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GSK321
GSK321 is a highly potent, selective inhibitor of mutant IDH1 enzymes, with IC50=4.6 nM against R132H, 3.8 nM against R132C and 2.9 nM against R132G. GSK321 stably decreased 2-hydroxyglutarate (2-HG) production in several different IDH1 mutant AML cells within a 2-3 week time frame ex vivo. Because of the allosteric nature of the interaction, GSK321 is able to inhibit multiple mutant forms of IDH1, which is consistent with our cell biological observations. Furthermore, GSK321 retains excellent potency in cells, since it does not compete with the tightly bound cofactor. Synonyms: (7R)-1-[(4-fluorophenyl)methyl]-N-[3-[(1S)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrole-2-carbonyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-3-carboxamide; (7R)-1-[(4-fluorophenyl)methyl]-N-[3-[(1S)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrole-2-carbonyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-3-carboxamide; GSK321; GSK 321; GSK-321; BDBM195601. Grades: >98%. CAS No. 1816331-63-1. Molecular formula: C28H28FN5O3. Mole weight: 501.56.
GSK343
GSK343 is a potent, selective inhibitor of EZH2 with cellular activity. GSK343 inhibits EZH2 with an IC50 of 4nM and is over 1000-fold selective for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC50 of <200nM as measured by immunofluorescence. GSK343 exhibited limited effects on the growth of EOC cells in conventional two-dimensional (2D) culture. In contrast, GSK343 significantly suppressed the growth of EOC cells cultured in 3D matrigel extracellular matrix (ECM), which more closely mimics the tumor microenvironment in vivo. Notably, GSK343 induces apoptosis of EOC cells in 3D but not 2D culture. In addition, GSK343 significantly inhibited the invasion of EOC cells. Synonyms: GSK343; GSK-343; GSK 343. CAS No. 1346704-33-3. Molecular formula: C31H39N7O2. Mole weight: 541.7.
GSK-345931A
GSK-345931A is an EP(1) receptor antagonist. It is efficient in preclinical models of inflammatory pain. Uses: Inflammatory pain. Synonyms: 869499-38-7(sodium); 6-(5'-chloro-2'-(2-methylpropoxy)(1,1'-biphenyl)-2-yl)- 2-Pyridinecarboxylic acid. Grades: 98%. CAS No. 869534-13-4. Molecular formula: C22H20ClNO3. Mole weight: 381.86.
GSK-345931A sodium
GSK-345931A is an EP(1) receptor antagonist. It is efficient in preclinical models of inflammatory pain. Uses: Inflammatory pain. Synonyms: GSK-345931A sodium; GSK 345931A sodium; GSK345931A sodium; 869534-13-4(Free); 6-(5'-chloro-2'-(2-methylpropoxy)(1,1'-biphenyl)-2-yl)- 2-Pyridinecarboxylic acid sodium salt. Grades: 98%. CAS No. 869499-38-7. Molecular formula: C22H19ClNNaO3. Mole weight: 403.83.
GSK369796 Dihydrochloride
SK369796, also known as N-tert-butylisoquine, shows antimalerial activity with IC50 values of 11.2 nM for 3D7 strain, 12.6 nM for HB3 strain, 17.6 nM for K1 strain. GSK369796 was rationally designed based on chemical, toxicological, pharmacokinetic, and pharmacodynamic considerations and was selected based on excellent activity against Plasmodium falciparum in vitro and rodent malaria parasites in vivo. Synonyms: 2-[(tert-Butylamino)methyl]-5-[(7-chloroquinolin-4-yl)amino]phenol Dihydrochloride; GSK369796 Dihydrochloride; GSK 369796; GSK-369796; GSK369796; N-tert-Butyl isoquine. CAS No. 1010411-21-8. Molecular formula: C20H24Cl3N3O. Mole weight: 428.78.
GSK3β Inhibitor II
GSK3β Inhibitor II is a potent and selective inhibitor of glycogen synthase kinase-3β (GSK3β) with an IC50 value of 390 nM. Synonyms: ?Glycogen Synthase Kinase 3β?? Inhibitor II; Tip-oxadiazole; 4-[5-[[(3-iodophenyl)methyl]thio]-1,3,4-oxadiazol-2-yl]-pyridine; 2-Thio(3-iodobenzyl)-5-(1-pyridyl)-[1,3,4]-oxadiazole. Grades: ≥95%. CAS No. 478482-75-6. Molecular formula: C14H10IN3OS. Mole weight: 395.2.
GSK3β Inhibitor XI
GSK3β inhibitor XI is a cell-permeable, potent and ATP-competitive inhibitor of glycogen synthase kinase 3β (GSK3β; Ki = 25 nM) which is selective for GSK3β over a panel of 79 commonly studied protein kinases. Synonyms: 3-[1-(3-hydroxypropyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-4-(2-pyrazinyl)-1H-pyrrole-2,5-dione. Grades: ≥98%. CAS No. 626604-39-5. Molecular formula: C18H15N5O3. Mole weight: 349.3.
GSK3β Inhibitor XVIII
GSK3β inhibitor XVIII is a cell-permeable, potent and selective inhibitor of glycogen synthase kinase 3β (GSK3β; IC50 = 64 nM). Synonyms: [2-chloro-4-[[4-(2-thienyl)-2-pyrimidinyl]amino]phenyl](4-methyl-1-piperazinyl)-methanone. Grades: ≥98%. CAS No. 1139875-74-3. Molecular formula: C20H20ClN5OS. Mole weight: 413.9.
