gc-a

SGC-AAK1-1, a potent and selective inhibitor of AAK1 (AP2-associated kinase 1), has an IC50 of 270 nM and a Ki of 9 nM, and serves as a chemical probe.

SGC-AAK1-1N is a potent and selective inhibitor of AAK1 (AP2 associated kinase 1), with an IC50 of 1.8 μM [1].

NCGC00092410 (ML008) is a glucocerebrosidase (GC) inhibitor with IC50 value of 31 nM. It can be used for the study of Gaucher disease caused by mutation of glucocerebrase gene.

Betaine chloride (Betaine hydrochloride) is an acidic form of betaine, a vitamin-like substance observed in grains and other foods; gains the amplification of DNA by decreasing the formation of secondary structure in GC-rich regions.

Docosane [Standard Material for GC] is a natural product.

Lexibulin (CYT-997)(CYT-997) is a potent tubulin polymerization inhibitor (IC50: 10-100 nM, in Y cell lines). Lexibulin blocks the formation of the mitotic spindle and leading to cell cycle arrest at the G2 M phase; this may result in disruption of the tumor vasculature and tumor blood flow, and tumor cell death.

BI 653048 phosphate is a selective, orally active agonist of nonsteroidal glucocorticoid (GC) with an IC50 of 55 nM.

Chromomycin A3 is an antibiotic produced by Streptomyces sp that binds to gc-rich DNA sequences in the presence of divalent cations and inhibits DNA replication and transcription; it is also used as a fluorescent DNA stain and assay; and it has anticancer activity against diseases such as Hodgkin's, lung adenocarcinomas, melanomas, and breast cancer.

GC 14 is a selective thyroid hormone receptor antagonist with IC50 values of 200 nM for hTRα and 35 nM for hTRβ.

Glutaminyl Cyclase Inhibitor 3, a designed anti-Alzheimer's compound, is a potent human Glutaminyl Cyclase (GC) inhibitor (IC50: 4.5 nM). It significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.

Plecanatide acetate is a agonist of guanylate cyclase-C (GC-C) receptor( EC50 of 190 nM in T84 cells), and shows anti-inflammatory activity in models of murine colitis.

SU16f (3-substituted indolin-2-one 16f) is a potent and selective PDGFRβ inhibitor (IC50s: 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively). Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs conditioned medium in gastric cancer cell proliferation and migration.

WK500B is a BCL6 inhibitor that binds to BCL6 within cells, obstructing the BCL6 repression complex and reactivating target genes of BCL6, which leads to the death of DLBCL cells and induces apoptosis and cell cycle arrest. In animal models, WK500B inhibits the formation of germinal centers (GC) and the growth of DLBCL tumors without toxic side effects. Moreover, WK500B demonstrates strong efficacy and favorable pharmacokinetic properties, indicating significant development potential.

GC-072 is a potent 4-oxoquinolizine antibiotic that selectively inhibits bacterial topoisomerase. It shows in vitro activity against both sensitive and resistant strains of B. pseudomallei, and it is also effective against other dangerous pathogens such as Burkholderia mallei, Bacillus anthracis, Yersinia pestis, and Francisella tularensis. In a murine model of melioidosis, oral administration of GC-072 demonstrated dose-dependent survival benefits, indicating its potential as a first-line oral treatment option for melioidosis.

13C15-Nivalenol is intended for use as an internal standard for the quantification of nivalenol by GC- or LC-MS. Nivalenol is a trichothecene mycotoxin that has been found inFusarium.1It is lethal to mice (LD50= 6.9 mg/kg).2Nivalenol (5, 10, and 15 mg/kg) also induces thymic, splenic, and Peyer's patch cell apoptosis in mice.3 1.Yang, Z., Concannon, J., Ng, K.S., et al.Tetrandrine identified in a small molecule screen to activate mesenchymal stem cells for enhanced immunomodulationSci. Rep.630263(2016) 2.Yoshizawa, T., and Morooka, N.Studies on the toxic substances in the infected cereals (part 3): Acute toxicities of new trichothecene mycotoxins: Deoxynivalenol and its monoacetateJ. Food Hyg.15(4)261-269(1974) 3.Poapolathep, A., Ohtsuka, R., Kiatipattanasakul, W., et al.Nivalenol-induced apoptosis in thymus, spleen and Peyer's patches of miceExp. Toxicol. Pathol.53(6)441-446(2002)

