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GSK3987
GSK3987 is a pan LXRα/β agonist. Synonyms: GSK-3987; GSK 3987; 1-Benzyl-3-[(4-methoxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione. Grade: >98%. CAS No. 264206-85-1. Molecular formula: C24H20N2O3. Mole weight: 384.43.
GSK-3β inhibitor 1
GSK-3β inhibitor 1 is a glycogen synthase kinase 3β (GSK-3β) inhibitor (IC50 = 4.9 nM) with high antidiabetic efficacy. Synonyms: 3-[(Z)-(2-Pyridinyl)methylene]indoline-2-one; (3Z)-3-(2-pyridinylmethylene)-1,3-dihydro-2H-indol-2-one; (3Z)-3-(pyridin-2-ylmethylene)-1,3-dihydro-2H-indol-2-one; 2H-Indol-2-one, 1,3-dihydro-3-(2-pyridinylmethylene)-, (3Z)-. Grade: ≥95%. CAS No. 187325-53-7. Molecular formula: C14H10N2O. Mole weight: 222.24.
GSK-3β inhibitor 12
GSK-3β inhibitor 12 is an inhibitor of GSK-3β, an enzyme playing an essential function in T cell differentiation and proliferation. Synonyms: GSK-3beta inhibitor 12; 2-(1H-Indol-3-yl)-N-(5-methylthiazol-2-yl)acetamide. CAS No. 784170-07-6. Molecular formula: C14H13N3OS. Mole weight: 271.34.
GSK-3β inhibitor 2
GSK-3β inhibitor 2 is a potent, selective and orally active GSK-3β inhibitor (IC50 = 1.1 nM) that can cross the blood-brain barrier and has the potential to treat Alzheimer's disease. Synonyms: 2-(2-(Cyclopropanecarboxamido)pyridin-4-yl)-4-methoxythiazole-5-carboxamide; 2-{2-[(Cyclopropylcarbonyl)amino]-4-pyridinyl}-4-methoxy-1,3-thiazole-5-carboxamide; 5-Thiazolecarboxamide, 2-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-4-methoxy-. Grade: ≥98%. CAS No. 1702428-31-6. Molecular formula: C14H14N4O3S. Mole weight: 318.35.
GSK-3β inhibitor 3
GSK-3β inhibitor 3, a potent, selective, irreversible and covalent glycogen synthase kinase 3β (GSK-3β) inhibitor (IC50 = 6.6 μM), is used in the study of acute promyelocytic leukemia. Synonyms: 5-Acryloyl-2-(4-fluorophenyl)-2,3-dihydrobenzo[b][1,4]thiazepin-4(5H)-one; 5-Acryloyl-2-(4-fluorophenyl)-2,3-dihydro-1,5-benzothiazepin-4(5H)-one; 1,5-Benzothiazepin-4(5H)-one, 2-(4-fluorophenyl)-2,3-dihydro-5-(1-oxo-2-propen-1-yl)-; 5-Acryloyl-2,3-dihydro-2-(4-fluorophenyl)-1,5-benzothiazepin-4(5H)-one. Grade: ≥95%. CAS No. 1448990-73-5. Molecular formula: C18H14FNO2S. Mole weight: 327.37.
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. Grade: ≥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. Grade: ≥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. Grade: ≥98%. CAS No. 1139875-74-3. Molecular formula: C20H20ClN5OS. Mole weight: 413.9.
GSK-3/CDK5/CDK2-IN-1
GSK-3/CDK5/CDK2-IN-1, an inhibitor of CDK5, CDK2 and GSK-3, can be used in the study of cancer and neurodegenerative diseases. (Extracted from patent WO2002010141A1, example 9a). Synonyms: 2-Naphthaleneacetamide, N-[1-[cis-3-(acetylamino)cyclobutyl]-1H-imidazol-4-yl]-; N-(1-((1s,3s)-3-acetamidocyclobutyl)-1H-imidazol-4-yl)-2-(naphthalen-2-yl)acetamide; N-[1-(cis-3-Acetamidocyclobutyl)-1H-imidazol-4-yl]-2-(2-naphthyl)acetamide. Grade: ≥98%. CAS No. 395074-72-3. Molecular formula: C21H22N4O2. Mole weight: 362.42.