GSK-3 inhibitor 1
GSK-3 inhibitor 1 is a potent GSK-3 inhibitor. Grades: >98%. CAS No. 603272-51-1. Molecular formula: C22H17ClFN5O2. Mole weight: 437.85.
GSK3 Inhibitor XIII
GSK3 Inhibitor XIII is a potent and ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK3). Synonyms: Glycogen Synthase Kinase 3 Inhibitor XIII; 5,6,7,8-tetrahydro-N-(5-methyl-1H-pyrazol-3-yl)-2-phenyl-4-quinazolinamine. Grades: ≥98%. CAS No. 404828-08-6. Molecular formula: C18H19N5. Mole weight: 305.4.
GSK3 Inhibitor XV
GSK3 inhibitor XV is a racemic mixture of (R)-GSK3 inhibitor XV and (S)-GSK3 inhibitor XV. (R)-GSK3 inhibitor XV inhibits glycogen synthase kinase (GSK) 3α and β with IC50 values of 0.35 and 0.55 nM respectively. (S)-GSK3 inhibitor XV is less potent than the (R)-GSK3 inhibitor XV. Synonyms: [11-bromo-9-hydroxypyrido[2, 3-a]pyrrolo[3, 4-c]carbazole-5, 7(1H, 6H)-dionato-κN1, κN12]carbonyl[(1, 2, 3, 4, 5-η)-1-(methoxycarbonyl)-2, 4-cyclopentadien-1-yl]-ruthenium. Grades: ≥98%. CAS No. 936112-69-5. Molecular formula: C25H14BrN3O6Ru. Mole weight: 633.40.
GSK 461364 analogue I
GSK 461364 analogue I is a potent polo-like kinase (PLK) inhibitor with selectivity for PLK1 (IC50: 2 nM) over PLK3 (IC50: 630 nM). Synonyms: GSK 461364 analogue I; GSK461364 analogue I; GSK-461364 analogue I; GSK579289A; GSK 579289A; GSK-579289A. Compound 25 [PMID 19237286]; 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-(1-methylpiperidin-4-yl)oxybenzimidazol-1-yl]thiophene-2-carboxamide. Grades: 99%. CAS No. 929095-23-8. Molecular formula: C26H27ClN4O3S. Mole weight: 511.04.
GSK 461364 analogue II
GSK 461364 analogue II is a potent polo-like kinase (PLK) inhibitor with selectivity for PLK1 (IC50: 2 nM) over PLK3 (IC50: 270 nM). Synonyms: GSK 461364 analogue II; GSK461364 analogue II; GSK-461364 analogue II; 5-[6- (1-methylpiperidin-4-yl) oxybenzimidazol-1-yl]-3-[ (1R) -1-[2- (trifluoromethyl) phenyl]ethoxy]thiophene-2-carboxamide. Grades: 99%. CAS No. 929095-22-7. Molecular formula: C27H27F3N4O3S. Mole weight: 544.59.
GSK 4716
GSK 4716 is a selective agonist of estrogen-related receptors ERRβ and ERRγ displaying selectivity over ERRα and the classical estrogen receptors. Activation of GSK 4716 regulates mitochondrial activity in skeletal muscle during exercise. Synonyms: GSK4716; GSK 4716; GSK-4716; 4-Hydroxy-2-[ (1E) -[4- (1-methylethyl) phenyl]methylene]hydrazide. Grades: ≥99% by HPLC. CAS No. 101574-65-6. Molecular formula: C17H18N2O2. Mole weight: 282.34.
GSK-503
GSK-503 is a potent EZH2 inhibitor with potential anticancer activity. Increased activity of the epigenetic modifier EZH2 has been associated with different cancers. Synonyms: GSK503; GSK 503; GSK503. Grades: 98%. CAS No. 1346572-63-1. Molecular formula: C31H38N6O2. Mole weight: 526.67.
GSK 525768A
GSK 525768A is a enantiomer analogue of GSK 525762A which is a BET family inhibitor aiming at the bromodomain and has potential effect against cancers and sorts of other diseases related to BET bromodomains. Uses: Gsk 525768a is a enantiomer analogue of gsk 525762a which is a bet family inhibitor aiming at the bromodomain and has potential effect against cancers and sorts of other diseases related to bet bromodomains. Synonyms: GSK 525768A; GSK525768A; GSK-525762A; CHEMBL2153435; SCHEMBL12966358; DTXSID50680634. Grades: 98%. CAS No. 1260530-25-3. Molecular formula: C22H22ClN5O2. Mole weight: 423.90.
GSK554418A
GSK-554418A is a azaindole Cannabinoid receptor type 2 (CB2) agonist. It can be used for the treatment of chronic pain. Uses: Chronic pain. Synonyms: GSK-554418A; GSK 554418A; GSK554418A. (4-((3-chlorophenyl)amino)-1-methyl-1H-pyrrolo(3,2-C)pyridin-7-yl)-4-morpholinyl- Methanone. Grades: 98%. CAS No. 871819-90-8. Molecular formula: C19H19ClN4O2. Mole weight: 370.84.
