and inhibits its activity. Aminopterin-polyglutamate is degraded intracellularly by γ-glutamyl hydrolase.
human ... FPGS(2356)
mouse ... Fpgs(14287)
C7493 Aminopurinyl pyranobenzopyranone monohydrate ≥98% (HPLC), solid Aminopurinyl pyranobenzopyranone monohydrate is an inhibitor of Aβ oligomer-induced cytotoxicity. It is a new Alzheimer′s research tool and potential therapeutic agent. Aminopurinyl pyranobenzopyranone monohydrate acts by inhibiting growth of Aβ oligomers and/or by preventing their toxic conformation or interaction with cellular substrates.
 
SML1723 2-Amino-9H-pyrido[2-3-b]indole ≥98% (HPLC) New AαC (2-Amino-9H-pyrido[2-3-b]indole) is a potential human carcinogen, which is generated by the combustion of tobacco, or by pyrolysis of protein. AαC potentially contributes to liver or digestive tract cancers. Inside body AαC is metabolized to intermediates (possibly short-lived nitrenium ion of AαC) that react with DNA.
 
A3105 2-Amino-N-quinolin-8-yl-benzenesulfonamide ≥98% (HPLC), solid Inhibitor of cell cycle at G2 phase; apoptosis inducer.
 
A3773 9-Amino-1,2,3,4-tetrahydroacridine hydrochloride hydrate ≥99%   human ... ACHE(43)
A8423 Amiodarone hydrochloride ≥98% Non-selective ion channel blocker with broad fungicidal activity. Amiodarone induces an immediate influx of Ca2+ in Saccharomyces cerevisiae, followed by mitochondrial fragmentation and cell death.
 
A2729 Amisulpride ≥98% (HPLC) Amisulpride is a highly selective D2/D3 dopamine receptor antagonist and atypical antipsychotic.
 
A8404 Amitriptyline hydrochloride ≥98% (TLC), powder Tricyclic antidepressant; inhibits the norepinephrine and serotonin transporters with Kis of 100 nM and 14.7 nM, respectively; high in vitro affinity for α1-adrenoceptors, serotonin and muscarinic acetylcholine receptors.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
SML0517 Amlexanox ≥98% (HPLC) Amlexanox is an anti-allergy and anti-asthma drug that blocks histamine and leukotriene release from leukocytes and mast cells. Amlexanox has also been shown to inhibit cahaperone activity of Hsp90, and S100A13, which is involved in transport of proteins devoid of signal peptide sequences.
 
A5605 Amlodipine besylate ≥98% (HPLC) Amlodipine is an L-type calcium channel blocker. Amlodipine belongs to a class of cardiovascular drugs, which act at the voltage gated calcium channel of the CaV1, or L-type, class. Amlodipine also has antihypertensive and antianginal effects. Its activity resides mainly in the (-)-isomer. Amlodipine inhibits growth of human epidermoid carcinoma A431 cells and has antireproductive effects in male rats.
 
SML0283 Amorolfine hydrochloride ≥98% (HPLC) Amorolfine is a broad-based antifungal agent with fungicidal effects against most fungi, dermatophytes and yeasts. Amorolfine blocks ergosterol biosynthesis by interfering with delta 14 reduction and the delta 7-8 isomerisation.
 
A129 Amoxapine Tricyclic antidepressant; inhibits uptake of norepinephrine; inhibits 5-HT2 serotonergic receptors.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
A0326 (S)-AMPA ≥98% Active enantiomer of (RS)-AMPA zwitterion. Potent agonist at the AMPA subclass of ionotropic glutamate receptors.
human ... GRIA1(2890), GRIA2(2891), GRIA4(2893), GRIK1(2897)
mouse ... Gria1(14799)
rat ... Gria1(50592), Gria2(29627), Gria3(29628), Gria4(29629), Grik1(29559), Grik2(54257), Grik4(24406), Grin2a(24409), Grin2b(24410), Grm6(24419)
A9111 (±)-AMPA hydrobromide ≥98% (HPLC) (±)-AMPA is a potent excitatory amino acid that interacts selectively with central AMPA/kainate receptors.
 
A5880 D-Amphetamine hemisulfate salt Induces release of catecholamines and serotonin by displacing the monoamines from their vesicular storage sites; blocks catecholamine reuptake.
 
SML1475 Ampiroxicam ≥98% (HPLC) Ampiroxicam is a non-steroidal anti-inflammatory drug (NSAID), a prodrug of Cox 1/2 inhibitor piroxicam.
 
SML0685   Amprenavir ≥98% (HPLC) Amprenavir is an antiretroviral HIV Protease Inhibitor. It is the active metabolite of fosamprenavir.
 
A9809 Amsacrine hydrochloride ≥98% (TLC), powder Amsacrine hydrochloride is a DNA topoisomerase II inhibitor.
human ... TOP2A(7153), TOP2B(7155)
SML0103 AMTB hydrate ≥98% (HPLC) AMTB is a TRPM8-selective antagonist with no cross reactivity to TRPV1 or 4. The pIC50 of icilin activation of TRPM8 is 6.23 i.v. administration of AMTB reduced the frequency of rhythmic contractions in volume-loaded bladder and inhibited blood pressure and visceromotor reflex responses to bladder distention.
 
A4730 Amthamine dihydrobromide ≥98% (HPLC), solid Amthamine dihydrobromide is a H2 histamine receptor agonist. Amthamine dihydrobromide, similar to histamine, inhibits H2 receptor-mediated eosinophil peroxidase (EPO) release with IC50 = 0.4 μM; a weak antagonist at H3 and shows no activity at H1 receptors.
 
A8486 N-(p-Amylcinnamoyl)anthranilic acid ≥98% (HPLC) Broad spectrum phospholipase A2 (PLA2) inhibitor and TRP channel blocker.
 
A0987 n-Amyl 2-[3,5-dihydroxy-2-(1-nonanoyl)phenyl]acetate ≥98% (HPLC) n-Amyl 2-[3,5-dihydroxy-2-(1-nonanoyl)phenyl]acetate is a Nur77 agonist. Nur77 is a steroid orphan receptor that plays a critical role in regulating proliferation, differentiation and apoptosis. n-Amyl 2-[3,5-dihydroxy-2-(1-nonanoyl)phenyl]acetate, a cytosporone B analog, is a stronger activator of Nur77 than it parent compound. n-Amyl 2-[3,5-dihydroxy-2-(1-nonanoyl)phenyl]acetate treatment causes Nur77 migration to mitochondria, which results in mitochondrial Cyt c release into the cytoplasm and mitochondrial AIF redistribution in both the cytoplasm and nucleus.
 
A1222   7-Methoxycoumarin-4-acetyl-[Asn670, Leu671]-Amyloid β/A4 Precursor Protein 770 Fragment 667-674-(2,4-dinitrophenol)Dap ≥97% (HPLC) β−Secretase substrate
human ... APP(351)
SML1467 ASP7663 ≥98% (HPLC) ASP7663 is a selective activator of transient receptor potential ankyrin 1 (TRPA1), known to play a role for chemical sensing in the pain pathway. ASP7663 activated human, rat, and mouse TRPA1 receptors with EC50 values of 510, 540, and 500 nM, respectively, and little or no affinity at more than 60 other related receptors, channels and enzymes. ASP7663 enhanced colonic motility and exerted analgesic effects against abdominal pain in mouse models.
 
SML1231 c-di-AMP sodium salt ≥98% (HPLC) c-di-AMP is a bacterial secondary messenger. c-di-AMP acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.