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SML1008   C527 ≥98% (HPLC) C527 is a potent inhibitor of the deubiquitinating enzyme complex USP1/UAF1 (IC50 = 0.88 μM). C527 dose dependently inhibits USP1 activity and induced proteasomal degradation of the trasnscriptional regulator ID1 in U20S osteosarcoma cells.
 
SML0002 C646 ≥98% (HPLC) C646 is a competitive histone acetyltransferase (HAT) p300/CBP inhibitor with a Ki of 400 nM and is selective versus other acetyltransferases.
C646 is a potent, cell permeable and selective inhibitor of p300 and CBP (p300/CBP) histone acetyltransferases. Inhibition of p300/CBP by C646 affects the activity of a variety of transcriptional factors such as NF-κB, p53 and MyoD that are associated with physiology, disease processes, hippocampal synaptic plasticity, spatial memory and contextual fear.
 
C5490 C75 ≥98% (HPLC), powder C75 is a novel, potent synthetic inhibitor of fatty acid synthase (FAS), which is used as a tool for studying fatty acid synthesis in metabolic disorders and cancer.
 
C5732 CA-074 ≥99% (TLC)    
C5857 CA-074 methyl ester ≥99% (TLC) CA-074 methyl ester is an inhibitor of cathepsin B.
 
C0246 Cabergoline ≥98% (HPLC) Cabergoline, a lysergic acid amide derivative, is a potent dopamine D2 receptor agonist. It also acts on dopamine receptors in lactophilic hypothalamus cells to suppress prolactin production in the pituitary gland. It has been used for monotherapy of Parkinson′s disease in the early phase; combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson′s disease and adjunctive therapy of prolactin-producing pituitary gland tumors (microprolactinomas).
 
SML0916   CaCCinh-A01 ≥98% (HPLC) CaCCinh-A01 is a potent calcium-activated chloride channel (CaCC) inhibitor that fully inhibits CaCC current in human bronchial and intestinal cells. CaCCinh-A01 does not inhibit CFTR.
 
C6374 Caerulomycin A from Streptomyces caeruleus, ≥98% (HPLC) Caerulomycins produced by Streptomyces caeruleus are bipyridinic molecules endowed with antibiotic properties. Caerulomycin A was found to have a strong anti-fungal and anti-amoebic activity, and a mild antibacterial activity.
 
C0625 Caffeic acid ≥98.0% (HPLC) A natural dietary phenolic compound found in plants that is an anti-oxidant. Inhibits the synthesis of leukotrienes that are involved in immunoregulation, inflammation and allergy. Inhibits Cu2+-induced LDL oxidation.
human ... ELA2(1991)
rat ... Alox5(25290)
C8221 Caffeic acid phenethyl ester ≥97% (HPLC), powder Caffeic acid phenethyl ester is a specific inhibitor of the nuclear transcription factor NF-κB.
human ... NFKB2(4791)
SML0304 Caged MK801 ≥98% (HPLC) Caged MK801 is an inactive caged form of the potent selective non-competitive irreversible NMDA glutamate receptor open-channel blocker MK801. Caged MK801 is cleaved by exposure to UV light, liberating the active MK801. The caged compound is stable within cells. Intracellular compartment-specific photorelease allowed study the locus of induction and expression of timing-dependent long-term depression (t-LTD). Caged MK801 is thus a useful tool to uncover compartment-specific biological functions.
 
C4369 Calcipotriol hydrate ≥98% (HPLC) Calcipotriol, a synthetic derivative of calcitriol or Vitamin D, is used in the treatment of psoriasis and marketed under the trade name Dovonex. It has comparable affinity with calcitriol (Vit. D) for the Vitamin D receptor (VDR), while being less than 1% as active as the calcitriol in regulating calcium metabolism. VDR belongs to the steroid/thyroid receptor superfamily, and is found on the cells of many different tissues including the thyroid, bone, kindney, and T cells of the immune system. Binding of calcipotriol to the VDR modulates the T cells gene transcription of cell differentiation and proliferation-related genes.
 
SML0668   Calhex 231 hydrochloride ≥98% (HPLC) Calhex 231 is a negative allosteric modulator of the calcium sensing receptor CaSR. Calhex 231 blocks calcium-induced accumulation of inositol phosphate with an IC50 of 0.36 μM.
 
SML1386 Calindol hydrochloride ≥98% (HPLC) Calindol is a calcimimetic Ca Sensing Receptor (CaSR) agonist. It is a positive allosteric modulator (PAM) with an EC50 value of 1 μM and a maximum stimulation of 130% of the 10mM Ca2+ activation in triggering PI hydrolysis.
 
A6185 Calpain Inhibitor I ≥97% (TLC), powder Can initiate apoptosis in HL-60 cells but blocks dexamethasone-induced apoptosis in thymocytes and cycloheximide-induced apoptosis in metamyelocytes. Inhibits cyclin B degradation and arrests the cell cycle at G1/S and at meta-/anaphase. Blocks induction of nitric oxide synthase by LPS in macrophages.
human ... CAPN1(823), CTSB(1508), PSMA1(5682)
A6060 Calpain Inhibitor II powder    
C8999 Calpeptin ≥98% (HPLC) Calpeptin is a rho kinase activator and an inhibitor of calpains, a family of calcium-dependent cysteine proteases involved in apoptosis, long-term potentiation in neurons, and cell cycle progression.
 
C6303 Calphostin C from Cladosporium cladosporioides ≥90% (HPLC), powder Highly specific inhibitor of protein kinase C (IC50 = 50 nM); requires light for activation. At higher concentrations (100 nM or greater), it has been shown to inhibit cell proliferation and induce apoptosis in vitro.
 
C5552 Calyculin A from Discodermia calyx ≥90% (HPLC), solid Inhibitor of protein phosphatases types 1 and 2A; marine toxin, potent tumor promotor.
 
21279 Calyculin A from Discodermia calyx ≥90% (HPLC) Inhibitor of protein phosphatases types 1 and 2A; marine toxin, potent tumor promotor.
 
SML1016 Camalexin ≥98% (HPLC) Camalexin is a phytoalexin isolated from cruciferous plants that exhibits antibacterial, antifungal, antiproliferative and cancer chemopreventive activities. Apparently, camalexin increases the ROS levels and is more effective in aggressive prostate cancer cells that express high ROS levels. In Arabidopsis thaliana, camalexin and salicylic acid confer resistance to Phytophthora capsici.
 
C0494 Cambinol ≥97% (HPLC), white powder Cambinol is a Sirtuin (Human Silent Information Regulator) Type 1/2 Inhibitor. Sirtuins are structurally and mechanistically unrelated to HDACs Class 1 & 2 deacetylases but share many protein targets. HDAC is a large complex enzyme family involved in epigenetic-control of gene expression. Sirt2 has an IC50 equal to 59 μM.
 
SML0958   Camfetamine hydrochloride ≥98% (HPLC) Camfetamine hydrochloride is a stimulant drug closely related to fencamfamine, which has been widely used as a central nervous system (CNS) stimulant and appetite suppressant.
 
SML0057 Camostat mesylate ≥98% (HPLC) Camostat is a synthetic, orally bioavailble serine protease inhibitor.
Camostat mesylate inhibits the production of TNF-α and monocyte chemoattractant protein-1 (MCP-1) by monocytes. It also inhibits the activity of pancreatic stellate cells. Camostat mesylate regulates the cytokine expression and inflammation and is effective in the treatment of dibutyltin dichloride-induced rat pancreatic fibrosis.
 
C9911 (S)-(+)-Camptothecin ≥90% (HPLC), powder (S)-(+)-Camptothecin binds irreversibly to the DNA-topoisomerase I complex, inhibiting the reassociation of DNA after cleavage by topoisomerase I and traps the enzyme in a covalent linkage with DNA. The enzyme complex is ubiquinated and destroyed by the 26S proteasome, thus depleting cellular topoisomerase I. Blocks the cell cycle in S-phase at low does and induces apoptosis in a large number of normal and tumor cell lines by cell cycle-dependent and cell cycle-independent processes.
human ... TOP1(7150)
mouse ... Prkca(18750)
rat ... Sstr2(54305)
SML0245 Candesartan cilexetil ≥98% (HPLC) Candesartan cilexetil is the prodrug form of the potent angiotensin II receptor antagonist, candesartan. The prodrug is cleaved by esterases within the intestine to liberate the active molecule.
 
C7287 Canrenoic acid potassium salt powder Competitive aldosterone receptor antagonist. Potassium canrenoate reduces the effects of aldosterone-induced increases in blood pressure and in cardiovascular fibrosis in animals with high sodium intake. It is used clinically for its anti-fibrotic effects. At higher doses it is genotoxic to liver and increases tumor incidence in rodent models.
 