GSK-3 inhibitor 1
GSK-3 inhibitor 1 is a potent GSK-3 inhibitor. Grade: >98%. CAS No. 603272-51-1. Molecular formula: C22H17ClFN5O2. Mole weight: 437.85.
GSK-3 Inhibitor XIII
An inhibitor of GSK-3. Synonyms: (5-Methyl-1H-pyrazol-3-yl)-(2-phenylquinazolin-4-yl)amine. Grade: >98%. CAS No. 404828-14-4. Molecular formula: C18H15N5. Mole weight: 301.3.
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. Grade: ≥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. Grade: ≥98%. CAS No. 936112-69-5. Molecular formula: C25H14BrN3O6Ru. Mole weight: 633.40.
GSK4027
GSK4027 is a potent and selective inhibitor of p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain (Ki = 1.4 nM; IC50 = 60 nM in a chromatin engagement assay). Synonyms: 4-bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenyl-3-piperidinyl]amino]-3(2H)-pyridazinone. Grade: ≥95%. CAS No. 2079896-25-4. Molecular formula: C17H21BrN4O. Mole weight: 377.3.
GSK4112
GSK 4112, a kind of synthetic agonist of REV-ERBα, could suppress the expression of sorts of genes involved in gluconeogenesis. IC50: 0.4 μM (EC50). Uses: Gsk 4112 is a kind of synthetic agonist of rev-erbα and could suppress the expression of sorts of genes involved in gluconeogenesis. Synonyms: GSK4112; GSK 4112; GSK-4112. SR6452; CHEMBL1961795; 1216744-19-2; MLS006010708; GTPL2903. Grade: 95%. CAS No. 1216744-19-2. Molecular formula: C18H21ClN2O4S. Mole weight: 396.89.
GSK429286A
GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. Uses: Reprogramming, self-renewal. Synonyms: GSK 429286A; GSK-429286A. Grade: 0.98. CAS No. 864082-47-3. Molecular formula: C21H16F4N4O2. Mole weight: 432.37.
GSK-461364
GSK-461364 is a Polo-like kinase 1 inhibitor, is also a small molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor GSK461364 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner. Synonyms: GSK461364; GSK 461364; GSK-461364; GSK461364A; GSK 461364A; GSK-461364A. 5-[6-[(4-Methyl-1-piperazinyl)methyl]-1h-benzimidazol-1-yl]-3-[(1r)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide. CAS No. 929095-18-1. Molecular formula: C27H28F3N5O2S. Mole weight: 543.609.
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. Grade: 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. Grade: 99%. CAS No. 929095-22-7. Molecular formula: C27H27F3N4O3S. Mole weight: 544.59.
GSK466317A
GSK466317A is a G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor. Synonyms: GSK466317A; GSK-466317A; GSK 466317A. N-(7-chloro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide. Grade: 98%. CAS No. 864082-48-4. Molecular formula: C21H16ClF3N4O2. Mole weight: 448.83.
GSK467
GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. Synonyms: GSK-467; GSK 467. CAS No. 1628332-52-4. Molecular formula: C17H13N5O2. Mole weight: 319.32.
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. Grade: ≥99% by HPLC. CAS No. 101574-65-6. Molecular formula: C17H18N2O2. Mole weight: 282.34.
GSK481
GSK481 is a potent inhibitor of Receptor-interacting serine/threonine-protein kinase 1 (RIPK1 or RIP1; IC50 value 2.8 nM for inhibition of Ser166 autophosphorylation of hWT RIP1) with preference for RIP1 over 450 other kinases. Synonyms: GSK481; GSK-481; GSK 481. 5-benzyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-1,2-oxazole-3-carboxamide. Grade: 98%. CAS No. 1622849-58-4. Molecular formula: C21H19N3O4. Mole weight: 377.39.