GSK-598809
GSK598809 is a selective Dopamine D3 receptor antagonist originated by GlaxoSmithKline. It may decrease the rewarding effects of contextual cues associated with drug intake preclinically and that may reduce drug craving in humans. No recent development for the treatment of Drug abuse. Eating disorders and Smoking withdrawal was reported. Uses: Drug abuse; eating disorders; smoking withdrawal. Synonyms: GSK-598809; GSK 598809; GSK598809; NII-Y5OZ63HC3V;5-(5-((3-((1S,5R)-1-(2-Fluoro-4-(trifluoromethyl)phenyl)-5-methyl-3-azabicyclo(3.1.0)hexan-3-yl)propyl)thio)-4-methyl-4H-1,2,4-triazol-3-yl)-4-methyloxazole. Grades: 98%. CAS No. 1310803-30-5. Molecular formula: C23H25F4N5OS. Mole weight: 495.54.
GSK-626616
GSK-626616 is a YAK3/DYRK3 kinase inhibitor. It is a chemoprotective agent for the potential treatment of chemotherapy-induced anaemia. Uses: Gsk-626616 is a chemoprotective agent for the potential treatment of chemotherapy-induced anaemia. Synonyms: GSK-626616; GSK 626616; GSK626616; (5Z)-2-(2,6-Dichloroanilino)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolone;GSK626616;(5Z)-2-(2,6-dichloroanilino)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazol-4-one. Grades: >98 %. CAS No. 1025821-33-3. Molecular formula: C18H10Cl2N4OS. Mole weight: 401.26.
GSK650394
GSK650394 is a competitive inhibitor that quantitatively blocks the effect of androgens on LNCaP cell growth. Synonyms: GSK650394; GSK-650394; GSK 650394. Grades: 0.98. CAS No. 890842-28-1. Molecular formula: C25H22N2O2. Mole weight: 382.45.
GSK6853
GSK6853 is a potent (pKd 9.5), soluble, cell active (20 nM), and highly selective inhibitor of the BRPF1 bromodomain with greater than 1600-fold selectivity over all other bromodomains tested. Synonyms: N-[1,3-dimethyl-6-[(2R)-2-methylpiperazin-1-yl]-2-oxobenzimidazol-5-yl]-2-methoxybenzamide; GSK6853; GSK-6853; GSK-6853. Grades: >98%. CAS No. 1910124-24-1. Molecular formula: C22H27N5O3. Mole weight: 409.49.
GSK-690693
GSK690693 is a pan-AKT kinase inhibitor, is also an aminofurazan-derived inhibitor of Akt kinases with potential antineoplastic activity. Pan-AKT kinase inhibitor GSK-690693 binds to and inhibits Akt kinases 1, 2, and 3, which may result in the inhibition of protein phosphorylation events downstream from Akt kinases in the PI3K/Akt signaling pathway, and, subsequently, the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. In addition, this agent may inhibit other protein kinases including protein kinase C (PKC) and protein kinase A (PKA). As serine/threonine protein kinases which are involved in a number of biological processes, AKT kinases promote cell survival by inhibiting apoptosis and are required for glucose transport. Synonyms: GSK-690693; GSK690693. CAS No. 937174-76-0. Molecular formula: C21H27N7O3. Mole weight: 425.48418.
GSK7227
GSK7227 is a novel class of PPARdelta partial agonists. It shows potent partial agonism of the PPARdelta target genes CPT1a and PDK4 in skeletal muscle cells. Synonyms: GSK-7227; GSK7227; GSK 7227; 2-[[3-(5-Methoxy-4-methylindol-1-yl)sulfonylbenzoyl]amino]-5-methylbenzoic acid;GSK-7227;Benzoic acid, 2-((3-((5-methoxy-4-methyl-1H-indol-1-yl)sulfonyl)benzoyl)amino)-5-methyl-. Grades: >98%. CAS No. 1067214-81-6. Molecular formula: C25H22N2O6S. Mole weight: 478.52.
GSK 789472 hydrochloride
GSK 789472 hydrochloride is a selective dopamine D3 receptor antagonist and D2 partial agonist (pEC50 values are <5.5 and 8.3, respectively). GSK 789472 exhibits selectivity against the D4 receptor in both agonist and antagonist assays. Synonyms: GSK 789472 hydrochloride; GSK-789472 hydrochloride; GSK789472 hydrochloride; 4,5-Dihydro-1-phenyl-3-(2-piperidinyl)methylimidazol-2(1H)-one hydrochloride; 1-phenyl-3-(piperidin-2-ylmethyl)imidazolidin-2-one hydrochloride. Grades: ≥99% by HPLC. CAS No. 1257326-24-1. Molecular formula: C15H21N3O.HCl. Mole weight: 295.81.
GSK837149
GSK837149 is a selective inhibitor of human fatty acid synthase (FAS; Ki value 30 nM) that acts via suppressing the β-ketoacyl reductase activity of the enzyme. Synonyms: GSK837149A; GSK-837149-A; GSK 837149 A; 1,3-bis[4-[(4-methylpyrimidin-2-yl)sulfamoyl]phenyl]urea. Grades: 99%. CAS No. 13616-29-0. Molecular formula: C23H22N8O5S2. Mole weight: 554.6.
GSK864
GSK864 is a cell penetrant, selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) mutant with IC50 values of 8.8, 15.2 and 16.6 nM for IDH1 mutants R132C, R132H, and R132G, respectively. Synonyms: (7S)-1-[(4-fluorophenyl)methyl]-3-N-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,6-dihydropyrazolo[4,3-c]pyridine-3,7-dicarboxamide; GSK 864; GSK-864. CAS No. 1816331-66-4. Molecular formula: C30H31FN6O4. Mole weight: 558.6.