SML1497 Canrenone ≥97% (HPLC) Canrenone is a mineralocorticoid (aldosterone) inhibitor. Aldosterone is known to be involved in hypertension, kidney disease, atherosclerosis, and heart failure. Blockade of the aldosterone receptor has been shown to improve cardiovascular function. In congestive heart failure, aldosterone antagonists are used in addition to other drugs for additive diuretic effect, which reduces edema and the cardiac workload. Canrenone is an active metabolite of spironolactone with potassium-sparing diuretic activity. Canrenone specifically antagonizes aldosterone at the mineralocorticoid receptor in the kidneys, thereby increasing sodium excretion and inhibiting potassium excretion.
 
C7632 Cantharidin Inhibitor of protein phosphatase 2A.
human ... PPP2CA(5515), PPP2CB(5516), PPP2CBP(5517), PPP2R1A(5518), PPP2R1B(5519), PPP2R2A(5520), PPP2R2B(5521), PPP2R2C(5522), PPP2R3A(5523), PPP2R5A(5525)
SML0653 Capecitabine ≥98% (HPLC) Capecitabine is an anti-cancer drug, a prodrug of doxifluridine, metabolized to 5-fluorouracil at the tumor site. The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites, 5′-Deoxy-5-fluorocytidine (5′-DFCR) and 5′-Deoxy-5-fluorouridine (5′-DFUR), to form 5-fluorouracil.
 
PZ0317 Capromorelin tartrate ≥98% (HPLC) Capromorelin tartrate is a potent ghrelin receptor agonist/growth hormone secretagogue (Ki = 7 nM). In rat pituitary cells, Capromorlelin incudes growth hormone (GH) secretion with an EC50 of 3 nM. Capromorelin also increases gastric motility and has been studied recently in patients with spinal cord injuries.
 
M2028 Capsaicin ≥95%, from Capsicum sp. Prototype vanilloid receptor agonist. Neurotoxin; activates sensory neurons that give rise to unmyelinated C-fibers, many of which contain substance P. Topical application desensitizes the sensory nerve endings giving a paradoxical antinociceptive effect; systemic administration can be neurotoxic to capsaicin-sensitive cells, especially in newborn animals. Active component of chili peppers.
human ... CYP1A2(1544), TRPV1(7442)
rat ... Trpv1(83810), Trpv4(66026)
360376 Capsaicin natural Prototype vanilloid receptor agonist. Neurotoxin; activates sensory neurons that give rise to unmyelinated C-fibers, many of which contain substance P. Topical application desensitizes the sensory nerve endings giving a paradoxical antinociceptive effect; systemic administration can be neurotoxic to capsaicin-sensitive cells, especially in newborn animals. Active component of chili peppers.
human ... CYP1A2(1544), TRPV1(7442)
rat ... Trpv1(83810), Trpv4(66026)
C191 Capsazepine ≥98% (HPLC), solid Capsazepine is a specific vanilloid receptor antagonist; synthetic analog of capsaicin.
human ... TRPV1(7442), TRPV4(59341)
rat ... Trpv1(83810)
C4042 Captopril ≥98% (HPLC), powder Angiotensin converting enzyme inhibitor. Inhibits the formation of angiotensin II, a bioactive peptide that stimulates angiogenesis and increases microvessel density.
human ... ACE(1636), AGTR1(185), AGTR2(186), ECE1(1889)
rat ... Ace(24310)
SML0319 Caramiphen hydrochloride ≥98% (HPLC) Caramiphen is an anti-muscarinic similar to atropine; muscarinic acetylcholine receptor antagonist. Caramiphen is commonly used as a cough suppresant, but is also administered for the treatment of Parkinson′s disease. The compound has also been shown to have anti-depressant properties that may involve inhibition of G protein-coupled inwardly rectifying potassium channel GIRK.
 
C4024 Carbamazepine powder Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site. Sodium channel inhibitor.
human ... BZRAP1(9256), GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), PRNP(5621), SCN5A(6331)
rat ... Scn2a1(24766), Scnn1a(25122), Scnn1g(24768), Slc6a1(79212)
C4382 Carbamoylcholine chloride ≥98% (titration), crystalline Non-selective cholinergic agonist that is resistant to the action of cholinesterases; inhibits apoptotic death of cultured neurons, and may induce apoptosis in thymocytes.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133), CHRNA2(1135)
mouse ... Chrm1(12669)
rat ... Chrm1(25229), Chrm2(81645), Chrm3(24260), Chrna2(170945), Chrna3(25101), Chrna4(25590)
SML0308 Carbazeran ≥96% (HPLC) Carbazeran is an Aldehyde oxidase (AO) substrate and a phosphodiesterase inhibitor that produces concentration-dependent positive inotropic responses. In humans, the compound is almost completely cleared via 4-hydroxylation to the phthalazinone metabolite by AO.
 
SML0748   Carbetocin acetate ≥93% (HPLC) Carbetocin is a potent agonist of the oxytocin receptor, with improved in vivo stability over oxytocin.
 
SML0931   Carbimazole ≥98% (HPLC) Carbimazole is a pro-drug of methimazole that is an inhibitor of thyroid enzyme thyroperoxidase. Carbimazole is used to treat hyperthyroidism. Also, carbimazole induces phosphorylation of eukaryotic elongation factor eEF2.
 
E006 β-Carboline-3-carboxylic acid N-methylamide Benzodiazepine inverse receptor agonist; potent anxiogenic agent.
human ... BZRAP1(9256)
C2759 Carbonyl cyanide 3-chlorophenylhydrazone ≥97% (TLC), powder Protonophore (H+ ionophore) and uncoupler of oxidative phosphorylation in mitochondria. Shown to have a number of effects on cellular calcium. Inhibits secretion of hepatic lipase and partially inhibits the pH gradient-activated Cl- uptake and Cl-/Cl- exchange activities in brush-border membrane vesicles.
 
C2920 Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone ≥98% (TLC), powder FCCP is a protonophore (H+ ionophore) and uncoupler of oxidative phosphorylation in mitochondria. It is capable of depolarizing plasma and mitochondrial membranes. FCCP has been shown to have a number of effects on cellular calcium. It also is reported to inhibit a background K+ current and induce a small inward current, reduce pH by 0.1 unit, and induce a rise of intracellular [Na+]. FCCP stimulates Mg2+-ATPase activity, inhibits β-amyloid production, and mimics the effect of selective glutamate agonist N-methyl-D-aspartate (NMDA) on mitochondrial superoxide production.
 
C2538 Carboplatin Carboplatin is a platinum-based antineoplastic drug that damages DNA by forming intrastrand cross-links with neighboring guanine residues. Tumors acquire resistance to these drugs through the loss of DNA-mismatch repair (MMR) activity and the resultant decrease in the induction of programmed cell death.
 
C117 5-Carboxamidotryptamine maleate salt powder, ≥98% (HPLC) Agonist at 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5 and 5-HT7 serotonin receptors.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR2A(3356), HTR2C(3358), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
rat ... Htr7(65032)
SML0408 Carboxyamidotriazole ≥98% (HPLC) Carboxyamidotriazole (L-651582) is an orally active calcium channel blocker. Carboxyamidotriazole blocks intracellular and mitochondrial calcium entry and flux, resulting in inhibition of cell proliferation, calcium-release-activated calcium channel (CRAC) function, and maintenance of mitochondrial membrane potential.
 
C4992 Carboxyatractyloside potassium salt ≥98% (HPLC), from Xanthium sibiricum, solid Carboxyatractyloside is a highly selective inhibitor of cytosolic side-specific mitochondrial ADP/ATP carrier; i.e. adenine nucleotide translocase (ANT); causes stabilization of the c conformation of ANT leading to permeability transition pore (PTP) opening, loss of mitochondrial membrane potential, and apoptosis.
 
SML1176   Carboxypyridostatin trifluoroacetate salt ≥95% (HPLC) Carboxypyridostatin (carboxyPDS) selectively stabilizes RNA-containg G-quadruplex stuctures. Immunofluorescent staining of carboxyPDS treated cells using an anti G-quadruplex antibody reveals staining only in the cytoplasm and not the nucleus, demonstrating selectivity against DNA G-quadruplex structures.
 
UC260 Carboxytolbutamide In vivo tolbutamide metabolite. Major urinary metabolite of tolbutamide.
 
SML0329 Carcinine dihydrochloride ≥98% (HPLC) Carcinine (β-alanyl histamine) is a selective histamine H3 antagonist, 100-1000-fold selective for H3 over H2 and H1, that also functions as an antioxidant and as a chemical chaperone to reduce non-enzymatic glycation of proteins and maintain native folding of proteins.
 
C8249 Cardamonin ≥98% (HPLC) Cardamonin is a calchone from Aplinia species (zingiberaceous plant species). Cardamonin inhibits pigmentation in melanocytes through suppression of Wnt/b-catenin signaling pathway. Cardamonin suppressed Wnt/b-catenin signaling by a mechanism involving proteasome-mediated degradation of b-catenin (GSK-3b-independent pathway). Research has shown that Cardamonin possesses anti-inflammatory activity via suppression of NF-kB nuclear translocation and Ik-Ba phosphorylation.
 