GSK-484
GSK-484 is a potent protein-arginine deiminase type-4 (PAD-4) inhibitor. Synonyms: GSK484; GSK 484. Grade: ≥98% by HPLC. CAS No. 1652629-23-6. Molecular formula: C27H31N5O3. Mole weight: 473.6.
GSK-484 hydrochloride
GSK-484, a benzoimidazole derivative, has been found to be an effective reversible PAD-4 inhibitor that could be significant in some inflammation and immune response studies and probably have potential activities in anticancer studies. IC50: 50nM (without calcium), 250 nM (2 mM calcium exists). Synonyms: GSK484; GSK 484; GSK-484; ((3S,4R)-3-Amino-4-hydroxypiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-indol-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone hydrochloride. Grade: 98%. CAS No. 1652591-81-5. Molecular formula: C27H32ClN5O3. Mole weight: 510.04.
GSK494581A
GSK494581A, a specific ligand for human GPR55 (pEC50 of 6.8), acts as an inhibitor of glycine transporter subtype 1 (GlyT1). Synonyms: GSK 494581A; GSK-494581A. CAS No. 909416-67-7. Molecular formula: C27H28F2N2O4S. Mole weight: 514.58.
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. Grade: 98%. CAS No. 1346572-63-1. Molecular formula: C31H38N6O2. Mole weight: 526.67.
GSK5182
GSK5182 is a small-molecule ERRγ inverse agonist, which inhibited pro-inflammatory cytokine-induced catabolic factors in mouse articular chondrocytes. Synonyms: GSK-5182; GSK 5182. CAS No. 877387-37-6. Molecular formula: C27H31NO3. Mole weight: 417.54.
GSK525762
GSK525762A, also known as I-BET-762 and GSK525762, is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins with potential antineoplastic activity. Upon administration, the BET inhibitor GSK525762 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, BET proteins, comprising of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth. Synonyms: GSK525762; GSK525762; GSK525762; GSK525762A; GSK-525762A; GSK 525762A; I-BET-762; I-BET762; I-BET 762; molibresib. CAS No. 1260907-17-2. Molecular formula: C22H22ClN5O2. Mole weight: 423.9.
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. Grade: 98%. CAS No. 1260530-25-3. Molecular formula: C22H22ClN5O2. Mole weight: 423.90.
GSK547
GSK547 is a highly selective and potent RIP1 (RIPK1) inhibitor which displays 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK963. Synonyms: RIP1i. Grade: ≥98%. CAS No. 2226735-55-1. Molecular formula: C20H18F2N6O. Mole weight: 396.39.
GSK-5498A
GSK-5498A, a CRAC channel blocker, has been found to have effect in restraining pro-inflammatory cytokine. IC50: 1 uM. Uses: Gsk-5498a is a crac channel blocker that has been found to have effect in restraining pro-inflammatory cytokine. Synonyms: GSK-5498A; GSK5498A; GSK 5498A; 2,6-Difluoro-N-(1-(2-fluoro-6-(trifluoromethyl)benzyl)-1H-pyrazol-3-yl)benzamide. Grade: 97%. CAS No. 1253186-49-0. Molecular formula: C18H11F6N3O. Mole weight: 399.29.
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. Grade: 98%. CAS No. 871819-90-8. Molecular formula: C19H19ClN4O2. Mole weight: 370.84.
GSK572A
GSK572A is a new and powerful EchA6 potent inhibitor that can be used to treat pulmonary tuberculosis. Synonyms: (5R,7S)-5-(4-Ethylphenyl)-N-[(5-Fluoropyridin-2-yl)methyl]-7-(Trifluoromethyl)-4,5,6,7-Tetrahydropyrazolo[1,5-A]pyrimidine-3-Carboxamide. Grade: >98.0%. CAS No. 1403602-32-3. Molecular formula: C22H21F4N5O. Mole weight: 447.44.
GSK583
GSK583 is a selective receptor-interacting serine/threonine-protein kinase 2 (RIP2 Kinase) inhibitor and the RIP2K binding IC50 is 5 nM. GSK583 can inhibit both TNF-α and IL-6 production with an IC50 value of 200 nM in an ex vivo human translational model. Synonyms: GSK583; GSK 583; GSK-583. 6 - (tert-Butylsulfonyl) - N - (5-fluoro - 1H - indazol-3-yl)quinolin-4-amine. Grade: 98%. CAS No. 1346547-00-9. Molecular formula: C20H19FN4O2S. Mole weight: 398.46.