GSK 9027
GSK 9027 is a glucocorticoid receptor agonist (pIC50 = 8) inhibiting production of the proinflammatory mediator IL-6 in vivo. GSK 9027 is used for the treatment of acute and chronic inflammatory conditions. Synonyms: GSK 9027; GSK9027; GSK-9027; N-[4-[1- (4-Fluorophenyl) -1H-indazol-5-yl-3- (trifluoromethyl) phenyl]benzenesulfonamide. Grades: ≥98% by HPLC. CAS No. 1229096-88-1. Molecular formula: C27H19F4N3O2S. Mole weight: 525.52.
GSK 962040
GSK 962040 is a selective motilin receptor agonist with pEC50 value of 7.9. It is effective as a stimulant of human and rabbit gastrointestinal motility. lt represents a new opportunity as a treatment in diabetic gastroparesis. It is discovered as a therapeutic agent for conditions associated with delayed gastric emptying. It is highly selective against motilin receptor over the human ghrelin receptor and hERG. It also has no significant activity against other receptors including 5-HT, adrenergic, dopamine, histamine and adenosine receptors. It is found to enhance the EFS-induced cholinergic contraction and cause a small muscle contraction at high concentration in rabbit isolated gastric antrum. It also induces the contraction of human-isolated stomach preparations at 10μM. It had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes in vitro. It was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM. It induced phasic contractions, the duration of which was dose-related. It strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only. It was developed by glaxosmithkline and has been in Cilinic Phase 2. Uses: Gsk 962040 may be used as a treatment in diabetic gastroparesis. Synonyms: GSK-962040; GSK 962040; GSK962040; Camicinal;1-[4-(3-fluoroanilino)piperidin-1-yl]-2-[4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]ethanone. Grades: >98%. CAS No. 923565-21-3. Molecular formula: C25H33FN4O. Mole weight: 424.55.
GSK 962040 hydrochloride
GSK 962040 hydrochloride is the hydrochloride form of GSK 962040, which is a selective motilin receptor agonist with pEC50 value of 7.9. It may be used as a treatment in diabetic gastroparesis. It was developed by glaxosmithkline and has been in Cilinic Phase 2. Uses: Gsk 962040 hydrochloride was developed by glaxosmithkline and has been in cilinic phase 2. Synonyms: Camicinal hydrochloride;GSK-962040 hydrochloride; GSK 962040 hydrochloride; GSK962040 hydrochloride; 2-[4-(3-Fluoroanilino)piperidin-1-yl]-1-[4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]ethanone hydrochloride. Grades: >98%. CAS No. 923565-22-4. Molecular formula: C25H34ClFN4O. Mole weight: 461.02.
GSK J1
GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases. Synonyms: GSKJ1; GSKJ 1; GSKJ-1. Grades: 98%. CAS No. 1373422-53-7. Molecular formula: C22H23N5O2. Mole weight: 389.45.
GSK-J1 sodium salt
GSK-J1 is a potent and selective inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50s = 18 and 56 μM, respectively; IC50 = 60 nM in JMJD3 antibody-based assays). Synonyms: N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine, monosodium salt. Grades: ≥95%. CAS No. 1797832-71-3. Molecular formula: C22H22N5O2·Na. Mole weight: 411.4.
GSK-J2
GSK-J2, a benzazepin derivative, has been found to have poor activity as a JMJD3 inhibitor so that could be used in the biological study of GSK-J1 as a negative control. IC50: > 100 μM. Uses: Gsk-j2 has been found to have poor activity as a jmjd3 inhibitor so that could be used in the biological study of gsk-j1 as a negative control. Synonyms: SK-J2; GSK J2; GSKJ2; 1394854-52-4; SCHEMBL15937902; 3705AH. Grades: 98%. CAS No. 1394854-52-4. Molecular formula: C22H23N5O2. Mole weight: 389.45.
GSK-J2 sodium salt
GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 with an IC50 value greater than 100 μM. Synonyms: 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-3-yl)pyrimidin-4-yl)amino)propanoic acid, monosodium salt. Grades: ≥90%. CAS No. 2108665-15-0. Molecular formula: C22H23N5O2·Na. Mole weight: 412.4.
GSK J4 HCl
GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family. Synonyms: GSK-J4; 1373423-53-0; GSK J4; Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoateethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate. Grades: >98%. CAS No. 1373423-53-0. Molecular formula: C24H27N5O2.HCl. Mole weight: 453.96.
GSK-J4 hydrochloride
GSK-J4 (hydrochloride) is an ethyl ester derivative of GSK-J1 which blocks demethylation of histone H3K27 with an IC50 value greater than 50 μM in vitro. Synonyms: N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine, ethyl ester, monohydrochloride. Grades: ≥95%. CAS No. 1797983-09-5. Molecular formula: C24H27N5O2·HCl. Mole weight: 454.
GSK-J5 hydrochloride
GSK-J5 is a pyridine regio-isomer of GSK-J4 and it is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition. Synonyms: N-[2-(3-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine, ethyl ester, monohydrochoride. Grades: ≥95%. CAS No. 1797983-32-4. Molecular formula: C24H27N5O2·HCl. Mole weight: 454.