3-Acetyldeoxy nivalenol-13C17is intended for use as an internal standard for the quantification of 3-acetyldeoxy nivalenol by GC- or LC-MS. 3-Acetyldeoxy nivalenol is a mycotoxin that has been found inF. graminearum.1In vivo, 3-acetyldeoxy nivalenol (40 mg/kg) induces duodenal and splenic cell necrosis, as well as lethality (LD50= 70 mg/kg) in mice.2 1.Jiao, F., Kawakami, A., and Nakajima, T.Effects of different carbon sources on trichothecene production and Tri gene expression by Fusarium graminearum in liquid cultureFEMS Microbiol.Lett.285(2)212-219(2008) 2.Schiefer, H.B., Nicholson, S., Kasali, O.B., et al.Pathology of acute 3-acetyldeoxynivalenol toxicity in miceCan. J. Comp. Med.49(3)315-318(1985)

4-deoxy Nivalenol-13C15is intended for use as an internal standard for the quantification of 4-deoxy nivalenol by GC- or LC-MS. 4-deoxy Nivalenol is a trichothecene mycotoxin that has been found inFusarium.1It binds to eukaryotic ribosomes and inhibits protein synthesis in mice when administered at doses ranging from 5 to 25 mg/kg. 4-deoxy Nivalenol (0.1 and 0.2 mg/kg) induces emesis in pigs and decreases feed consumption in pigs when administered at a dose of 40 ppb in the diet.2It induces lethality in mice (LD50= 46-78 mg/kg).34-deoxy Nivalenol has been found inF. graminearum-infected cereal grains such as wheat, barley, and corn. 1.Pestka, J.J., and Smolinski, A.T.Deoxynivalenol: Toxicology and potential effects on humansJ.Toxicol.Environ.Health B.Crit.Rev.8(1)39-69(2005) 2.Forsyth, D.M., Yoshizawa, T., Morooka, N., et al.Emetic and refusal activity of deoxynivalenol to swineAppl. Environ. Microbiol.34(5)547-552(1977) 3.Pestka, J.J.Deoxynivalenol: Mechanisms of action, human exposure, and toxicological relevanceArch. Toxicol.84(9)663-679(2010)

Aflatoxin B2-13C17(AFB2-13C17) is intended for use as an internal standard for the quantification of AFB2by GC- or LC-MS. AFB2is a mycotoxin that has been found inA. terricola.1It induces hepatic autophagy and apoptosis in broiler chickens when administered at doses of 0.2, 0.4, and 0.8 mg/kg.2AFB2(0.5 and 1 mg/animal) also induces parenchymal cell hyperplasia in rats.3 1.Moubasher, A.H., el-Kady, I.A., and Shoriet, A.Toxigenic Aspergilli isolated from different sources in EgyptAnn. Nutr. Aliment.31(4-6)607-615(1977) 2.Chen, B., Li, D., Li, M., et al.Induction of mitochondria-mediated apoptosis and PI3K/Akt/mTOR-mediated autophagy by aflatoxin B2 in hepatocytes of broilersOncotarget7(51)84989-84998(2016) 3.Wogan, G.N., Edwards, G.S., and Newberne, P.M.Structure-activity relationships in toxicity and carcinogenicity of aflatoxins and analogsCancer Res.31(12)1936-1942(1971)

Aflatoxin G1-13C17is intended for use as an internal standard for the quantification of aflatoxin G1by GC- or LC-MS. Aflatoxin G1is a mycotoxin that has been found inA. terricola.1In vivo, aflatoxin G1is lethal to ducklings (LD50= 1.18 mg/kg).2It induces hepatocellular carcinoma tumor formation and lethality in rats when administered at doses of 1.4 and 3 mg/animal, respectively. Aflatoxin G1also inhibits liver and kidney succinate dehydrogenase and fumarase, as well as kidney cytochrome oxidase, NADH oxidase, α-glycerophosphate dehydrogenase, isocitrate dehydrogenase, and malate dehydrogenase in rats.3 1.Moubasher, A.H., el-Kady, I.A., and Shoriet, A.Toxigenic Aspergilli isolated from different sources in EgyptAnn. Nutr. Aliment.31(4-6)607-615(1977) 2.Wogan, G.N., Edwards, G.S., and Newberne, P.M.Structure-activity relationships in toxicity and carcinogenicity of aflatoxins and analogsCancer Res.31(12)1936-1942(1971) 3.Bai, N.J., Pai, M.R., and Venkitasubramanian, T.A.Mitochondrial function in aflatoxin toxicityIndian J. Biochem. Biophys.14(4)347-349(1977)