SML0458 Cardionogen-1 ≥98% (HPLC) Cardionogen-1 is cardiomyocyte promoter and an inhibitor of Wnt/β-catenin dependent transcriptional activity with an EC50 of 23 nM in murine stem cells and zebrafish embryos. It induces cardiac cell formation in both murine stem cells and zebrafish embryos, expanding cardiac progenitor cells.
 
SML0427 Cardionogen-2 ≥98% (HPLC) Cardionogen-2 is a biphasic modulator of cardiogenesis that enlarges the size of the zebrafish embryonic heart by promoting cardiomyocyte formation. Also, cardionogen-2 promotes murine ES cells to differentiate into beating cardiomyocytes. Apparently, cardionogen-2 inhibits Wnt/b-catenin dependent transcriptional activity. Treatment of zebrafish embryos with cardionogen-2 significantly enlarged both the atrium and ventricle, without causing apparent defects of embryonic morphology or other organ development.
 
LO2219   Cardiotoxicity Ligand Set Cardiotoxicity is an important cause for concern in drug development and appears to cut across therapeutic indications and drug classes. Several drugs have been removed from the market recently because of prolonging the QT interval or causing Torsades de Pointes (TdP).

The Cardiotoxicity Ligand Set features a wide variety of drugs including anti-arrhythmics, antihistamines, antibiotics, anticonvulsants, antidepressants and antipsychotics that are known to have cardiotoxic side-effects.
 
C9759   Cardiotoxin from Naja mossambica mossambica    
SML1360 Cariporide ≥98% (HPLC) Cariporide is a selective inhibitor of the Na+/H+ exchanger subtype 1 (NHE-1), also known as the Na+/H+ antiporter. Cariporide has shown cardioprotective and antiarrhythmic effects, and has recently been investigated for anticancer activity.
 
C1494 Carmofur ≥98% (HPLC), powder Carmofur is a derivative of fluorouracil, an antimetabolite used as an antineoplastic agent.
 
C0400 Carmustine ≥98% Carmustine is a DNA alkylating agent causing DNA interstrand crosslinks. Effective against glioma and other solid tumors.
human ... GSR(2936)
C4582 β-Carotene Type II, synthetic, ≥95% (HPLC), crystalline The most important of the provitamins A, β-carotene can be classified as an antioxidant due to its inhibition of radical initiated peroxidation in vitro. However, in vivo it appears to act either as an antioxidant or a prooxidant depending on cellular environment. It reduces the incidence of many cancers, but enhances lung cancer incidence in smokers.
 
C1119 Caroverine hydrochloride ≥98% (HPLC), solid Caroverine hydrochloride is a nonselective NMDA and AMPA glutamate receptor antagonist. Also, Caroverine hydrochloride is a class B calcium-channel-blocker, antiglutamatergic agent, and acts as an antioxidant when administered to lab animals.
 
SML1713 Carprofen ≥97% (HPLC) Carprofen is a non-steroidal anti-inflammatory drug (NSAID) that has been found to have antimicrobial activity. Carprofen is primarily used as a veterinary analgesic and anti-inflammatory for arthritis and pain. Its anti-inflammatory activity is due to cyclooxygenase inihbition with selectivity for COX-2 inhibition, while its antimicrobial activity is less certain. Carprofen can kill B. subtilis by permeabilizing its membrane. Other studies have shown carprofen can target the Escherichia coli DNA polymerase III β subunit.
 
C3993 Carvedilol ≥98% (HPLC), solid Cavedilol is a non-selective β-adrenergic blocker with α1 blocking activity. Carvedilol is used specifically for the treatment of heart failure and high blood pressure. It has been shown to improve left ventricular ejection fraction and may reduce mortality.
 
C4330 Casein Kinase II-β fragment 198-215 ≥95% (HPLC) Cdc2 substrate and competitive inhibitor of apoptosis. Sequence contains CK II autophosphorylation site plus p34cdc2 consensus phosphorylation site Ser209.
human ... CSNK2B(1460)
SML1253 CASIN ≥98% (HPLC) CASIN is an inhibitor of Cdc42 GTPase, a small GTPase of the Rho-subfamily that plays important roles in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. CASIN generated a rejuvenated phenotype of Hematopoietic stem cells (HSCs), reversing the aging-related and polarity phenotype of aged HSCs to that of young HSCs in vivo..
 
SML0425 Caspofungin diacetate ≥97% (HPLC) Caspofungin is an echinocandin antifungal that inhibits 1,3-β-D-glucan synthase, which is required for cell wall synthesis, thereby disturbing the integrity of the fungal cell wall.
 
C0567 (−)-Catechin ≥97% (HPLC), from green tea   human ... BACE1(23621)
C1251 (+)-Catechin hydrate ≥98% (HPLC), powder An antioxidant flavonoid of plant origin; a free radical scavenger, preventing free radical-mediated damage in a variety of biological systems. For example, at physiological pH catechin suppressed DNA strand breaks by hydroxyl radicals. It has also been shown to prevent human plasma oxidation. It delayed the consumption of endogenous lipid-soluble antioxidants and inhibited lipid oxidation.
 
C0692 (−)-Catechin gallate ≥98% (HPLC), from green tea Antioxidant constituent of green tea. At μM concentrations, it inhibits VEGF-induced tyrosine phosphorylation. It also inhibits aromatase activity, an enzyme that converts androgens to estrogen and is thought to play a role in the etiology of breast cancer.
human ... BACE1(23621)
SML0259 Catharanthine ≥95% (HPLC) Catharanthine is a precursor of the anti-tumor drugs vinblastine and vincristine, formed by dimerization of catharanthine with vindoline. Catharanthine itself is an inhibitor of tubulin self-assembly into microtubules, although not so potent as vinblastine or vincristine. Catharanthine also has anticholinergic activity. It showed muscarinic antagonism at 10 microM and fully inhibited nicotinic receptor mediated diaphragm contractions with an IC50 of 59.6 microM.
 
C222 Cathine hydrochloride Anorexic; with pharmacological effects similar to those of the amphetamines.
 
C3196 S(−)-Cathinone hydrochloride Alkaloid that is the major central nervous system stimulant of the Khat shrub. Like amphetamine, it is a potent releaser of norepinephrine and dopamine from their intracellular stores.
 
SML1782 CATPB ≥98% (HPLC) CATPB is an acetamidophenylbutanoate derivative with inverse agonist and antagonist activity against human, but not mouse or rat, FFA2 (GPR43). CATPB inhibits both constitutive and propionate (C3) -stimulated hFFA2 GTPγS incorporation (IC50 ~35 and 320 nM, respectively; [C3] = EC80, ~125 nM), as well as C3-induced hFFA2 G159E activity (IC50 ~400 nM). CATPB is shown to inhibit C3-induced intracellular ERK phosphorylation in hFFA2-expressing cells (IC50 ~3 μM against 10 mM C3).
 
C6734 CAY10397 >98%, solid Potent and selective inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-hydroxy-PGDH). Acts to prolong the lifetime and activity of endogenously produced prostaglandins both in vitro and in vivo.
 
C5374 CB-DMB ≥98% (HPLC) CB-DMB is a specific and potent inhibitor of the Na+-Ca2+exchanger (NCX); pan-inhibitor of the NA+-Ca2+exchanger isoforms.
 
SML0274 CBIO ≥95% (HPLC) CBIO is a potent, cell-permeable, D-amino acid oxidase (DAO) reversible inhibitor. In rat model, CBIO prevents formalin-induced tonic pain but not acute nociception.
 
C9749   CBiPES hydrochloride ≥98% (HPLC) CBiPES is a positive allosteric modulator of the mGlu2 receptor. CBiPES attenuates stress-induced hyperthermia and blocks the hyperlocomotor effects of PCP in murine models. In rat brain, CBiPES attenuates ketamine-induced increase in extracellular histamine concentration. This compound is a sulfonamide, different chemical class from other mGlu2R agonists in the Sigma catalog.
 
C6617 CBIQ ≥98% (HPLC), solid CBIQ is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) and the intermediate-conductance calcium-sensitive K+ channel (KCNN4). CBIQ is a novel tool for a new ion channel; first activator of ΔF508 CFTR, the mutant form of CFTR chloride channel present in 75% of cystic fibrosis patients. Other benzoquinolines act at the normal CFTR but not at ΔF508 CFTR. CBIQ also activates KCNN4, which hyperpolarizes airway epithelial cells to promote anion flux, a further benefit in cystic fibrosis.
 