GT 2016
GT 2016 is a high affinity and brain-penetrant histamine H3 receptor antagonist (Ki = 43.8 nM). It displays selectivity against H1 and H2 receptors (IC50 >10 μM). GT 2016 increases the release of histamine in the cerebral cortex. GT 2016 exhibits no effect on histamine methyltransferase in vitro at concentrations up to 3 μM. Synonyms: GT-2016,GT2016, GT 2016; 5-Cyclohexyl-1-[4-(1H-imidazol-5-yl)-1-piperidinyl]-1-pentanone. Grades: ≥98% by HPLC. CAS No. 152241-24-2. Molecular formula: C19H31N3O. Mole weight: 317.47.
G-TPP
G-TPP is a mitochondria-targeted Hsp90 inhibitor that increases cell death in HeLa and MCF7 cells, consistently inhibits cell death induced by oxidative stress and mitochondrial dysfunction induced by PINK1 mutation in mouse embryonic fibroblast cells and DA cell models such as SH-SY5Y and SN4741 cells. Additionally, G-TPP also suppresses the defective locomotive activity and DA neuron loss in Drosophila PINK1 null mutants. Synonyms: G-TPP; G TPP. Grades: >98%. CAS No. 1131626-46-4. Molecular formula: C52H65N3O8P. Mole weight: 890.85.
GTS-21
GTS-21 is a highly efficacious pharmaceutical compound used in studying the intricate afflictions of Alzheimer's disease and cognitive impairments. Uses: Nicotinic agonists. Synonyms: 3-[(2,4-Dimethoxyphenyl)methylene]-3,4,5,6-tetrahydro-2,3'-bipyridine; GTS-21; GTS21; GTS 21; DMXB-A. CAS No. 148372-04-7. Molecular formula: C19H20N2O2. Mole weight: 308.381.
Guanabenz Acetate
Guanabenz Acetate is an selective agonist of α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor with pEC50 of 8.25, 7.01 and ~5, respectively. It is used as an antihypertensive drug. Synonyms: WY-8678 Acetate; Wytensin, WY-8678, WY 8678, WY8678, EIPA. Grades: >98%. CAS No. 23256-50-0. Molecular formula: C8H8Cl2N4.C2H4O2. Mole weight: 291.13.
Guanabenz hydrochloride
Guanabenz is an agonist of α2-adrenergic receptor with hypotensive effects. Synonyms: Wytensin; 2-[(2,6-dichlorophenyl)methylene]-hydrazinecarboximidamide, monohydrochloride. Grades: ≥98%. CAS No. 23113-43-1. Molecular formula: C8H8Cl2N4·HCl. Mole weight: 267.5.
Guanadrel Hemisulfate
Guanadrel, as an antihypertensive agent, is an orally active postganglionic sympathetic inhibitor. Synonyms: N-(1,4-Dioxaspiro[4.5]dec-2-ylmethyl)guanidine Sulfate; (1,4-Dioxaspiro[4.5]dec-2-ylmethyl)guanidine Sulfate; Anarel; CL 1388R; Guanadrel Sulfate; Hylorel; U 28288D. Grades: 95%. CAS No. 22195-34-2. Molecular formula: C10H19N3O2.1/2H2O4S. Mole weight: 524.636.
Guanfacine
Guanfacine, a selective agonist of α2A receptor, is a sympatholytic drug to treat attention deficit hyperactivity disorder (ADHD) and hypertension. It lowers both systolic and diastolic blood pressure due to activating the central nervous system α2A norep. Uses: Adrenergic alpha-2 receptor agonists. Synonyms: N-(diaminomethylidene)-2-(2,6-dichlorophenyl)acetamide BS 100 141 BS-100-141 BS100141 Estulic Guanfacine Guanfacine Hydrochloride Guanfacine Monohydrochloride Hydrochloride, Guanfacine Lon798 Monohydrochloride, Guanfacine Tenex. Grades: > 95%. CAS No. 29110-47-2. Molecular formula: C9H9Cl2N3O. Mole weight: 246.10.
Guanidinoethyl sulfonate
Guanidinoethyl sulfonate is a natural guanidine-taurine analog derived from taurine. It acts as a competitive glycine receptor antagonist. Synonyms: NSC 667063; Taurocyamine; 2-[(aminoiminomethyl)amino]-ethanesulfonic acid. Grades: ≥95%. CAS No. 543-18-0. Molecular formula: C3H9N3O3S. Mole weight: 167.2.
Guanoxabenz
Guanoxabenz, a metabolite of guanaben, is an α2 adrenergic receptor agonist. Synonyms: 2-[(E)-(2,6-dichlorophenyl)methylideneamino]-1-hydroxyguanidine; 1-(2,6-dichlorobenzylideneamino)-3-hydroxyguanidine; guanoxabenz; guanoxabenz hydrochloride; guanoxabenz monohydrochloride. CAS No. 24047-25-4. Molecular formula: C8H8Cl2N4O. Mole weight: 247.08.
Guvacine hydrochloride
Guvacine hydrochloride is a specific GABA uptake inhibitor (IC50 = 14, 58, 119 and 1870 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1, respectively). Guvacine may be beneficial for the treatment of neuropsychiatric disorders. Synonyms: 1,2,5,6-Tetrahydropyridine-3-carboxylic acid hydrochloride. Grades: ≥99% by HPLC. CAS No. 6027-91-4. Molecular formula: C6H9NO2.HCl. Mole weight: 163.6.