Aflatoxin G2-13C17is intended for use as an internal standard for the quantification of aflatoxin G2by GC- or LC-MS. Aflatoxin G2is a mycotoxin that has been found inAspergillus.1It is lethal to ducklings (LD50= 2.83 mg/kg) but is non-toxic to rats when administered at a dose of 200 mg/kg.2 1.Bennett, J.W., and Klich, M.MycotoxinsClin. Microbiol. Rev.16(3)497-516(2003) 2.Wogan, G.N., Edwards, G.S., and Newberne, P.M.Structure-activity relationships in toxicity and carcinogenicity of aflatoxins and analogsCancer Res.31(12)1936-1942(1971)

Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD). 1.Jasper, J.R., Lesnick, J.D., Chang, L.K., et al.Ligand efficacy and potency at recombinant α2 adrenergic receptors: Agonist-mediated [35S]GTPγS bindingBiochem. Pharmacol.55(7)1035-1043(1998) 2.Nikolic, K., Filipic, S., and Agbaba, D.QSAR study of imidazoline antihypertensive drugsBioorg. Med. Chem.16(15)7134-7140(2008) 3.Scholtysik, G.Pharmacology of guanfacineBr. J. Clin. Pharmacol.10(Suppl 1)21S-24S(1980) 4.Kauser, H., Sahu, S., Kumar, S., et al.Guanfacine is an effective countermeasure for hypobaric hypoxia-induced cognitive declineNeuroscience254110-119(2013)

2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B osteosarcoma cells cultured under hypoxic conditions when used at a concentration of 2 mg ml.4,5In vivo, 2-deoxy-D-glucose (500 mg kg) reduces tumor growth in 143B osteosarcoma and MV522 non-small cell lung cancer mouse xenograft models when used alone or in combination with doxorubicin or paclitaxel .6 1.Kang, H.T., and Hwang, E.S.2-Deoxyglucose: An anticancer and antiviral therapeutic, but not any more a low glucose mimeticLife Sci.78(12)1392-1399(2006) 2.Aft, R.L., Zhang, F.W., and Gius, D.Evaluation of 2-deoxy-D-glucose as a chemotherapeutic agent: Mechanism of cell deathBr. J. Cancer87(7)805-812(2002) 3.Ralser, M., Wamelink, M.M., Struys, E.A., et al.A catabolic block does not sufficiently explain how 2-deoxy-D-glucose inhibits cell growthProc. Natl. Acad. Sci. USA105(46)17807-17811(2008) 4.Liu, H., Savaraj, N., Priebe, W., et al.Hypoxia increases tumor cell sensitivity to glycolytic inhibitors: A strategy for solid tumor therapy (Model C)Biochem. Pharmacol.64(12)1745-1751(2002) 5.Zhang, X.D., Deslandes, E., Villedieu, M., et al.Effect of 2-deoxy-D-glucose on various malignant cell lines in vitroAnticancer Res.26(5A)3561-3566(2006) 6.Maschek, G., Savaraj, N., Priebe, W., et al.2-deoxy-D-glucose increases the efficacy of adriamycin and paclitaxel in human osteosarcoma and non-small cell lung cancers in vivoCancer Res.64(1)31-34(2004)

Oleic acid-13C is intended for use as an internal standard for the quantification of oleic acid by GC- or LC-MS. Oleic acid is a monounsaturated fatty acid and a major component of membrane phospholipids that has been found in human plasma, cell membranes, and adipose tissue.1,2 It contributes approximately 17% of the total fatty acids esterified to phosphatidylcholine, the major phospholipid class in porcine platelets.1 Oleic acid inhibits collagen-stimulated platelet aggregation by approximately 90% when used at a concentration of 10 μg/ml. It also inhibits fMLF-induced neutrophil aggregation and degranulation by 55 and 68%, respectively, when used at a concentration of 5 μM, similar to arachidonic acid .3 Oleic acid (60 μM) induces release of intracellular calcium in human platelets.4

Lauric acid-13C is intended for use as an internal standard for the quantification of lauric acid by GC- or LC-MS. Lauric acid is a medium-chain saturated fatty acid. It has been found at high levels in coconut oil.1Lauric acid induces the activation of NF-κB and the expression of COX-2, inducible nitric oxide synthase (iNOS), and IL-1α in RAW 264.7 cells when used at a concentration of 25 μM.2