GSK5959
GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 value of 80 nM. It exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. It is used at 10 μM final concentration in various in vitro assays. It disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3 in vitro. Uses: Gsk-5959 disrupts chromatin binding of brpf1 in a cellular assay. Synonyms: N-(1,3-dimethyl-2-oxo-6-piperidin-1-ylbenzimidazol-5-yl)-2-methoxybenzamide; GSK-5959; GSK 5959; GSK5959. Grade: >98%. CAS No. 901245-65-6. Molecular formula: C22H26N4O3. Mole weight: 394.47.
GSK598809
GSK598809 is a potent and selective antagonist of dopamine D3 Receptor (DRD3), with a pKi of 8.9. Synonyms: 5-(5-(3-(1-(2-fluoro-4-(trifluoromethyl)phenyl)-3-azabicyclo[3.1.0]hexan-3-yl)propylthio)-4-methyl-4H-1,2,4-triazol-3-yl)-4-methyloxazole; 3-Azabicyclo[3.1.0]hexane, 1-[2-fluoro-4-(trifluoromethyl)phenyl]-3-[3-[[4-methyl-5-(4-methyl-5-oxazolyl)-4H-1,2,4-triazol-3-yl]thio]propyl]-; 1-[2-Fluoro-4-(trifluoromethyl)phenyl]-3-(3-{[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]sulfanyl}propyl)-3-azabicyclo[3.1.0]hexane. Grade: ≥95%. CAS No. 863680-45-9. Molecular formula: C22H23F4N5OS. Mole weight: 481.51.
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. Grade: 98%. CAS No. 1310803-30-5. Molecular formula: C23H25F4N5OS. Mole weight: 495.54.
GSK620
GSK620 is a potent, selective and orally active pan-BD2 inhibitor. GSK620 shows an anti-inflammatory phenotype in human whole blood. GSK620 reduces the MCP-1 response in a concentration-dependent manner with (an expected) ?1 log drop off in potency relative to the biochemical BRD4 BD2 potencies observed. Synonyms: QCZ. CAS No. 2088410-46-0. Molecular formula: C18H19N3O3. Mole weight: 325.36.
GSK621
GSK621 is an activator of AMP-activated protein kinase (AMPK). GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation. Synonyms: GSK-621; GSK 621. Grade: 98%. CAS No. 1346607-05-3. Molecular formula: C26H20ClN3O5. Mole weight: 489.91.
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. Grade: >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. Grade: 0.98. CAS No. 890842-28-1. Molecular formula: C25H22N2O2. Mole weight: 382.45.
GSK656
GSK656 is a potent inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM. Synonyms: Ethanol, 2-(((3S)-3-(aminomethyl)-4-chloro-1,3-dihydro-1-hydroxy-2,1-benzoxaborol-7-yl)oxy)-, hydrochloride (1:1). Grade: 99%. CAS No. 2131798-13-3. Molecular formula: C10H14BCl2NO4. Mole weight: 293.94.
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. Grade: >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.
GSK 690 Hydrochloride
GSK 690 Hydrochloride is a reversible lysine specific demethylase 1 (LSD1) inhibitor, with a Kd of 9 nM and a biochemical IC50 of 37 nM. Synonyms: 4-{2-(4-Methylphenyl)-5-[(3R)-3-pyrrolidinylmethoxy]-3-pyridinyl}benzonitrile hydrochloride (1:1); Benzonitrile, 4-[2-(4-methylphenyl)-5-[(3R)-3-pyrrolidinylmethoxy]-3-pyridinyl]-, hydrochloride (1:1). Grade: ≥95%. Molecular formula: C24H24ClN3O. Mole weight: 405.92.