GV-196771
GV-196771, an indole derivative, has been found to be a non-opioid analgesic agent which is also a NMDA antagonist binds to glycine-binding site and was once studied in pain therapy. Synonyms: GV-196771; GW-196771; GV 196771; GW 196771; GV196771; GW196771; AC1OC7O7; SCHEMBL499308; 4,6-dichloro-3-[(E)-(2-oxo-1-phenylpyrrolidin-3-ylidene)methyl]-1H-indole-2-carboxylic acid; GV196771A; GV 196771A; GV-196771A. Grades: 98%. CAS No. 166974-22-7. Molecular formula: C20H14Cl2N2O3. Mole weight: 401.24.
GV-58
GV-58, a pupin derivative, has been found to be a P/Q-type Ca²?-channel agonist that could be used to against neuromuscular weakness. IC50: 7.21/8.81 uM (N-type/P-Q-type Ca2+ channel). Uses: Gv-58 has been found to be a p/q-type ca²?-channel agonist that could be used to against neuromuscular weakness. Synonyms: GV-58; CS-3617; GV 58; CS 3617; GV58; CS3617; CHEMBL2206242; SCHEMBL17628602; BDBM50400564. Grades: 98%. CAS No. 1402821-41-3. Molecular formula: C18H26N6OS. Mole weight: 374.50.
GW-1100
A cell-permeable pyrimidinylmethyl-pyrimidinone compound that acts as potent, reversible and non-competitive GPR40 antagonist. Shown to significantly reverse glucose-induced insulin secretion potentiated by GW9508 and only partially reduce linoleic acid effect in MIN6 cells. Synonyms: GW 1100; GW-1100; GW1100. Grades: >98%. CAS No. 306974-70-9. Molecular formula: C27H25FN4O4S. Mole weight: 520.58.
GW2580
GW2580 is an orally bioavailable inhibitor of cFMS kinase. GW2580 was found to completely inhibit human cFMS kinase in vitro at 0.06 microM and was inactive against 26 other kinases. GW2580 at 1 microM completely inhibited CSF-1-induced growth of mouse M-NFS-60 myeloid cells and human monocytes and completely inhibited bone degradation in cultures of human osteoclasts, rat calvaria, and rat fetal long bone. In contrast, GW2580 did not affect the growth of mouse NS0 lymphoblastoid cells, human endothelial cells, human fibroblasts, or five human tumor cell lines. GW2580 also did not affect lipopolysaccharide (LPS)-induced TNF, IL-6, and prostaglandin E2 production in freshly isolated human monocytes and mouse macrophages. After oral administration, GW2580 blocked the ability of exogenous CSF-1 to increase LPS-induced IL-6 production in mice, inhibited the growth of CSF-1-dependent M-NFS-60 tumor cells in the peritoneal cavity, and diminished the accumulation of macrophages in the peritoneal cavity after thioglycolate injection. Unexpectedly, GW2580 inhibited LPS-induced TNF production in mice, in contrast to effects on monocytes and macrophages in vitro. In conclusion, GW2580's selective inhibition of monocyte growth and bone degradation is consistent with cFMS kinase inhibition. The ability of GW2580 to chronically inhibit CSF-1 signaling through cFMS kinase in normal and tumor cells in vivo makes GW2580 a useful tool in assessing the role of cFMS kinase in normal and disease processes. Synonyms: GW 2580; GW-2580; GW2580. Grades: 0.98. CAS No. 870483-87-7. Molecular formula: C20H22N4O3. Mole weight: 366.421.
GW 274150
GW 274150 is a potent, long-acting and highly selective inhibitor of iNOS which have a very high degree of selectivity for iNOS versus both eNOS (>100-fold) and nNOS (>80-fold). GW 274150 shows analgesic effects in rat models of inflammatory and neuropath. Synonyms: (2S) -2-amino-4-[2- (1-aminoethylideneamino) ethylsulfanyl]butanoic acidGW-274150; GW 274150; GW274150. CAS No. 210354-22-6. Molecular formula: C8H17N3O2S. Mole weight: 219.30.
GW284543
GW284543 (UNC10225170) is a selective MEK5 inhibitor. It can reduce pERK5 and reduce endogenous MYC protein. Synonyms: CHEMBL531447; BCP31359; MFCD32067894; HY-114189. Grades: 98%. CAS No. 790186-68-4. Molecular formula: C23H20N2O3. Mole weight: 372.4.
GW311616
Potent, selective and orally active human neutrophil elastase (HNE) inhibitor (IC50 value 22 nM). GW311616A is selective over other human serine proteases (IC50 values >100 μM for trypsin, cathepsin G, and plasmin, >3 μM for chymotrypsin and tissue plasminogen activator), and does not inhibit AchE at 100 μM. Synonyms: GW-311616; GW 311616. Grades: >98%. CAS No. 198062-54-3. Molecular formula: C19H31N3O4S. Mole weight: 397.53.
GW311616 hydrochloride
Potent, selective and orally active human neutrophil elastase (HNE) inhibitor (IC50 value 22 nM). GW311616A is selective over other human serine proteases (IC50 values >100 μM for trypsin, cathepsin G, and plasmin, >3 μM for chymotrypsin and tissue plasminogen activator), and does not inhibit AchE at 100 μM. Synonyms: GW-311616 hydrochloride; GW 311616 hydrochloride; GW311616A. Grades: >98%. CAS No. 197890-44-1. Molecular formula: C19H32ClN3O4S. Mole weight: 433.99.