SML1656 CBR-5884 ≥98% (HPLC) CBR-5884 is a cell penetrant, potent and selective noncompetitive inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) that inhibits proliferation of melanoma and breast cancer lines. CBR-5884 inhibits de novo serine synthesis in in cancer cells.
 
SML1705 Cbz-B3A ≥98% (HPLC) Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that inhibits the phosphorylation of eIF4E binding protein 1 (4EBP1) and blocks 68% of translation. Cbz-B3A binds to ubiquilins 1, 2, and 4, which prevents mTORC1 activation.
 
SML0852   CC4 ≥98% (HPLC) CC4 is a a partial agonist of α4β2 and α6β2 nicotinic acetylcholine receptors with low affinity for α3β4 and α7 containing receptors. CC4 reduces nicotine-induced self-administration and conditioned place preference without affecting motor functions.
 
SML1613 CC-401 dihydrochloride ≥95% (HPLC) CC-401 is a cell penetrant, potent and selective c-Jun N terminal kinase (JNK) inhibitor that blocks JNK signaling in the rat obstructed kidney and inhibits renal fibrosis in the unilateral ureteral obstruction model. CC-401 in combination with chemotherapy exhibits synergism in colon cancer cell lines.
 
SML0988   CCCI-01 ≥98% (HPLC) CCCI-01 induces the fomation of multipolar spindles in cancer cells containing multiple, or supernumerary centromeres. CCCI-01 leads to centromere declustering, disruption of cell cycle and apoptsis in BT-549 breast cancer cells without affecting bipolar spindles in normal primary human mammary epithelial cells.
 
SML1827 CCF642 ≥98% (HPLC) CCF642 is a cell-permeable protein disulfide isomerase (PDI) inhibitor that exhibits 100-fold higher potency than PACMA 31 (by di-E-GSSG assay) via an alternative mode of action that most likely involves PDI active-site CGHCK motifs instead of cysteine known to be targeted by PACMA 31. CCF642 displays anti-multiple myeloma (MM) activity both in cultures in vitro (IC50 <1 μM against murine 5TGM1 and nine human MM lines) and in mice in vivo (10 mg/kg, 3X i.p. per wk) without apparent adverse effects to the animals or being cytotoxic to normal bone marrow (NLBM) cells even at concentrations as high as 6.75 μM. Consistent with PDI′s role in ER protein folding process, CCF642 treatment causes acute ER stress accompanied by apoptosis-inducing calcium release in MM cells.
 
SML0987   CCG-1423 ≥98% (HPLC) CCG-1423 is a potent and specific inhibitor of Rho pathway signaling and activation of serum response factor (SRF) transcription. CCG-1423 inhibits SRF-driven luciferase expression in PC-3 cells following stimulation with constitutively active Gα13. Also CCG-1423 selectively inhibits DNA synthesis, proliferation and invasion of Rho-overexpressing cell lines.
 
SML1422 CCG-203971 ≥98% (HPLC) CCG-203971 is an inhibitor of the Rho/MKL1/SRF transcriptional pathway, which has been shown to play a role in metastasis of melanoma and breast cancer and clinically associated with castration-resistant prostate cancer. CCG-203971 is a second-generation analog of CCG-1423 (SML0987) with an IC50 of 4.2 μM vs 1 μM for CCG-1423, but less cytotoxicity. In mouse studies, CCG-203971 inhibited invasion of PC-3 prostate cancer cells and was well tolerated up to doses of 100 mg/kg IP over 5 days.

The Rho/MRTF/SRF pathway has also been shown to be involved in multiple types of solid organ fibrosis. CCG-203971 repressed both matrix-stiffness and TGF-β-mediated fibrogenesis in human colonic myofibroblasts and showed antifibrotic activity in a murine model of skin injury and in pulmonary fibrosis lung fibroblasts.
 
SML0908   CCG-50014 ≥98% (HPLC) CCG-50014 is an inhibitor of Regulators of G protein Signaling (RGS) proteins RGS4 and RGS8, which bind to the Gα -subunits of activated heterotrimeric G-proteins, and accelerate the rate of GTP hydrolysis, acting as GTPase activating proteins. CCG-50014 irreversibly binds and destabilizes RGS proteins with no affect on Gα0, while blocking GTPase activity and Gα0-dependent translocation of RGS4 to the membrane.
 
SML0016   CCG-63802 GCC-63802 binds to RGS4 and blocks interaction with Goa (IC50 = 1.9 uM). RGS4 (Regulator of G protein Signaling) is one of the RGP proteins responsible for terminating mu opioid receptor signaling. RSG proteins are GTPase activators, and drive G protein subunits to an inactive, GDP-bound form.
 
SML0249 βCCt ≥98% (HPLC) βCCt has been characterized as an α1selective antagonist and benzodiazepine mixed agonist/antagonist.. A recent study found Ki values for the GABA-A subtypes were 0.72, 15, 18.9, 110.8, and >5,000 nM at five recombinant GABAA/BzR subtypes α1, α2, α3, α5, and α6 respectively. βCCt was a near ‘neutral’ antagonist (i.e., little or no efficacy) at all these 5 recombnant GABAA/BzR receptor subtypes. βCCt has been shown to reduce alcohol self-administration in alcohol preferring (P) and high alcohol drinking (HAD) rats.
 
C9369 CCT007093 ≥98% (HPLC), powder, yellow CCT007093 is an effective PPM1D inhibitor that selectively reduces viability of human tumour cell lines.
 
SML1399 CCT031374 hydrobromide ≥98% (HPLC) CCT031374 is an inhibitor of TCF-dependent transcription. CCT031374 is a selective β-catenin signaling inhibitor that decreases the intracellular/soluble β-cat level. CCT031374 inhibits  proliferation of numberous cancer cell lines by induction of apoptosis.
 
SML0151 CCT036477 ≥98% (HPLC) CCT036477 is an inhibitor of Wnt signaling. It does not alter β-catenin levels but blocks transcription at the β-catenin level. CCT036477 inhibited growth in several cancer cell lines and showed clear activity in vivo, blocking development of Zebrafish and Xenopus embryos and expression of Wnt target genes.
 
SML1237 CCT137690 ≥98% (HPLC) CCT137690 is a very potent, orally bioavailble, pan aurora kinase inhbitor (IC50 = 15, 25, and 19 nM for Aurora A, B and C respectively). CCT137690 inhibits tumor growth in amouse xenograft model and causes multipolar spindle formation, chromosome misalignment, polyploidy and apoptosis in tumor cell lines.
 
SML1160 CD40-TRAF6 signaling inhibitor ≥98% (HPLC) CD40-TRAF6 signaling inhibitor is a small molecule that binds to TRAF6, blocking interactions with CD40. The compound inhibits CD40-induced production of IL-1b and IL-6 in primary macrophages. The compound reduces insulin resistance and adipose tissue inflammation in a mouse diet induced obesity model.
 
C5865 CD437 ≥98% (HPLC), solid CD437 is a retinoic acid receptor (RAR)γ-selective agonist, γ-selective retinoid; potent inducer of apoptosis.
human ... RARA(5914), RARB(5915), RARG(5916)
C3242 CDKi hydrochloride ≥98% (HPLC), solid CDKi hydrochloride is a potent and selective ATP competitiive inhibitor of cycB-CDK1, cycE-CDK2, and cycD1-CDK4. Demonstrates significant inhibitory activity against a variety of tumor type both in vitro and in vivo.
 
SML1682 CDN1163 ≥98% (HPLC) CDN1163 is an allosteric activator of sarco/ endoplasmic reticulum Ca2+-ATPase (SERCA) that potently lowered fasting blood glucose, improved glucose tolerance and ameliorated hepatosteatosis in ob/ob mice. Additionally CDN1163 induces significant reduction in adipose tissue weight with no change in lean mass in ob/ob mice. CDN1163 has no effect on glucose levels or body weight in lean control mice.
 
C0996 cDPCP ≥98% (HPLC), solid cDPCP is a tumor cell permeable, potent platinum-based antineoplastic agent. It is a cationic monofunctional platinum(II) complex with unique chemical and biological properties. cDPCP binds covalently only to a single DNA base (the N7 atom of a single guanosine residue), and thus forms monofunctional rather than bifunctional lesions with DNA. cDPCP effectively blocks transcription from DNA templates carrying adducts of the complex, unlike DNA lesions of other monofunctional platinum(II) compounds.
 
SML0235 CDPPB ≥98% (HPLC) Activation of metabotropic glutamate 5 receptor by CDPPB enhances the function of NMDA receptor and markers of neuronal plasticity. This improves recognition memory and cognition deficits in schizophrenia.
CDPPB is a glutamate metabotropic mGluR5 positive allosteric modulator.
 
PZ0205 CE-178253 benzenesulfonate salt ≥98% (HPLC) CE-178253 is an extremely potent and selective CB1 antagonist with sub-nanomolar potency. In binding assays, CE-178253 has a 0.33 nM Ki for human CB1, vs. a Ki of > 10 mM for human CB2.
 