GSK-693
A novel direct InhA inhibitor of Mtb (IC50 = 7 nM). Synonyms: (S)-1-(4-Methylthiazol-2-yl)-1-(5-((1-((2-methylthiazol-4-yl)methyl)-1H-pyrazol-3-yl)amino)-1,3,4-thiadiazol-2-yl)ethan-1-ol. CAS No. 1372891-37-6. Molecular formula: C16H17N7OS3. Mole weight: 419.55.
GSK717
GSK717 is a potent and selective NOD2 inhibitor. It inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells. Grade: 99%. CAS No. 1595278-21-9. Molecular formula: C28H28N4O2. Mole weight: 452.55.
GSK-7186
GSK-7186 is a novel inhibitor of HIV integrase that is used for the treatment of Non-cross-resistant HIV infection. Uses: The treatment of non-cross-resistant hiv infection. Synonyms: GSK7186; GSK 7186.
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-. Grade: >98%. CAS No. 1067214-81-6. Molecular formula: C25H22N2O6S. Mole weight: 478.52.
GSK726701A
GSK726701A is a prostaglandin E2 receptor 4 (EP4) partial agonist with pEC50 value of 7.4. Synonyms: {4-[4,9-Bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid. Grade: 98%. CAS No. 945721-87-9. Molecular formula: C24H22FNO5. Mole weight: 423.43.
GSK778
GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. Synonyms: GSK-778; GSK 778; iBET-BD1. Grade: 99%. CAS No. 2451862-42-1. Molecular formula: C30H33N5O3. Mole weight: 511.63.
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. Grade: ≥99% by HPLC. CAS No. 1257326-24-1. Molecular formula: C15H21N3O.HCl. Mole weight: 295.81.
GSK-7975A
This active molecular is a calcium release-activated calcium modulator (ORAI1) inhibitor. GSK-7975A inhibited toxin-induced activation of ORAI1 and/or activation of Ca(2+) currents after Ca(2+) release in mouse and human pancreatic acinar cells. GSK-7975A may be used for the treatment of pancreatitis in the future. Uses: Pancreatitis. Synonyms: GSK-7975A; GSK 7975A; GSK7975A; GSK-7975; GSK 7975; GSK7975. SCHEMBL705705; AOB4124; CPYTVBALBFSXSH-UHFFFAOYSA-N; 2,6-difluoro-N-[1-[[4-hydroxy-2-(trifluoromethyl)phenyl]methyl]pyrazol-3-yl]benzamide. Grade: 98%. CAS No. 1253186-56-9. Molecular formula: C18H12F5N3O2. Mole weight: 397.31.
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. Grade: 99%. CAS No. 13616-29-0. Molecular formula: C23H22N8O5S2. Mole weight: 554.6.
GSK840
GSK840 is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which suppressed recombinant RIP3 kinase activity with IC50 of 0.3 nM. Synonyms: GSK 840; GSK-840. Grade: >98%. CAS No. 2361146-30-5. Molecular formula: C21H23N3O3. Mole weight: 365.4.
GSK-843
GSK-843 is a potent and selective receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with IC50 of 8.6 nM. Synonyms: GSK843; GSK 843. Grade: >98%. CAS No. 1601496-05-2. Molecular formula: C19H15N5S2. Mole weight: 377.5.
GSK-8573
GSK-8573 is an inactive control of GSK-2801, which is a potent inhibitor of BAZ2A and BAZ2B bromodomains. Synonyms: GSK8573; GSK 8573; GSK-8573; 1-[1-(3-Methoxyphenyl)-7-propoxyindolizin-3-yl]ethanone. CAS No. 1693766-04-9. Molecular formula: C20H21NO3. Mole weight: 323.392.
GSK8612
GSK8612 is a novel potent and highly selective TBK1 inhibitor, displaying an excellent selectivity profile and therefore represents an ideal probe to further dissect the biology of TBK1 in models of immunity, neuroinflammation, obesity, or cancer. Synonyms: GSK-8612; GSK 8612. CAS No. 2361659-62-1. Molecular formula: C17H17BrF3N7O2S. Mole weight: 520.33.