GW3965
GW3965 is a potent, selective LXR agonist for hLXRα and hLXR&beta. When screened against a panel of nuclear receptors, it cross-reacted with only the pregnane X receptor (PXR). In Vitro: Recruit the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay; Potent antagonistic activity against hLXRα and hLXRβ in cell-based assays with EC50 of 190 nM and 30 nM, respectively; In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor In Vivo: At a dose of 10 mg/kg upregulates ABCA1 expression 8-fold and raises circulating levels of HDL by 30% with Cmax of 12.7 μg/mL and t1/2 of 2 hours. Uses: A liver x receptor agonist; represses the production of pro-inflammatory cytokines by murine mast cells; in vitro: reduces tissue factor production and inflammatory responses in human islets. Synonyms: GW3965; GW 3965; GW-3965; 2- (3- (3- ( (2-chloro-3- (trifluoromethyl) benzyl) (2, 2-diphenylethyl) amino) propoxy) phenyl) acetic acid hydrochloride. Grades: ≥ 98.0%. CAS No. 405911-09-3. Molecular formula: C33H31ClF3NO3. Mole weight: 582.05.
GW4064
GW4064 is a selective non-steroidal agonist of farnesoid X receptor (FXR) with EC50 value of 15 nM. Synonyms: GW4064; GW-4064; GW 4064. Grades: >98%. CAS No. 278779-30-9. Molecular formula: C28H22Cl3NO4. Mole weight: 542.84.
GW5074
GW5074 is a c-Raf inhibitor. GW5074 has no direct effect on the activities of several apoptosis-associated kinases when assayed in vitro. In contrast to its effect in vitro, treatment of neurons with GW5074 causes c-Raf activation (when measured in vitro in the absence of the drug) and stimulates the Raf-MEK-ERK pathway. GW5074 prevents neurodegeneration and improves behavioral outcome in an animal model of Huntington's disease. GW5074 could have therapeutic value against neurodegenerative pathologies in humans. Synonyms: GW5074; GW 5074; GW-5074. CAS No. 220904-83-6. Molecular formula: C15H8Br2INO2. Mole weight: 520.94.
GW 542573X
GW 542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2) with selectivity for KCa2.1 (EC50 = 8.2 μM in HEK293 cells expressing hKCa2.1). Synonyms: GW542573X; GW 542573X; GW-542573X. 4-[[[[ (2-Methoxyphenyl) amino]carbonyl]oxy]methyl]-piperidinecarboxylic acid-1,1-dimethylethyl ester; tert-butyl 4-[ (2-methoxyphenyl) carbamoyloxymethyl]piperidine-1-carboxylate. Grades: ≥99% by HPLC. CAS No. 660846-41-3. Molecular formula: C19H28N2O5. Mole weight: 364.44.
GW 583340 dihydrochloride
GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50 = 0.01 and 0.014 μM, respectively). GW 583340 selectively inhibits growth of human tumor cells overexpressing EGFR and ErbB2 (IC50 = 0.11 μM for inhibition of HN5, N87 and BT474 tumor cell lines vs. > 30 μM for inhibition of non-tumor cell line HFF). it is used in the treatment of breast cancer. Synonyms: GW 583340 dihydrochloride; GW-583340 dihydrochloride; GW583340 dihydrochloride; N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[2-[[[2-(methylsulfonyl)ethyl]amino]methyl]-4-thiazolyl]-4-quinazolinamine dihydrochloride. Grades: ≥97% by HPLC. CAS No. 1173023-85-2. Molecular formula: C28H25ClFN5O3S2.2HCl. Mole weight: 671.03.
GW-590735
GW-590735 is a potent and selective agonist of PPAR&alpha. Its EC50 value is 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity than PPARγ and PPAR&delta. It significantly increased HDL cholesterol and decreased LDL and VLDL cholesterol. It also significantly reduced triglycerides. Uses: Gw-590735 significantly increased hdl cholesterol and decreased ldl and vldl cholesterol. it also significantly reduced triglycerides. Synonyms: GW590735; GW-590735; GW 590735. 2-Methyl-2-(4-((4-Methyl-2-(4-(trifluoromethyl)phenyl)thiazole-5-carboxamido)methyl)phenoxy)propanoic acid; 2-Methyl-2- [4- [ [ [4-methyl-2- [4- (trifluoromethyl) phenyl] -1, 3-thiazole-5-carbonyl] amino] methyl] phenoxy] propanoic acid. Grades: 98%. CAS No. 622402-22-6. Molecular formula: C23H21F3N2O4S. Mole weight: 478.49.
GW6471
GW6471 is a PPARα antagonist (IC50 = 0.24 μM). GW6471 enhances the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR. Synonyms: GW-6471; GW 6471; Propanamide, N-[(2S)-2-[[(1Z)-1-methyl-3-oxo-3-[4-(trifluoromethyl)phenyl]-1-propen-1-yl]amino]-3-[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]propyl]-; N-[ (2S) -2-[[ (1Z) -1-Methyl-3-oxo-3-[4- (trifluoromethyl) phenyl]-1-propen-1-yl]amino]-3-[4-[2- (5-methyl-2-phenyl-4-oxazolyl) ethoxy]phenyl]propyl]propanamide; Propanamide, N-[(2S)-2-[[(1Z)-1-methyl-3-oxo-3-[4-(trifluoromethyl)phenyl]-1-propenyl]amino]-3-[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]propyl]-; (S,Z)-N-(3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-((4-oxo-4-(4-(trifluoromethyl)phenyl)but-2-en-2-yl)amino)propyl)propionamide. Grades: ≥95%. CAS No. 880635-03-0. Molecular formula: C35H36F3N3O4. Mole weight: 619.67.