SML0056   Cefotiam dihydrochloride hydrate ≥98% (HPLC) Cefotiam is a second generation cephalosporin antibiotic which has been used as a prophylatic antibiotic for MRSA.
Cefotiam, a derivative of cephalosporin, exhibits broad-spectrum anti-bacterial activity. It inhibits the cross-linking stage of peptidoglycan and blocks the synthesis of bacterial cell wall. It is resistant to β-lactamases.
 
SML0037 Ceftibuten hydrate ≥98% (HPLC) Ceftibuten is a third generation cephalosporin antibiotic
 
C0869 Celastrol ≥98% (HPLC), solid Celastrol is a potent antioxidant, and anti-inflammatory agent. It is a novel HSP90 inhibitor (disrupts Hsp90/Cdc37 complex), that exhibits anticancer (anti-angiogenic - suppresses VEGFR expression); antioxidant (inhibits lipid peroxidation) and anti-inflammatory activity (suppresses iNOS and inflammatory cytokine production).
 
PZ0008 Celecoxib ≥98% (HPLC) Celecoxib is a non-steroidal, anti-inflammatory drug (NSAID) and a cyclooxygenase-2 (COX-2) selective inhibitor. Celecoxib is at least 10-20 times more selective for COX-2 over COX-1.
 
SML1060   Celecoxib-NBD ≥98% (HPLC) Celecoxib-NBD is a flourescent COX2-specific inhibitor. The molecule binds to, and inhibits COX2 with an IC50 of 0.19 μM, and a selectivity index of 443 for COX2 vs. COX1. Celecoxib-NBD fluorescently labels COX2-expressing HCA-7 colon cells, but not COX2-negative HCT116 cells.
 
SML1801 CeMMEC13 ≥98% (HPLC) CeMMEC13 is a potent inhibitor of the second bromodomain of the transcription initiation factor TAF1 with an an IC50 value of 2.1 μM and with minimal inhibition of BRD4, BRD9, CREBBP, or EP300. CeMMEC13 was found to synergize with BRD4 inhibitor (S)-JQ1 to arrest the proliferation of leukemia cell line THP1 and lung adenocarcinoma cell line H23.
 
C7869 CEP-701 hydrate ≥98% (HPLC) CEP-701 is a Flt-3 receptor tyrosine kinase inhibitor.
 
C4991 Cephalomannine ≥97% (HPLC), solid Cephalomannine is a taxol derivative with antitumor, antiproliferative properties.
 
SMB00418 Cepharanthine ≥98% (HPLC) Cepharanthine has anticancer, anti-inflammatory, anti-allergic, immunomodulatory, anti-angiogenic, and apoptosis-inducing activities.
 
SML1269 Cepharanthine ≥95% (HPLC) Cepharanthine is an anti-inflammatory, antiallergic, immunomo- modulatory and antineoplastic alkaloid isolated from Stephania cepharantha Hayata. Cepharanthine is an inhibitor of efflux transporter ABCC10. Also, Cepharanthine binds to central portion of Hsp90 with Kd 15 nM. Recent studies suggest that Cepharanthine inhibits the entry of HIV-1 by reducing plasma membrane fluidity.
 
C8355 D-erythro-Ceramide C8 1-phosphate ≥93% (TLC), solid Cell permeable stimulator of DNA synthesis in cultured fibroblasts; antagonizes mitogenic activity.
 
C4832 Ceramide 1-phosphate from bovine brain ~95% Putative second messenger of agonist-stimulated sphingomyelin metabolism; may participate in cell regulation and transmembrane signaling.
 
C4987 Ceramide phosphorylethanolamine ≥98% (TLC) Sphingolipid with ethanolamine base, found in insect membranes.
 
C8480 D-erythro-Ceramine C8 98% (TLC), solid Inert to ceramidases; induces peak DNA fragmentation in 6 hrs; induces apoptosis in U937 cells.
 
SML0607   Ceranib-2 ≥98% (HPLC) Ceranib-2 is a nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity, decreases levels of sphingosine and sphingosine-1-phosphate (S1P), and inhibits cell proliferation.
 
SML0172   Cercosporamide from Cercosporidium henningsii ≥98% (HPLC) Cercosporamide was initially identified as a phytotoxin with broad-spectrum anti-fungal activity. Studies have shown that cercosporamide is a specific, highly potent fungal inhibitor of the cell wall integrity-signaling pathway mediator, protein kinase (Pkc1) inhibitor. Semisynthetic cercosporamide analogues demonstrated hypoglycemic activity and therefore, serve as candidates for potential new anti diabetic drugs. Cercosporamide was found to block eIF4E (Eukaryotic Initiation Factor) phosphorylation in cultured cancer cells, inducing apoptosis, suppressing proliferation, and reducing soft agar colonization. Its eIF4E phosphorylation inhibitory effect was also shown when administrated orally on xenograft human tissue and mouse liver tissue. Cercosporamide is a potent and selective Mnk inhibitor. It reduces tumor growth in xenografted HCT116 tumor and suppresses the outgrowth of B16 melanoma lung metastases. Hence, blocking Mnk function and eIF4E phosphorylation may be an attractive anticancer strategy.
 
SML0005 Cerivastatin sodium salt hydrate ≥98% (HPLC) Accumulated macrophages in atherosclerotic plaques result in plaque rupture and thrombus formation. Cerivastatin suppresses the growth of macrophages and decreases the expression of matrix metalloproteinases and tissue factor molecules, thus reduces acute coronary events.
Cerivastatin sodium is an HMG-CoA reductase inhibitor. HMG-CoA is a key enzyme in the production of cholesterol.
 
C2389 Cerulenin ≥98% (HPLC), from Cephalosporium caerulens Cerulenin, an antibiotic and antifungal, is an inhibitor of fatty acid biosynthesis; in vitro inhibition of HIV-1 proteinase.
human ... FASN(2194)
C3618 Cetirizine dihydrochloride ≥98% (HPLC) Cetirizine hydrochloride is an orally active and selective H1-receptor antagonist. Antihistaminic; Piperazines. Non-sedating type histamine H1-receptor antagonist; major metabolite of hydroxyzine. Pharmacological activity resides primarily in the (R)-isomer.
 
C5249 Cetrorelix acetate ≥98% (HPLC) Cetrorelix acetate is a luteinizing hormone releasing hormone receptor antagonist. It causes prepubertal reduction in bone modeling, bone density and bone strength comparable to post-menopausal bone loss.
 
SML0007 Cevimeline hydrochloride hemihydrate ≥95% (HPLC, NMR) Cevimeline is a muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and is used to treat the symptoms of dry mouth.
Cevimeline stimulates the peripheral muscarinic acetylcholine receptors of salivary glands and increases the concentration of Ca+2 in parotic acini and duct cells of rats. It thus acts as therapeutic agent for xerostomia.
 
C124 β-CFT naphthalenedisulfonate monohydrate solid Cocaine analog that inhibits the dopamine, norepinephrine, and serotonin transporters with Kis of 26.1 nM, 31.9 nM, and 127 nM, respectively. [11C]-β-CFT and [18F]-β-CFT are ligands for PET imaging of the dopamine transporter in vivo.
 
C2992 CFTR(inh)-172 ≥98% (HPLC), powder CFTR(inh)-172 is an inhibitor of the cystic fibrosis transmembrane conductance regulator (CFTR). With a Ki = 300 nM,. CFTR(inh)-172 leads to rapid, reversible and voltage-independent inhibition; it is an antidiarrheal agent in animals. CTFR(inh)-172 may be a useful tool to study animal models of cystic fibrosis and intestinal fluid loss in cholera and other secretory diarrheas. CTFR(inh)-172 is structurally-unrelated to known, but non-specific CFTR inhibitors DPC, NPPB (Cat. No. N4779) and Glibenclamide.
 
C9867 CGK733 ≥98% (HPLC), solid Originally published as a selective ataxia telangiectasia-mutated (ATM) and ATM- and Rad3-related (ATR) kinase inhibitor, which causes reversible reprogramming of cellular lifespan, conferred robust growth to senescent cells that had ceased proliferation.
 
C125 (±)-CGP-12177A ≥98% (HPLC), solid β-adrenoceptor nonconventional partial agonist.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
C0987 CGP-13501 ≥98% (HPLC), solid Positive allosteric modulator of GABAB receptors.
human ... GABBR1(2550), GABBR2(9568)
C231 CGP-20712A methanesulfonate salt solid, ≥98% (HPLC) CGP-20712A methanesulfonate salt is a selective β1-adrenoceptor antagonist.
human ... ADRB1(153)
C5851 CGP 35348 hydrate ≥97% (NMR), solid CGP 35348 hydrate is a GABAB-receptor antagonist.
 