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'872
GSK'872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with high affinity (IC50=1.8 nM), and is approximately >1,000-fold selective over 300 kinases in a fluorescence polarization assay at a concentration of 1 μM. Besides, GSK'872 inhibits kinase activity (IC50=1.3 nM). Synonyms: GSK872; GSK-872; GSK 872; N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine. CAS No. 1346546-69-7. Molecular formula: C19H17N3O2S2. Mole weight: 383.49.
GSK-872 hydrochloride
GSK-872 hydrochloride is an RIPK3 inhibitor. It binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. Grade: 99%. CAS No. 2703752-81-0. Molecular formula: C19H18ClN3O2S2. Mole weight: 419.95.
GSK894490A
GSK894490A is a non-peptide ghrelin receptor agonist. It crosses the blood/brain barrier and elicit pro-cognitive effects in recognition and spatial learning and memory tests. It may be used as a potential drug target for therapeutic approaches to treat diseases affecting cognition. Uses: Gsk894490a may be used as a potential drug target for therapeutic approaches to treat diseases affecting cognition. Synonyms: Benzenesulfonamide, N-(5-((3R,5S)-3,5-dimethyl-1-piperazinyl)-2-methoxyphenyl)-4-(5-methyl-2-furanyl)-, hydrochloride (1:1), rel-; N-[5-[(3R,5S)-3,5-dimethylpiperazin-1-yl]-2-methoxyphenyl]-4-(5-methylfuran-2-yl)benzenesulfonamide hydrochloride; GSK-894490A. Grade: >98 %. CAS No. 1012035-06-1. Molecular formula: C24H30ClN3O4S. Mole weight: 492.03.
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. Grade: ≥98% by HPLC. CAS No. 1229096-88-1. Molecular formula: C27H19F4N3O2S. Mole weight: 525.52.
GSK-923295
GSK-923295 is a novel antimitotic inhibitor of centromere-associated protein E (CENP-E) with potential anticancer activity. GSK-923295 demonstrated significant antitumor activity against solid tumor models, inducing CRs in Ewing sarcoma, rhabdoid, and rhabdomyosarcoma xenografts. Clinical study showed that GSK-923295 had dose-proportional pharmacokinetics and a low number of grade 3 or 4 adverse events. The observed incidence of myelosuppression and neuropathy was low. Further investigations may provide a more complete understanding of the potential for GSK-923295 as an antiproliferative agent. Synonyms: GSK923295; GSK 923295; GSK-923295; GSK-923295A; GSK923295A; GSK 923295A. Grade: 98%. CAS No. 1088965-37-0. Molecular formula: C32H38ClN5O4. Mole weight: 592.14.
GSK 9311 hydrochloride
GSK9311 is a potent inhibitor of the BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively. GSK 9311 is a negative control for the SGC epigenetic probe GSK6853. Synonyms: N-[2,3-Dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-N-ethyl-2-methoxybenzamide hydrochloride. Grade: ≥98% by HPLC. CAS No. 1923851-49-3. Molecular formula: C24H31N5O3·HCl. Mole weight: 474.
GSK9311 hydrochloride
GSK9311 hydrochloride is a less active analogue of GSK6853 and can be used as a negative control. It inhibits BRPF bromodomain with pIC50s of 6.0 and 4.3 for BRPF1 and BRPF2, respectively. Synonyms: N-{1,3-Dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl}-N-ethyl-2-methoxybenzamide hydrochloride (1:1); N-[2,3-Dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-N-ethyl-2-methoxybenzamide hydrochloride; Benzamide, N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-N-ethyl-2-methoxy-, hydrochloride (1:1). CAS No. 2253733-09-2. Molecular formula: C24H32ClN5O3. Mole weight: 474.00.
GSK962
GSK962 is an inactive enantiomer of GSK963, a novel highly potent and selective RIP1 inhibitor. Synonyms: GSK 962; GSK-962. Grade: >98%. CAS No. 2049872-86-6. Molecular formula: C14H18N2O. Mole weight: 230.31.
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-
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. Grade: >98%. CAS No. 923565-22-4. Molecular formula: C25H34ClFN4O. Mole weight: 461.02.