GW 7647
GW 7647 is a potent and highly selective PPARα agonist (EC50 = 6, 1100 and 6200 nM for human PPARα, PPARγ and PPARδ receptors, respectively) with 200-fold selectivity over PPARγ and PPAR&delta. GW 7647 modulates oleate metabolism and mitochondrial enzyme gene expression in mature myotubules in vitro via activating PPAR&alpha. GW 7647 exhibits lipid-lowering and anti-inflammatory effects. Synonyms: GW-7647; GW 7647; GW7647. 2-[[4-[2-[[ (Cyclohexylamino) carbonyl] (4-cyclohexylbutyl) amino]ethyl]phenyl]thio]-2-methylpropanoic acid. Grades: ≥99% by HPLC. CAS No. 265129-71-3. Molecular formula: C29H46N2O3S. Mole weight: 502.75.
GW 791343 dihydrochloride
The hydrochlorie salt form of GW791343 that is a non-competitive inhibitor of human P2X7 receptors amd it seems to show species-specific activity which is probably negative allosteric modulators of the human P2X7 receptor and the agonist of the same recep. Uses: The hydrochlorie salt form of gw791343 that is a non-competitive inhibitor of human p2x7 receptors. Synonyms: GW791343 (dihydrochloride); 1019779-04-4; 2-((3,4-Difluorophenyl)amino)-N-(2-methyl-5-(piperazin-1-ylmethyl)phenyl)acetamide dihydrochloride; GW 791343; GW-791343; 3075AH. Grades: >99 %. CAS No. 1019779-04-4. Molecular formula: C20H26Cl2F2N4O. Mole weight: 447.3.
GW 791343 trihydrochloride
GW791343 HCl is aHCl salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7. Synonyms: GW791343; GW 791343; GW-791343; 1019779-04-4. Grades: >98%. CAS No. 309712-55-8. Molecular formula: C20H24F2N4O.3HCl. Mole weight: 483.81.
GW843682X
GW843682X is a cell-permeable thiophene-benzimidazole compound that acts a selective PLK1 and PLK3 inhibitor with IC50s of 2.2 nM(PLK1) and 9.1 nM(PLK3). Uses: A polo-like kinase-1 (plk1) and polo-like kinase-3 (plk3) inhibitor. Synonyms: GW843682X; GW 843682X; GW-843682X. 5- (5, 6-dimethoxybenzimidazol-1-yl) -3-[[2- (trifluoromethyl) phenyl]methoxy]thiophene-2-carboxamide; Polo-like Kinase Inhibitor III. Grades: ≥98%. CAS No. 660868-91-7. Molecular formula: C22H18F3N3O4S. Mole weight: 477.46.
GW 848687X
GW 848687X is a potent and selective antagonist of EP1 receptor (IC50 = 2.5 nM). GW 848687X displays >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. Synonyms: 6-[2-[5-chloro-2-[(2,4-digluorophenyl)methoxy]phenyl]-1-cyclopenten-1-yl]-2-pyridinecarboxylic acid. Grades: ≥98%. CAS No. 612831-24-0. Molecular formula: C24H18ClF2NO3. Mole weight: 441.9.
GW 9578
GW 9578 is a potent agonist of PPARα, which is highly selective for PPARα compared to PPARγ and PPAR&delta. Synonyms: 2- [ [4- [2- [ [ [ (2, 4-difluorophenyl) amino] carbonyl] heptylamino] ethyl] phenyl] thio] -2-methyl-propanoic acid. Grades: ≥98%. CAS No. 247923-29-1. Molecular formula: C26H34F2N2O3S. Mole weight: 492.6.
GW-9820
GW-9820 is a PPAR-gamma agonist with potential antidiabetic effect. Synonyms: 2-[4-[2-[(4-fluorophenyl)carbamoyl-heptylamino]ethyl]phenoxy]-2-methylpropanoic acid; GW-9820; GW 9820; GW9820. Grades: >98%. CAS No. 195131-60-3. Molecular formula: C26H35FN2O4. Mole weight: 458.57.
GYKI-16084
GYKI-16084 is a postsynaptic alpha2-blocker with the potential to treat benign prostatic hyperplasia. Synonyms: 2-[3-[[(3R)-2,3-dihydro-1,4-benzodioxin-3-yl]methylamino]propyl]pyridazin-3-one; GYKI16084; GYKI 16084; GYKI-16084R-2-(3-N-(2-benzo(1,4)dioxanylmethyl)-amino-1-propyl)-3(2H)-pyridazinone hydrochloride. Grades: >98%. CAS No. 185739-21-3. Molecular formula: C16H19N3O3. Mole weight: 301.346.
GYKI-16638
GYKI-16638 is Potassium channel and Sodium channel antagonist originated by Nonindustrial source. It is a novel antiarrhythmic agent. Uses: Arrhythmias. Synonyms: GYKI-16638; GYKI 16638; GYKI16638; N- (4- (2- ( (1- (2, 6-dimethoxyphenoxy) propan-2-yl) (methyl) amino) ethyl) phenyl) methanesulfonamide. Grades: 98%. CAS No. 778564-77-5. Molecular formula: C21H30N2O5S. Mole weight: 422.54.