SML0475 CGP36742 ≥97% (NMR) CGP36742 was the first orally active GABAB-selective antagonist. The IC50 for blocking GABAergic transmission is 36 μM. Oral administration of CGP36742 in rats blocks baclofen-induced neuronal depression, and reduces learning deficit and passive avoidance in an olfactory bulbectomy depression model.
 
C8874 CGP-37157 ≥98% (HPLC), powder Specific inhibitor of mitochondrial Na+/Ca2+ exchange as well as sarcoplasmic reticulum calcium-stimulated ATPase and possibly other calcium channels.
 
SML0050 CGP 37849 ≥98% (HPLC) CGP 37849 induces phencyclidine-like behavioral syndrome in amygdala-kindled rats that includes ataxia, locomotion and stereotypies.
CGP 37849 is a potent orally active competitive NMDA antagonist and anticonvulsant.
 
SML0058 CGP 39551 ≥98% (HPLC) CGP 39551 is an orally active competitive NMDA antagonist and anticonvulsant.
CGP 39551 produces excitatory effects and causes psychotomimetic effects in humans.
 
SML0593   CGP52432 ≥98% (HPLC) CGP52432 is a very potent antagonist of GABAB receptors. (IC50 = 85 nM).
 
C5749 CGP 52608 ≥98%, solid CGP 52608 is a specific activator of retinoic acid receptor-related orphan receptor α (RORA).
 
C7866 CGP-53353 solid Selective PKCβII inhibitor. IC50 - 410 nM for PKCβII vs 3.8 μM for PKCβI. Inhibits nPKCs and aPKCs only above 22 μM and other kinases such as protein kinase A, casein kinase I and II, c-src kinase, c-lyn kinase, c-fgr kinase, and v-abl kinase at an IC50 of greater than 50 μM.
human ... EGFR(1956)
SML0594   CGP 55845 hydrochloride ≥98% (HPLC) CGP 55845 is a potent selective GABA-B receptor antagonist with an IC50 of 5 nM.
 
C0993 CGP 57380 ≥98% (HPLC) CGP 57380 is a cell-permeable selective inhibitor of mitogen-activated protein kinase-interacting kinase 1 (MNK1).
 
SML0314 CGP77675 ≥98% (HPLC) CGP77675 is a potent Src kinase inhibitor. CGP77675 is selective toward other protein kinases including Cdc2 (>500-fold), epidermal growth factor (EGF) receptor (7.5-fold), vascular endothelial growth factor receptor (>50-fold), and for v-Abl (15-fold) and focal adhesion kinase (Fak) (>25-fold).
 
C106 CGS-12066 maleate salt solid 5-HT1B serotonin receptor agonist.
human ... HTR1B(3351)
C199 CGS-15943 solid Highly potent, non-selective adenosine receptor antagonist.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316)
C1619 CGS-9343B ≥98% (HPLC), powder CGS-9343B is a selective calmodulin antagonist with minimal protein kinase C or antidopaminergic activity. CGS-9343B is a potent inhibitor of calmodulin-activated (Type I) phosphodiesterase activity with IC50 in the nanomolar range.
 
SML0376 CGS 9895 ≥98% (HPLC) CGS 9895 is a GABA antagonist that acts via the benzodiazepine binding site of ag containing GABA receptors. CGS 9895 is the only known compound that can specifically enhance GABA-induced currents in ab subunit containing receptors, and acts at the extracellular a1+b3- subunit interface.
 
C8124 CH-223191 CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist. It inhibited TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibited TCDD-induced luciferase activity with an IC50 of 30nM. Unlike some other AhR antagonists which display agonist activity at high concentrations, CH-223191 did not stimulate AhR-dependent transcription even at 100 micromolar. It is also specific for AhR, displaying no affinity for the estrogen receptor, as some other antagonists do.
 
SML0642   Chaetoglobosin A from Chaetomium globosum, ≥98% (HPLC) Chaetomium globosum is a fungus commonly found in water-damaged walls and causes Sick Building Syndrome (SBS). Chaetoglobosin A is a mycotoxic cytochalasin. Over 40 chaetoglobosins were characterized, many of which show acute toxicity to mammals, as well as cytotoxicity to human cancer cell lines such as KB, K562, MCF-7, and HepG2.

Cytochalasins were also found to inhibit glucose transport in human erythrocytes by binding to the glucose carrier on the erythrocyte membrane. Chaetoglobosin A was found to inhibit nematode proliferation and egg hatching. It also causes mortality of second stage juveniles of Meloidogyne incognita.
 
C7870 Chalcone 4 hydrate ≥98% (HPLC) Chalcone 4 is a potent, selective inhibitor of the chemokine CXCL12 via direct binding. It is also a small molecule anti-ligand (or neutraligand) of CXCR4 and CXCR7. The chemokine CXCL12 (stromal cell-derived factor-1) and its receptors play pivotal roles in inflammatory responses, normal vascular and neuronal development, as well as in infectious diseases and cancer. Chalcone 4 binds to and activates the chemokine receptors CXCR4 and CXCR7 and stimulates a rapid receptor-mediated intracellular calcium mobilization and signaling through a Pertussis toxin sensitive Gi protein. Chalcone 4 potently and selectively inhibits CXCL12 binding to CXCR4 and CXCR7, and consequent CXCL12-evoked calcium cellular responses. Chalcone 4 binds to the chemokine CXCL12, but not to its receptors.
 
C5856   Charybdotoxin, recombinant from Leiurus quinquestriatus hebraeus recombinant, expressed in E. coli, lyophilized powder Exhibits the same activity as the natural form of the toxin
 
SML0368 CHD-5 ≥98% (HPLC) CHD-5 is a potent aryl hydrocarbon receptor antagonist.
 
C2932 Chelerythrine chloride ≥95% (TLC), powder Chelerythrine affects translocation of PKC from cytosol to plasma membrane. Chelerythrine prevents neurite growth and induces apoptosis in a concentration- and schedule-dependent manner.
 
C9623   Chetomin from Chaetomium cochliodes, ≥98% (HPLC) Chetomin is a natural metabolite produced by several species of the genus Chaetomium. Chetomin is an epidithiodioxopiperazine known to disrupt the hypoxia-inducible factor (HIF) pathway. Chetomin blocks the interaction of HIF1α and HIF2α with transcriptional co-activators p300 and cAMP response element binding (CREB) binding protein (CBP), thereby attenuating hypoxia-inducible transcription. Disrupting the ability of tumors to adapt to hypoxia leads to decreased tumor growth and can serve as an antitumor stratagy. Chetomin also suppresses the proliferation of LPS-induced mouse spleen lymphocytes.
Chetomin is a natural metabolite produced by several species of the genus Chaetomium. Chetomin disrupts the hypoxia-inducible factor (HIF) pathway, blockomg the interaction of HIF1α and HIF2α with transcriptional co-activators p300 and cAMP response element binding (CREB) binding protein (CBP), thereby attenuating hypoxia-inducible transcription. Disrupting the ability of tumors to adapt to hypoxia leads to decreased tumor growth; hypoxia can also promote resistance to radiotherapeutics. By both of these mechanisms, chetomin shows promise as a lead compound in antitumor research. Chetomin also suppresses the proliferation of LPS-induced mouse spleen lymphocytes.
 
C8742 CHIC-35 ≥97% (chiral, HPLC) CHIC-35 is cell-permeable, metabolically stable, and very potent inhibitor of SIRT1; IC50 of S-isomer is 60 nM; IC50 of mixed isomers is 124 nM. There is no inhibition of SIRT3 or HDAC. The IC50 for SIRT2 is 2.77 μM. Sirtuins are protein deacetylases, which represent a new class of histone deacetylases (HDAC) involved in gene silencing. SIRT modulators are potential therapeutics for cancer, diabetes, muscle differentiation, heart failure, neurodegeneration, and aging.
 
SML1094 CHIR 98014 ≥98% (HPLC) CHIR 98014 is a glycogen synthase kinase-3 (GSK-3) inhibitor with IC50 values of 0.65 nM and 0.58 nM for GSK3α and GSK3β, respectively. CHIR98014 is 500-fold to >10,000-fold selectivity for GSK-3 versus 20 other protein kinases tested, including closest homologs Cdc2 and ERK2.
 
SML1046 CHIR99021 ≥98% (HPLC) CHIR99021 is a very potent inhibitor of Glycogen synthase kinase 3 (GSK3, IC50 values for GSK3α and GSK3β = 10 and 6.7 nM, respectively). There is no cross-reactivity against CDKs. CHIR99201 potentiates self-renewal of human and mouse embryonic stem cells, and enhances reprogramming of somatic cells into stem cells.
 
C3742 Chk2 Inhibitor II hydrate ≥98% (HPLC) Chk2 Inhibitor II is a checkpoint kinase 2 inhibitor, which controls the p53 response to DNA breaks induced by radiation, leading to apoptosis. Protection of T-cells from apoptosis implies use as an adjuvant for radiation therapy in cancer. IC50 = 15 nM; Ki = 37 nM. Chk2 Inhibitor II shows 1000-fold greater selectivity for the Chk2 serine/threonine kinase than for the Cdk1/B and CK1 kinases (for which IC50 = 12 μM and 17 μM, respectively). Chk2 Inhibitor II weakly inhibits a panel of 31 other kinases (<25% inhibition at a concentration of 10 μM and prevents apoptosis of human CD4+ and CD8+ T-cells subjected to ionizing radiation (EC50 = 3 μM and 7.6 μM, respectively).
human ... CHEK2(11200)
C8383 Chloral hydrate Chloral hydrate is a sedative/hypnotic.
 
C8849   α-Chloralose−HBC complex ≥92% α-anomer basis    
C0253 Chlorambucil Chlorambucil is an anti-cancer drug that alkylates DNA and induces apoptosis. Death of chronic lymphocytic leukemia cells occurs via a p53-dependent mechanism.
human ... CYP2D6(1565)
SML1473 Chlorcyclizine ≥98% (HPLC) Chlorcyclizine is a first-generation antihistamine being studied as a potential treatment for hepatitis C. Chlorcyclizine is believed to inhibit an early stage of HCV infection, targeting viral entry into host cells. Chlorcyclizine inihbited the entry of cell culture-produced HCV with an IC50 value 2.3 nM. In human hepatoma cells and primary human hepatocytes, Chlorcyclizine showed a synergistic effect with other hepatitis C drugs such as ribavirin, interferon, telaprevir, boceprevir, sofosbuvir, daclatasvir, and cyclosporin A.
 
C5366 Chlorisondamine diiodide ≥98% (HPLC), white solid Irreversible, long-lasting nicotinic acetylcholine receptor antagonist.
 
C1240 Chlormethiazole hydrochloride ≥98% (HPLC), powder GABAA agonist; glycine receptor modulator.
 
O001 β-Chlornaltrexamine dihydrochloride solid Irreversible μ, δ and κ opioid receptor antagonist.
 
C5134 2-Chloroadenosine Selective A1 adenosine receptor agonist.
human ... ADORA1(134), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
C1081 8-Chloroadenosine 3′,5′-cyclic-monophosphate ≥85% Membrane-permeable cAMP analog; resistant to hydrolysis by phosphodiesterases.
 
C0610 8-Chloroadenosine-3′,5′-cyclic monophosphorothioate, Rp-isomer ≥99% (HPLC) Competitive inhibitor of cyclic AMP-dependent protein kinase A (PKA) type I. Membrane-permeable analog of the cAMP inhibitor Rp-cAMPS (Prod. No. A-165).
 
C9635 DL-p-Chloroamphetamine hydrochloride ≥94% (HPLC) Neurotoxic on prolonged administration or at high dosage; substrate for the serotonin transporter that releases serotonin from axon terminals by a nonexocytotic mechanism and blocks the reuptake of serotonin; inhibits tryptophan hydroxylase.
 
C130 Chloro-APB hydrobromide solid Full D1 dopamine receptor agonist.
human ... DRD1(1812)
C1610 1-(4-Chlorobenzyl)-5-methoxy-2-methylindole-3-acetic acid >98% (HPLC) Putative inhibitor of multidrug resistance-associated protein 1 (MRP1).
human ... ABCC1(4363)
C4528 Chlorobimane    
C5174 4′-Chlorodiazepam ≥98% (TLC) 4′-Chlorodiazepam (Ro5-4864) is a potent selective ligand for the mitochondrial translocator protein 18kDa (TSPO), formerly known as the peripheral benzodiazepine receptor (PBR). Ro5-4864 does not bind to GABA(A) receptors and lacks typical benzodiazepine effects, but has been found to be neuroprotective in several studies.
rat ... Tspo(24230)
C8417 N-(2-Chloroethyl)-N-ethyl-2-bromobenzylamine hydrochloride ≥98%, solid Adrenergic neurotoxin that induces acute and relatively selective degeneration of both central and peripheral noradrenergic nerve terminals.
 
SML0447 3-Chloro-5-hydroxybenzoic acid ≥97% (HPLC) 3-Chloro-5-hydroxybenzoic acid is a selective agonist of the lactate receptor, GPR81. Stimulation of either GPR81 or GPR109a in adipose tissue leads to a similar decrease in triglyceride lipolysis. Niacin is used to treat dyslipidemia via its agonism of GPR109a, but compliance is low due to side effects (flushing and pruritus), which are associated with GPR109a agonism. 3-Chloro-5-hydroxybenzoic acid is selective for GPR81 over other GPCRs, including GPR109a. While less potent than niacin (16 vs. 0.78 μM), it has similar activity as the same dose as niacin in animal studies and should not cause the flushing that is associated with niacin.
 
S143 (±)-6-Chloro-PB hydrobromide ≥98% (HPLC), solid (+/-)-6-Chloro-PB HBr is a full D1 dopamine receptor agonist.
human ... DRD1(1812)
C144 1-(3-Chlorophenyl)biguanide hydrochloride solid Very potent 5-HT3 serotonin receptor agonist.
human ... HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242)
C3912 8-(4-Chlorophenylthio)adenosine 3′,5′-cyclic monophosphate sodium salt ≥97.0% (HPLC), powder Membrane permeable cAMP analog. Used as a selective activator of cAMP dependent protein kinase (PKA). Inhibits cGMP-dependent phosphodiesterase and, at higher concentrations, inhibits cAMP-dependent phosphodiesterase. Inhibits phosphoinositide hydrolysis and secretion stimulated by n-formyl-Met-Leu-Phe but not platelet-activating factor in leukocytes. Renders HL-60 cells more resistant to NO-induced DNA damage.
human ... PRKAR1A(5573), PRKAR1AP(5574), PRKAR1B(5575), PRKAR2A(5576), PRKAR2B(5577)
C0735 8-(4-Chlorophenylthio)adenosine-3′,5′-cyclic Monophosphorothioate, Rp-isomer sodium salt ≥99% (HPLC), solid Lipophilic analog of the competitive inhibitor of protein kinase A (cyclic AMP antagonist).
 
C5438 8-(4-Chlorophenylthio)-guanosine 3′,5′-cyclic monophosphate sodium salt ≥95% (HPLC), powder Membrane-permeable analog of cGMP that does not affect cGMP-regulated phosphodiesterase. A more potent cGMP analog than 8-Br-cGMP due to greater membrane permeability and a higher resistance to hydrolysis by phosphodiesterase. Used as a selective activator of cGMP dependent protein kinase (PKG). Found to be a very potent cyclic nucleotide-gated channel agonist.
 
C240 8-(4-Chlorophenylthio)-guanosine 3′,5′-cyclic monophosphorothioate, Rp Isomer triethylammonium salt ≥98% (HPLC), solid Rp-8-CPT-cGMP is a potent inhibitor of protein kinase G Ia, Ib, and type II.
 
C8988 8-(4-Chlorophenylthio)-2′-O-methyladenosine 3′,5′-cyclic monophosphate monosodium hydrate ≥98% (HPLC) Analog of natural cAMP, potent and specific membrane-permeant activator of exchange factors directly activated by cAMP (Epac or cAMP-GEF), a new receptor for cyclic AMP
 
C6628 Chloroquine diphosphate salt solid, ≥98% Standard anti-malarial drug. Substrate for MRP in multidrug resistant cell line and inhibits photoaffinity labeling of MRP by quinoline-based photoactive drug IAAQ (N-[4-[1-hydroxy-2-(dibutylamino)ethyl]quinolin-8-yl]-4-azidosalicylamide).
human ... ABCC1(4363)
C197 8-(3-Chlorostyryl)caffeine ≥98% (HPLC), solid Selective A2A adenosine receptor antagonist.
human ... ADORA2A(135)
mouse ... Maob(109731)
rat ... Adora1(29290), Adora2a(25369)
C5238   Chlorotoxin from Leiurus quinquestriatus (north Africa) recombinant, expressed in E. coli, ≥98% (HPLC), lyophilized powder Potent blocker of small-conductance Cl- channels.
 
C3025 (±)-Chlorpheniramine maleate salt ≥99% (perchloric acid titration) H1 Histamine receptor antagonist.
human ... HRH1(3269)
C4915 S-(+)-Chlorpheniramine maleate salt H1 histamine receptor antagonist; active isomer.
Chlorpheniramine maleate is clinically used as a topical ointment to treat skin disorders such as sunburn, urticaria, angioedema, pruritus and insect bites.
human ... HRH1(3269)
C8138 Chlorpromazine hydrochloride ≥98% (TLC) Chlorpromazine demonstrates cytotoxic and antiproliferative activity against leukemic cells, but does not affect the viability of normal lymphocytes.
Phenothiazine antipsychotic; D2 dopamine receptor antagonist, H1 histamine receptor antagonist; inhibits calmodulin-dependent stimulation of cyclic nucleotide phosphodiesterase and nitric oxide synthase.
human ... DRD2(1813), HRH1(3269)
C1671 Chlorprothixene hydrochloride D2 dopamine receptor antagonist; blocks a subset of GABAA receptors in rat cortex that is also blocked by clozapine; thioxanthine antipsychotic.
human ... DRD2(1813)
SML0591   Chlorthalidone ≥98% (HPLC) Chlorthalidone is a thiazide-like diuretic, an inhibitor of the Na+-Cl- cotransporter. Chlorthalidone inhibits sodium ion transport across the renal tubular epithelium increasing the delivery of sodium to the distal renal tubule and indirectly increasing potassium excretion via the sodium-potassium exchange mechanism. Chlorthalidone also promotes Ca++ reabsorption by an unknown mechanism. Several recent comparison studies inidcate that chlorthalidone may be a better drug in preventing cardiovascular events than hydrochlorothiazide.
 
C4397 Chlorzoxazone Chlorzoxazone is a skeletal muscle relaxant.
 
C1244 CHM-1 hydrate ≥99% (HPLC), solid CHM-1 possess antimitotic antitumor activity. It is a potent and selective antitumor agent in human hepatocellular carcinoma. CHM-1 induces apoptosis, and it binds tubulin and inhibits tubulin polymerization.
 
C7628 5β-Cholanic acid ≥99% (TLC)    
C2525 5β-Cholanic acid-3α,12α-diol 3-acetate methyl ester    
C2400 5α-Cholanic acid-3α-ol-6-one 3-acetate methyl ester ~97%    
C9774 Cholecalciferol analytical standard Vitamin D acts through a receptor that is a member of the ligand-dependent transcription factor superfamily. Modulates the proliferation and differentiation of both normal and cancer cells. Has antiproliferative and antimetastatic effects on breast, colon, and prostate cancer cells. Activated vitamin D receptors in intestine and bone maintain calcium absorbance and homeostasis.
 
C8772   Cholera filtrate lyophilized powder    
C8052   Cholera Toxin from Vibrio cholerae ~95% (SDS-PAGE), lyophilized powder Toxin consisting of an A subunit (27 kDa) surrounded by five B subunits (approximately 12 kDa each), which attach the toxin to ganglioside GM1 on the cell surface. The A subunit catalyzes ADP-ribosylation of the α-subunit of the stimulatory G protein (Gαs), reducing GTPase activity and activating the α-subunit. This activation of Gαs leads to an increase in the activity of adenylyl cyclase, resulting in increased levels of cAMP. Also ADP-ribosylates transducin in the eye rod outer segments, inactivating its GTPase activity. Cholera toxin has also been reported to ADP-ribosylate tubulin. Shown to be a potent mucosal vaccine adjuvant, inducing T helper cell type 2 responses by inhibiting the production of interleukin-12.
 
C8180   Cholera Toxin A Subunit from Vibrio cholerae lyophilized powder Catalyzes ADP-ribosylation of the α-subunit of G proteins, reducing GTPase activity and activating the α-subunit; also catalyzes ADP-ribosylation of cell membrane adenylyl cyclase
 
C9903   Cholera Toxin B subunit ≥95% (SDS-PAGE), lyophilized powder The cholera toxin B subunit is used for track tracing in neurological research, taking advantage of GM1 ganglioside binding and retrograde transport. Tissue culture cells treated with cholera toxin are not killed and tissues of animals do not become necrotic.
 
C167   Cholera Toxin B subunit solid The cholera toxin B subunit is used for track tracing in neurological research, taking advantage of GM1 ganglioside binding and retrograde transport. Tissue culture cells treated with cholera toxin are not killed and tissues of animals do not become necrotic.
 
C9972   Cholera Toxin B subunit biotin conjugate, lyophilized powder The cholera toxin B subunit is used for track tracing in neurological research, taking advantage of GM1 ganglioside binding and retrograde transport. Tissue culture cells treated with cholera toxin are not killed and tissues of animals do not become necrotic.
 
C1655   Cholera Toxin B subunit FITC conjugate, lyophilized powder The cholera toxin B subunit is used for track tracing in neurological research, taking advantage of GM1 ganglioside binding and retrograde transport. Tissue culture cells treated with cholera toxin are not killed and tissues of animals do not become necrotic.
 
C3741   Cholera Toxin B subunit peroxidase conjugate (Contains ~ 2 moles HRP/mole of CTB. ~100 μg HRP conjugated to ~45 μg CTB), lyophilized powder The cholera toxin B subunit is used for track tracing in neurological research, taking advantage of GM1 ganglioside binding and retrograde transport. Tissue culture cells treated with cholera toxin are not killed and tissues of animals do not become necrotic.
 
C8128 5α-Cholestan-3-one crystalline    
C1145   Cholesterol–PEG 600    
C2832 Cholesteryl 3β-N-(di­methyl­amino­ethyl)­carbamate hydrochloride ≥95%    
C7259 Cholesteryl erucate ≥95%    
C6399 Cholesteryl n-valerate ≥90% (HPLC; detection at 205 nm)    
C1629 Choline bitartrate Acyl group acceptor
 
C1879 Choline chloride ≥98% The enzymatic activities of butyrylcholinesterase (BChE) and paraoxonase 1 (PON1), two serum enzymes synthesized by the liver and related with inflammation, were decreased in a sepsis animal model injected with LPS. Choline chloride administered intravenously at 20 mg/kg body weight prevents the LPS-mediated decreases in the activities of these two enzymes .
 
C7743 CHPG ≥98% (HPLC), white solid CHPG is a selective, potent mGluR5 agonist. CHO cells expressing mGluR5 (but not those expressing mGluR1) are activated by CHPG. In vivo, CHPG stimulates thalamic neurons and is antagonized by MPEP (selective mGluR5 antagonist); CHPG potentiates NMDA and AMPA responses in spinal cord and produces oscillations in intracellular calcium in dorsal root ganglion cells.
 
SML0648 CHR-6494 trifluoroacetate salt ≥98% (HPLC) CHR-6494 is a potent and selective Haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase) inhibitor that blocks H3T3ph phosphorylation. CHR-6494 causes cell cycle arrest in G2/M and subsequent apoptosis. CHR-6494 causes an abnormal duplication of centrosomes and mitotic catastrophe in cancer cells.
 
C2615 Chromanol 293B ≥98% (HPLC), powder Blocker of the slow delayed rectifier K+ current via KCNQ1 channels
 
C0868 Chromeceptin ≥98% (HPLC), solid Chromeceptin inhibits Insulin-like growth factor 2 (IGF2) signaling by a process that begins with chromeceptin binding to multifunctional protein 2 (MFP-2). This interaction stimulates the expression of IGF binding protein 1 (IGFBP-1) and suppressor of cytokine signaling-3 (SOCS-3), both of which activate signal transducers and activators of transcription 6 (STAT6) to attenuate IGF signals.
 
C2659 Chromomycin A3 from Streptomyces griseus ≥95% (HPLC) An antibiotic exhibiting anti-bacterial, anti-fungal and antitumor activities. Serves as a fluorescent DNA stain. Useful for the detection of protamine deficiency in sperm chromatin. The compound blocks macromolecule synthesis by a specific, reversible interaction with DNA in the presence of bivalent metal ions. Binding to DNA minor groove mediates an efficient competitive inhibition of DNA gyrase and significantly affects topoisomerase II activity.
 
C1115 Chrysamine G ≥95% (HPLC), solid New probe for ß-amyloid aggregates.
 
C6491 Chrysomycin B ≥98% (HPLC), solid Antibiotic from Streptomyces sp. Inhibits the catalytic activity of human topoisomerase II. Exhibits antitumor activity against human cell lines K562, HT29, MCF7, PC6, and MKN28.
 
SML1508 C-DIM12 ≥98% (HPLC) C-DIM12 is a potent and selective nuclear receptor Nurr1 (NR4A2) activator that activates Nurr1 in urothelial carcinoma cells and in pancreatic cells. C-DIM12 suppresses inflammatory signaling in microglia.
 
SML1238   Ertapenem sodium ≥90% (HPLC) Ertapenem is a broad spectrum carbopenem antibiotic. Ertapenem is active against both gram-positive and gram-negative bacteria. Ertapenem shows an extended duration of action in vivo due to its reversible binding to serum protein.
 
SML0067 IOX1 ≥97% (HPLC) IOX1 (5-Carboxy-8-hydroxyquinoline) is a broad spectrum inhibitor of 2-oxoglutarate (2OG) oxygenases, including Jumonji C domain (JmjC) demethylases. It is useful for the study of histone demethylation and hypoxic sensing and results in translocation of active site iron on the 2OG oxygenases. For full characterization details, please visit the IOX1 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc