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| Product | Description | |
|---|---|---|
| GSK2194069 | GSK2194069 is a fatty acid synthase (FAS) inhibitor. GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM for the overall hFAS reaction. FAS is upregulated in some cancers, including prostate cancer. GSK2194069 was found to inhibit tumour growth in prostate cancer C42b cell xenografts generated in Nod-SCID-gamma mice. Cellular FAS inhibition reduced cell growth were also demonstrated in non-small-cell lung (A549) cancer cell lines with an average EC50 of 15 ± 0.5 nM. Synonyms: GSK 2194069; GSK-2194069. Grade: >98%. CAS No. 1332331-08-4. Molecular formula: C25H24N4O3. Mole weight: 428.48. |  |
| GSK2200150A | GSK2200150A, identified by high-throughput screening (HTS) campaign, is an anti-tuberculosis (TB) agent. It is a novel antimycobacterial agent against Mycobacterium tuberculosis. Synonyms: GSK-2200150A. Grade: 95%. CAS No. 1443138-53-1. Molecular formula: C20H23NO3S. Mole weight: 357.47. | |
| GSK2245035 | This active molecular is a selective TLR7 (Toll-like receptor 7) agonist with preferential Type-1 IFN-stimulating properties which is under development of GlaxoSmithKline. GSK2245035 displays potent IFNα inducing potency and IFNα/TNFα selectivity. In Aug 2015, GlaxoSmithKline completed a phase II follow-up trial for Allergic asthma and Allergic rhinitis in Canada. In Jul 2016, GlaxoSmithKline planed a phase II trial for Allergic asthma in Germany (Intranasal). Uses: Allergic asthma; allergic rhinitis. Synonyms: GSK2245035; GSK 2245035; GSK-2245035; (S)-6-amino-2-(pentan-2-yloxy)-9-(5-(piperidin-1-yl)pentyl)-7,9-dihydro-8H-purin-8-one; 1325212-97-2 (maleate salt). Grade: 98%. CAS No. 1207629-49-9. Molecular formula: C20H34N6O2. Mole weight: 390.52. | |
| GSK 2250665A | GSK 2250665A is an Itk inhibitor (pKi = 9.2) displaying selectivity for Itk over Aurora B kinase and Btk (pIC50 = 6.4 and 6.5, respectively) and a panel of other kinases. GSK 2250665A was shown to inhibit IFNγ production in PBMCs. Synonyms: GSK-2250665A; GSK 2250665A; GSK2250665A; GSK-2250665; GSK 2250665; GSK2250665; trans-4-[[4-[(6-Ethyl-2-benzothiazolyl)amino]-6-(phenylmethyl)-2-pyrimidinyl]amino]cyclohexanol. Grade: ≥97% by HPLC. CAS No. 1246030-96-5. Molecular formula: C26H29N5OS. Mole weight: 459.61. | |
| GSK-2256098 | GSK2256098, also known as GTPL7939, is a focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. Synonyms: GSK2256098; GSK 2256098; GSK-2256098; GTPL7939; GTPL-7939; GTP L7939. Grade: 98%. CAS No. 1224887-10-8. Molecular formula: C20H23ClN6O2. Mole weight: 414.89. | |
| GSK2256294A | GSK2256294A, an effective inhibitor of human soluble epoxide hydrolase(sEH), was developed by GSK and still under Phase I trial in Chronic obstructive pulmonary disease. IC50: 27pM. Uses: Gsk2256294a is an effective inhibitor of human soluble epoxide hydrolase(seh). Synonyms: GSK2256294; GSK-2256294; GSK 2256294; GSK-2256294A; GSK 2256294A. Grade: 98%. CAS No. 1142090-23-0. Molecular formula: C21H24F3N7O. Mole weight: 447.46. | |
| GSK-2262167 hydrate | GSK-2262167 is a potent S1P3-sparing and S1P1 agonist and has a potent activity is in a collagen-induced arthritis model as efficacious as fingolimod and shows excellent pharmacokinetic properties preclinically. Uses: Arthritis. Synonyms: GSK-2262167 sodium; GSK 2262167 sodium; GSK2262167 sodium; sodium 3-(6-(5-(3-cyano-4-isopropoxyphenyl)-1,2,4-oxadiazol-3-yl)-5-methyl-3,4-dihydroisoquinolin-2(1H)-yl)propanoate. Grade: ≥98%. CAS No. 1458576-13-0. Molecular formula: C25H28N4O5. Mole weight: 464.51. | |
| GSK-2262167 sodium | This molecular is a potent S1P3-sparing and S1P1 agonist. Meanwhile GSK-2262167 has a potent activity is in a collagen-induced arthritis model as efficacious as fingolimod and shows excellent pharmacokinetic properties preclinically. Uses: Arthritis. Synonyms: GSK-2262167 sodium; GSK 2262167 sodium; GSK2262167 sodium; sodium 3-(6-(5-(3-cyano-4-isopropoxyphenyl)-1,2,4-oxadiazol-3-yl)-5-methyl-3,4-dihydroisoquinolin-2(1H)-yl)propanoate,1165924-28-6 (free acid); 458576-13-0 (hydrate). Grade: 98%. CAS No. 1165923-54-5. Molecular formula: C25H25N4NaO4. Mole weight: 468.49. | |
| GSK2269557 | GSK2269557, an effective PI3K inhibitor, could be used as against inflammatory and some autoimmune diseases. It has just completes a phase II trial against Asthma. Uses: Gsk2269557 is an effective pi3k inhibitor that could be used as against inflammatory and some autoimmune diseases. Synonyms: CHEMBL2216859; GSK2269557 (free base); GSK2269557; GSK-2269557; GSK 2269557; Nemiralisib; 2-(6-(1H-indol-4-yl)-1H-indazol-4-yl)-5-((4-isopropylpiperazin-1-yl)methyl)oxazole; 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole. Grade: 95%. CAS No. 1254036-71-9. Molecular formula: C26H28N6O. Mole weight: 440.54. | |
| GSK-2269557 HCl salt | GSK-2269557 is a selective Phosphatidylinositol 3 kinase delta inhibitor originated by GlaxoSmithKline. GSK-2269557 is highly selective for PI3Kδ over the closely related isoforms and is active in a animal model of Th2-driven lung inflammation. Treatment for Asthma and Chronic obstructive pulmonary disease(COPD) is in clinical trials Phase II. Uses: Asthma; chronic obstructive pulmonary disease. Synonyms: GSK-2269557 HCl salt; GSK 2269557 HCl salt; GSK2269557 HCl salt; 6-(1H-indol-4-yl)?-4-[5-[[4-(1-methylethyl)?-1-piperazinyl]?methyl]?-2-oxazolyl]?-1H-indazole, monohydrochloride; 1254036-71-9(free base). Grade: 98%. CAS No. 1254036-77-5. Molecular formula: C26H28N6O; HCl. Mole weight: 477.01. | |
| GSK2292767 | GSK2292767 is a Phosphatidylinositol 3 kinase delta inhibitor applicated for the treatment of respiratory diseases including asthma and COPD in clinical trials. GSK2292767 is highly selective for PI3Kδ over the closely related isoforms and is really active in the animal model of Th2-driven lung inflammation. Uses: Asthma and copd. Synonyms: GSK2292767; GSK-2292767; GSK 2292767. N-[5-[4-[5-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]methyl]-1,3-oxazol-2-yl]-1H-indazol-6-yl]-2-methoxypyridin-3-yl]methanesulfonamide; SCHEMBL173490; ZINC95938263; KB-78330; 1254036-66-2; Methanesulfonamide,N-[5-[4-[5-[[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]. Grade: 98%. CAS No. 1254036-66-2. Molecular formula: C24H28N6O5S. Mole weight: 512.58. | |
| GSK232 | GSK232, a highly selective, cellularly penetrant inhibitor of CECR2, has excellent physicochemical properties. Synonyms: (S)-N-(4-chloro-3-((3-cyclopropylpyrrolidin-1-yl)sulfonyl)phenyl)-2-(5-methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridin-1-yl)acetamide. CAS No. 2702984-69-6. Molecular formula: C21H27ClN6O3S. Mole weight: 479.00. | |
| GSK2330672 | GSK-2330672, an ASBT inhibitor, has been developed for the treatment of type 2 diabetes and is currently under Phase II trail against primary biliary cirrhosis and type 2 diabetes. IC50: 42 ± 3 nM. Uses: Gsk-2330672 is an asbt inhibitor that has been developed for the treatment of type 2 diabetes and is currently under phase ii trail against primary biliary cirrhosis and type 2 diabetes. Synonyms: CHEMBL2387408; UNII-386012Z45S; GSK2330672; GSK-2330672; SCHEMBL2586025; CZGVOBIGEBDYTP-VSGBNLITSA-N. Grade: 98%. CAS No. 1345982-69-5. Molecular formula: C28H38N2O7S. Mole weight: 546.68. | |
| GSK2332255B | GSK2332255B is a potent and selective antagonist of TRPC3 and TRPC6 with IC50s of 5 and 4 nM for rat TRPC3 and rat TRPC6, respectively. It exhibits ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels. Synonyms: (5-chloro-2-((6-fluorobenzo[d][1,3]dioxol-5-yl)amino)thiazol-4-yl)(2,3-dimethylpiperidin-1-yl)methanone; Methanone, [5-chloro-2-[(6-fluoro-1,3-benzodioxol-5-yl)amino]-4-thiazolyl](2,3-dimethyl-1-piperidinyl)-; GSK-255B. Grade: ≥90%. CAS No. 1366233-41-1. Molecular formula: C18H19ClFN3O3S. Mole weight: 411.88. | |
| GSK2334470 | GSK2334470 is a potent 3-phosphoinositide-dependent protein kinase (PDK1) inhibitor (IC50 ~ 10 nM), which does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. GSK2334470 also inhibited T-loop phosphorylation and activation of Akt. GSK2334470 will be a useful tool for delineating the roles of PDK1 in biological processes. Synonyms: GSK2334470; GSK2334470; GSK2334470. Grade: 0.98. CAS No. 1227911-45-6. Molecular formula: C25H34N8O. Mole weight: 462.602. | |
| GSK-239512 | GSK-239512 is a histamine H3 receptor antagonist. In Jun 2015, Phase-II for Schizophrenia in USA was discontinued. Phase II clinical trilas for the treatment of Multiple sclerosis are on-going. Uses: Multiple sclerosis. Synonyms: GSK-239512; GSK239512; GSK 239512; 1-(6-((3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-3-pyridinyl)-2-Pyrrolidinone. Grade: 98%. CAS No. 720691-69-0. Molecular formula: C23H27N3O2. Mole weight: 377.48. | |
| GSK-25 | GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor with an IC50 of 7 nM. GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50 = 398 nM, p70S6K: IC50 = 1 μM). Synonyms: GSK25; GSK 25; 5-Pyrimidinecarboxamide, 4-(4-chloro-2-fluorophenyl)-2-(2-chloro-4-pyridinyl)-N-(6-fluoro-1H-indazol-5-yl)-1,4-dihydro-6-Methyl-. Grade: 99%. CAS No. 874119-56-9. Molecular formula: C24H16Cl2F2N6O. Mole weight: 513.33. | |
| GSK251 | GSK251 is a potent and selective PI3Kδ inhibitor. Synonyms: GSK-251; GSK 251. Grade: 98% by HPLC. CAS No. 2125968-05-8. Molecular formula: C29H37FN6O4S. Mole weight: 584.7. | |
| GSK256066 | GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. Synonyms: GSK256066; GSK 256066; GSK-256066. Grade: >98%. CAS No. 801312-28-7. Molecular formula: C27H26N4O5S. Mole weight: 518.58. | |
| GSK256066 2,2,2-trifluoroacetic acid | GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. Synonyms: GSK-256066; GSK 256066. Grade: >98%. CAS No. 1415560-64-3. Molecular formula: C29H27F3N4O7S. Mole weight: 632.61. | |
| GSK256073 | GSK256073 is a potent, selective and orally active G-protein coupled receptor 109A (GPR109A) agonist and a long-lasting and non-flushing hydroxy-carboxylic acid receptor 2 (HCA2) full agonist with a pEC50 of 7.5 for human HCA2. It acutely improves glucose homeostasis by inhibiting lipid breakdown and has the potential to study type 2 diabetes mellitus (T2DM) and dyslipidemia. Synonyms: 8-Chloro-3-pentyl-1H-purine-2,6(3H,7H)-dione; 1H-Purine-2,6-dione, 8-chloro-3,9-dihydro-3-pentyl-; 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione; 8-Chloro-6-hydroxy-3-pentyl-3,9-dihydro-2H-purin-2-one. Grade: ≥95%. CAS No. 862892-90-8. Molecular formula: C10H13ClN4O2. Mole weight: 256.69. | |
| GSK256471 | This active molecular is a selective and potent NK(3) antagonist. It has a high affinity for recombinant human (pK(I) value 8.9) and native guinea pig (pK(I) value 8.4) tachykinin NK(3) receptors. In the near future, GSK256471 may be potentially very useful in the treatment of schizophrenia. Uses: Treatment of schizophrenia. Synonyms: GSK256471; GSK-256471; GSK 256471. N-[(S)-cyclopropyl(phenyl)methyl]-3-[[methyl(methylsulfonyl)amino]methyl]-2-phenylquinoline-4-carboxamide. Grade: 98%. CAS No. 1133706-08-7. Molecular formula: C29H29N3O3S. Mole weight: 499.63. | |
| GSK2578215A | GSK2578215A induces a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells. Synonyms: GSK2578215A; GSK-2578215A; GSK 2578215A. Grade: >98%. CAS No. 1285515-21-0. Molecular formula: C24H18FN3O2. Mole weight: 399.42. | |
| GSK2578999A | GSK2578999A is a potent HIV-1 maturation inhibitor with IC50 values of 17 nM, 23 nM, 25 nM, and 8 nM for wild type, Q369H, V370A, and T371A respectively. Synonyms: GSK-8999; (3β)-3-(3-carboxy-3-methyl-1-oxobutoxy)-N-[1-(4-chlorophenyl)cyclopropyl]-α,21-dioxo-28-norlup-18-ene-17-acetamide. CAS No. 1422355-59-6. Molecular formula: C46H62ClNO7. Mole weight: 776.4. | |
| GSK2593074A | GSK2593074A is a necroptosis inhibitor for dual-targeting to both RIP1 and RIP3. Synonyms: GSK'074; 7-(1-methyl-1H-pyrazol-4-yl)-3-[1-(phenylacetyl)-2,3-dihydro-1H-indol-5-yl]thieno[3,2-c]pyridin-4-amine. Grade: 99%. CAS No. 1337531-06-2. Molecular formula: C27H23N5OS. Mole weight: 465.57. | |
| GSK 2606414 | GSK 2606414 is a potent and selective PERK inhibitor that suppresses PERK activation in cells and inhibits the growth of a human tumor xenograft in mice. Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. Evidence that PERK is implicated in tumorigenesis and cancer cell survival stimulated our search for small-molecule inhibitors. Synonyms: GSK2606414; GSK-2606414; GSK 2606414; GSK PERK Inhibitor. 1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone. Grade: 98%. CAS No. 1337531-36-8. Molecular formula: C24H20F3N5O. Mole weight: 451.453. | |
| GSK2636771 | GSK2636771 is an orally bioavailable, substituted benzimidazole inhibitor of the class I phosphoinositide 3-kinase (PI3K) beta isoform with potential antineoplastic activity. PI3K beta inhibitor GSK2636771 selectively inhibits PI3K beta kinase activity in the PI3K/Akt/mTOR pathway, which may result in tumor cell apoptosis and growth inhibition in PI3K beta-expressing and/or PTEN-driven tumor cells. Dysregulation of the PI3K/Akt/mTOR pathway is frequently found in solid tumors and results in the promotion of tumor cell growth, survival, and resistance to both chemotherapy and radiotherapy. PI3K beta is the p110-beta catalytic subunit of the class I PI3K. PTEN, a tumor suppressor protein and negative regulator of PI3K activity, is often mutated in a variety of cancer cells. Uses: Antineoplastic agents. Synonyms: GSK2636771; GSK-2636771; GSK 2636771. CAS No. 1372540-25-4. Molecular formula: C22H22F3N3O3. Mole weight: 433.431. | |
| GSK 2636771 dihydrochloride | GSK 2636771 is an orally bioavailable, substituted benzimidazole inhibitor of the class I phosphoinositide 3-kinase (PI3K) beta isoform with potential antineoplastic activity. PI3K beta inhibitor GSK 2636771 selectively inhibits PI3K beta kinase activity in the PI3K/Akt/mTOR pathway, which may result in tumor cell apoptosis and growth inhibition in PI3K beta-expressing and/or PTEN-driven tumor cells. Dysregulation of the PI3K/Akt/mTOR pathway is frequently found in solid tumors and results in the promotion of tumor cell growth, survival, and resistance to both chemotherapy and radiotherapy. PI3K beta is the p110-beta catalytic subunit of the class I PI3K. PTEN, a tumor suppressor protein and negative regulator of PI3K activity, is often mutated in a variety of cancer cells. Synonyms: GSK-2636771 dihydrochloride; GSK2636771 dihydrochloride; 2-methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acid dihydrochloride. Grade: 99%. CAS No. 2108806-07-9. Molecular formula: C22H22F3N3O3.2HCl. Mole weight: 506.35. | |
| GSK 264220A | GSK 264220A is an endothelial lipase and lipoprotein lipase inhibitor (IC50 = 0.13 and 0.10 μM, respectively). Inhibition of endothelial lipase may lead to an increase in HDL levels and GSK 264220A is expected to be a therapy for cardiovascular disease. Uses: Potential treatment of cardiovascular disease. Synonyms: GSK-264220A; GSK 264220A; GSK264220A. N-[2-Methyl-5-(1-piperidinylsulfonyl)-3-furanyl]-N'-phenylurea; 3-[2-methyl-5-(piperidine-1-sulfonyl)furan-3-yl]-1-phenylurea; 1-(2-methyl-5-piperidin-1-ylsulfonylfuran-3-yl)-3-phenylurea. Grade: ≥98% by HPLC. CAS No. 685506-42-7. Molecular formula: C17H21N3O4S. Mole weight: 363.43. | |
| GSK2643943A | GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor with IC50 of 160 nM for USP20/Ub-Rho. Synonyms: GSK 2643943A; GSK-2643943A. CAS No. 2449301-27-1. Molecular formula: C17H12FN3. Mole weight: 277.30. | |
| GSK2656157 | GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC50 of 0.9 nM. It is highly selective for PERK with IC50 values >100 nM against a panel of 300 kinases. GSK2656157 inhibits PERK activity in cells with an IC50 in the range of 10-30 nM as shown by inhibition of stress-induced PERK autophosphorylation, eIF2α substrate phosphorylation, together with corresponding decreases in ATF4 and CHOP proteins in multiple cell lines. Oral administration of GSK2656157 to mice shows a dose- and time-dependent pharmacodynamic response in pancreas as measured by PERK auto-phosphorylation. Twice daily dosing of GSK2656157 results in dose dependent inhibition of multiple human tumor xenografts growth in mice. Altered amino acid metabolism, decreased blood vessel density and vascular perfusion are potential mechanisms for the observed anti-tumor effect. However, despite its anti-tumor activity, given the on-target pharmacological effects of PERK inhibition on pancreatic function, development of any PERK inhibitor in human subjects would need to be cautiously pursued in cancer patients. Synonyms: GSK2656157; GSK 2656157; GSK-2656157. Grade: 0.98. CAS No. 1337532-29-2. Molecular formula: C23H21FN6O. Mole weight: 416.46. | |
| GSK 269962 | GSK 269962 is a potent ROCK inhibitor with IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively, which displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. It may be used in OAB treatment. It has been shown to block the generation of inflammatory cytokines in lipopolysaccharide-stimulated monocytes and to induce vasorelaxation in preconstricted rat aorta (IC50 = 35 nM). It lowers blood pressure in a rat model of hypertension. It induced a reduction in blood pressure of approximately 10, 20, and 50 mm Hg at doses of 1, 3, and 30 mg/kg. It represent a novel class of ROCK inhibitors that have profound effects in the vasculature, which may enable us to further evaluate the potential beneficial effects of ROCK inhibition in animal models of cardiovascular as well as other chronic diseases. Uses: Gsk 269962 may be used in oab treatment. it represent a novel class of rock inhibitors. Synonyms: GSK269962A; N-[3-[[2-(4-Aminofurazan-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy]phenyl]-4-[[2-(4-morpholinyl)ethyl]oxy]benzamide; Aminofurazanyl-azabenzimidazole 6n; N-[3-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethylimidazo[4,5-c]pyridin-6-yl]oxyphenyl]-4-(2-morpholin-4-ylethoxy)benzamide. Grade: >99 %. CAS No. 850664-21-0. Molecular formula: C29H30N8O5. Mole weight: 570.60. | |
| GSK269962A HCl | GSK269962 is a selective inhibitor of ROCK (Rho-associated protein kinase) with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively. GSK269962 displays > 30-fold selectivity for ROCK against a panel of serine/threonine kinases. Synonyms: GSK269962B; GSK269962; GSK 269962. Molecular formula: C29H30N8O5·HCl. Mole weight: 607.06. | |
| GSK269962A hydrochloride | GSK269962A hydrochloride is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A hydrochloride has anti-inflammatory and vasodilatory activities. Synonyms: GSK269962 HCl; GSK 269962 hydrochloride. CAS No. 2095432-71-4. Molecular formula: C29H31ClN8O5. Mole weight: 607.06. | |
| GSK-269984A | GSK-269984A is a Prostaglandin E2 Receptor 1 antagonist with a pIC50 of 8.1. Synonyms: 2-Pyridinecarboxylic acid, 6-((5-chloro-2-((4-chloro-2-fluorophenyl)methoxy)phenyl)methyl)-, sodium salt. Grade: 95%. CAS No. 892664-04-9. Molecular formula: C20H13Cl2FNNaO3. Mole weight: 428.22. | |
| GSK-270822A | GSK-270822A is a G protein-coupled receptor kinases(GRK2) inhibitor, which has been directly implicated in the progression of heart failure. It would be used as useful chemical probes and leads for therapeutic applications ranging from heart failure to Parkinson's disease. Uses: Gsk-270822a would be used as useful chemical probes and leads for therapeutic applications ranging from heart failure to parkinson's disease. Synonyms: GSK270822A; GSK 270822A; N-(1H-indazol-5-yl)-2-methyl-4-(naphthalen-2-yl)-6-oxo-1,4,5,6-tetrahydropyridine-3-carboxamide; NSC-756163. Grade: 98%. CAS No. 864082-23-5. Molecular formula: C24H20N4O2. Mole weight: 396.45. | |
| GSK2795039 | GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2) with pIC50 of 6. GSK2795039 inhibited both the formation of ROS and the utilization of the enzyme substrates, NADPH and oxygen, in a variety of semirecombinant cell-free and cell-based NOX2 assays. Synonyms: GSK-2795039; GSK 2795039. CAS No. 1415925-18-6. Molecular formula: C23H26N6O2S. Mole weight: 450.56. | |
| GSK2801 | GSK2801 is a A Selective Chemical Probe for BAZ2B/A bromodomains. BAZ2A/B belong to a family of ubiquitously expressed bromodomain containing proteins.probes/GSK2801). Synonyms: GSK2801; GSK-2801; GSK 2801. Grade: 98%. CAS No. 1619994-68-1. Molecular formula: C20H21NO4S. Mole weight: 371.45. | |
| GSK2807 Trifluoroacetate | GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive SMYD3 inhibitor, with a Ki of 14 nM and an IC50 of 130 nM. Synonyms: (S)-2-Amino-4-((((2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(3-(dimethylamino)propyl)amino)butanoic acid 2,2,2-trifluoroacetic acid; 5'-{[(3S)-3-Amino-3-carboxypropyl][3-(dimethylamino)propyl]amino}-5'-deoxyadenosine trifluoroacetate (1:1); Acetic acid, 2,2,2-trifluoro-, compd. with adenosine, 5'-[[(3S)-3-amino-3-carboxypropyl][3-(dimethylamino)propyl]amino]-5'-deoxy- (1:1). Grade: ≥95%. CAS No. 2245255-66-5. Molecular formula: C21H33F3N8O7. Mole weight: 566.53. | |
| GSK-2818713 | GSK-2818713 is a second-generation inhibitor of hepatitis C virus (HCV) NS5A replication. Compared to daclatasvir, a first-generation NS5A replication complex inhibitor, GSK-2818713 exhibited picomolar potency on genotype 1 variants. Uses: The treatment of hepatitis c. Synonyms: GSK-2818713; GSK2818713; GSK 2818713. | |
| GSK2830371 | GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM. Synonyms: GSK 2830371; GSK2830371; GSK-2830371. Grade: >98%. CAS No. 1404456-53-6. Molecular formula: C23H29ClN4O2S. Mole weight: 461.02. | |
| GSK2837808A | GSK2837808A is a potent and specific lactate dehydrogenase A (LDHA) with IC50 values of 1.9 and 14 nM for LDHA and LDHB, respectively and inhibits lactate production in selected cancer cell lines. Synonyms: GSK2837808A; GSK-2837808A; GSK 2837808A; GSK2837808; GSK-2837808; GSK 2837808. 3-[[3-(cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl]amino]-5-(3,5-difluorophenoxy)benzoic acid. CAS No. 1445879-21-9. Molecular formula: C31H25F2N5O7S. Mole weight: 649.62. | |
| GSK2838232 | GSK2838232, a derivative of Betulin, is a novel human immune virus (HIV) maturation inhibitor being developed for the treatment of chronic HIV infection. Uses: Anti-hiv agents. Synonyms: GSK2838232; GSK-2838232; GSK 2838232; 4-[[(3aR,5aR,5bR,7aR,9S,11aR,11bR,13aS)-3a-[(1R)-2-[(4-chlorophenyl)methyl-[2-(dimethylamino)ethyl]amino]-1-hydroxyethyl]-5a,5b,8,8,11a-pentamethyl-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3H-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dime. Grade: 99.34%. CAS No. 1443460-91-0. Molecular formula: C48H73ClN2O6. Mole weight: 809.56. | |
| GSK2850163 hydrochloride | GSK2850163 hydrochloride, an inositol-requiring enzyme-1 alpha (IRE1α) inhibitor, can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively. Synonyms: 2,7-Diazaspiro[4.5]decane-7-carboxamide, 2-[(3,4-dichlorophenyl)methyl]-N-[(4-methylphenyl)methyl]-, hydrochloride (1:1), (5R)-; (5R)-2-(3,4-Dichlorobenzyl)-N-(4-methylbenzyl)-2,7-diazaspiro[4.5]decane-7-carboxamide hydrochloride (1:1). CAS No. 2319838-09-8. Molecular formula: C24H30Cl3N3O. Mole weight: 482.87. | |
| GSK2879552 | GSK2879552 has been found to be a LSD1 inhibitor that could have antineoplastic effect through restraining the growth of overexpressed tumor cells. It was just planed a Phase I/II trail by GSK against Myelodysplastic syndromes. Uses: Gsk2879552 has been found to be a lsd1 inhibitor that could have antineoplastic effect through restraining the growth of overexpressed tumor cells. Synonyms: GSK2879552; UNII-GT77Z6Y09Z; GSK-2879552; GSK 2879552; GT77Z6Y09Z; 1401966-69-5; 4-((4-((((1R,2S)-2-Phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)benzoic acid. Grade: 98%. CAS No. 1401966-69-5. Molecular formula: C23H28N2O2. Mole weight: 364.48. | |
| GSK2879552 dihydrochloride | GSK2879552 dihydrochloride, a selective, irreversible and orally active lysine specific demethylase 1 (LSD1/KDM1A) inhibitor, has potential antineoplastic activity. Synonyms: Benzoic acid, 4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]-, hydrochloride (1:2); 4-{[4-({[(1R,2S)-2-Phenylcyclopropyl]amino}methyl)-1-piperidinyl]methyl}benzoic acid dihydrochloride. Grade: ≥95%. CAS No. 1902123-72-1. Molecular formula: C23H30Cl2N2O2. Mole weight: 437.40. | |
| GSK-2881078 | GSK-2881078, an indole derivative, has been found to be an androgen receptor modulator that could probably be effective against Cachexia. It is still under Phase I trail. Uses: Anabolic agents. Synonyms: GSK 2881078; GSK2881078; CS-5736; (R)-1-(1-(methylsulfonyl)propan-2-yl)-4-(trifluoromethyl)-1H-indole-5-carbonitrile. Grade: 98%. CAS No. 1539314-06-1. Molecular formula: C14H13F3N2O2S. Mole weight: 330.33. | |
| GSK-2894631A | GSK2894631A is an inhibitor of hematopoietic PGD synthase (HPGDS). Synonyms: HPGDS inhibitor 2. CAS No. 2101626-26-8. Molecular formula: C20H24F2N2O3. Mole weight: 378.4. | |
| GSK2982772 | GSK2982772, with potential effect to treat inflammatory diseases, potently binds to RIP1 with exquisite kinase specificity. In phase 2a clinical studies for psoriasis, rheumatoid arthritis, and ulcerative colitis. Synonyms: GSK2982772; GSK 2982772; GSK-2982772; 5-benzyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide. CAS No. 1622848-92-3. Molecular formula: C20H19N5O3. Mole weight: 377.4. | |
| GSK2983559 | GSK2983559 is a potent, selective and oral active inhibitor of receptor interacting protein 2 (RIP2) kinase. GSK2983559 exhibits activity in blocking many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples. Synonyms: RIP2 kinase inhibitor 1; RIPK2-IN-1; GSK-2983559; GSK 2983559. CAS No. 1579965-12-0. Molecular formula: C21H23N4O7PS2. Mole weight: 538.53. | |
| GSK299115A | GSK299115A is a G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor. Synonyms: GSK299115A; GSK 299115A; GSK-299115A. 4-(3,4-dichlorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyridine-5-carboxamide. Grade: 98%. CAS No. 864082-35-9. Molecular formula: C20H16Cl2N4O2. Mole weight: 415.27. | |
| GSK299423 | GSK299423 is an antibiotic agent and it seems potentially effective in treating patients infected with bacteria expressing the New Delhi metallo-beta-lactamase. GSK299423 is a Type II bacterial DNA topoisomerase inhibitor under the development of GlaxoSmithKline. Early research for the treatment of Gram-negative infections and Nosocomial infections was on-going in USA. Uses: Gram-negative infections; nosocomial infections. Synonyms: GSK299423; GSK 299423; GSK-299423; 4-(2-(4-(([1,3]oxathiolo[5,4-c]pyridin-6-ylmethyl)amino)piperidin-1-yl)ethyl)-6-methoxyquinoline-3-carbonitrile. Grade: 98%. CAS No. 1352149-24-6. Molecular formula: C25H27N5O2S. Mole weight: 461.58. | |
| GSK3004774 | GSK3004774 is a potent, nonabsorbable, gastrointestinally-restricted CaSR agonist, with an EC50 of 50 nM for human and pEC50s of 7.3, 6.6 and 6.5 for human, mouse and rat, respectively. Synonyms: 1-[3-({4-[(3R)-3-{[(1S)-1-(1-Naphthyl)ethyl]amino}-1-pyrrolidinyl]benzoyl}amino)propyl]-4-piperidinecarboxylic acid; 4-Piperidinecarboxylic acid, 1-[3-[[4-[(3R)-3-[[(1S)-1-(1-naphthalenyl)ethyl]amino]-1-pyrrolidinyl]benzoyl]amino]propyl]-. Grade: ≥97%. CAS No. 2138814-32-9. Molecular formula: C32H40N4O3. Mole weight: 528.69. | |
| GSK-3008348 | GSK-3008348 is an integrin αvβ6 antagonist developed for the treatment of idiopathic pulmonary fibrosis (IPF). Synonyms: GSK 3008348; GSK3008348. Grade: 98% by HPLC. CAS No. 1629249-33-7. Molecular formula: C29H38ClN5O2. Mole weight: 524.1. | |
| GSK3117391 | GSK3117391, a HDAC inhibitor, was developed by GSK considering its potential effect in the treatment of arthritis and rheumatoid. It was already being terminated the phase 1 trial. Uses: Gsk3117391, a hdac inhibitor, was developed by gsk considering its potential effect in the treatment of arthritis and rheumatoid. Synonyms: GSK3117391; GSK-3117391; GSK 3117391; GSK3117391A; GSK-3117391A; GSK 3117391A; HDAC-IN-3; SCHEMBL15144242; AFDPFLDWOXXHQM-NRFANRHFSA-N; CS-5448; HY-19772; 121555-EP2295410A1. Grade: 95%. CAS No. 1018673-42-1. Molecular formula: C22H33N3O4. Mole weight: 403.52. | |
| GSK3145095 | GSK3145095 is an orally active RIP1 kinase inhibitor with IC50 of 6.3 nM. It potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking RIP1 kinase-dependent cellular responses. Synonyms: GSK 3145095; GSK-3145095. CAS No. 1622849-43-7. Molecular formula: C20H17F2N5O2. Mole weight: 397.38. | |
| GSK317354A | GSK317354A is a G-Protein-Coupled Receptor Kinase 2 (GRK2) inhibitor,but no detailed information has been published yet. Synonyms: GSK317354A; GSK-317354A; GSK 317354A. 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-(6-(trifluoromethyl)pyridin-3-yl)-1,4-dihydropyrimidine-5-carboxamide. Grade: 98%. CAS No. 874119-13-8. Molecular formula: C25H18F4N6O. Mole weight: 494.45. | |
| 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. Grade: >98%. CAS No. 1816331-63-1. Molecular formula: C28H28FN5O3. Mole weight: 501.56. | |
| GSK329 | GSK329 is a potent and selective inhibitor of cardiac-specific kinase TNNI3K (TNNI3 interacting kinase) with IC50 of 10 nM. Synonyms: GSK-329; GSK 329; N-(3,5-dichloro-4-{[6-(methylamino)pyrimidin-4-yl]oxy}phenyl)-N'-[3-(trifluoromethyl)phenyl]urea; N-[3,5-Dichloro-4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]-N-[3-(trifluoromethyl)phenyl]-urea. Grade: 98% by HPLC. CAS No. 1268490-12-5. Molecular formula: C19H14Cl2F3N5O2. Mole weight: 472.2. | |
| GSK3326595 | GSK3326595, also called as EPZ015938, is an orally available and specific inhibitor of protein arginine methyltransferase 5 (PRMT5) that potently inhibits tumor growth in vitro and in vivo in animal models and has entered clinical trials for the treatment of solid tumors and non-Hodgkin's lymphoma. Synonyms: GSK-3326595; GSK 3326595; GSK3326595; EPZ015938; EPZ 015938; EPZ-015938; 6-[(1-acetylpiperidin-4-yl)amino]-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]pyrimidine-4-carboxamide. CAS No. 1616392-22-3. Molecular formula: C24H32N6O3. Mole weight: 452.55. | |
| GSK3368715 3HCl | GSK3368715 is a potent reversible inhibitor of type I protein arginine methyltransferases (PRMT) with antitumor activity. Synonyms: EPZ019997 3HCl. CAS No. 2227587-26-8. Molecular formula: C20H41Cl3N4O2. Mole weight: 475.92. | |
| GSK3368715 dihydrochloride | GSK3368715 dihydrochloride is a reversible, orally active and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor with IC50s of 3.1, 48, 1148, 5.7 and 1.7 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively. It can change the methylation states of arginine, alter the use of exons, and has strong anticancer activity. Synonyms: EPZ019997 dihydrochloride; N-({3-[4,4-Bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl}methyl)-N,N'-dimethyl-1,2-ethanediamine dihydrochloride; 1,2-Ethanediamine, N1-[[3-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N1,N2-dimethyl-, hydrochloride (1:2). Grade: ≥95%. CAS No. 1628925-77-8. Molecular formula: C20H40Cl2N4O2. Mole weight: 439.46. | |
| 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. Grade: 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. Grade: 98%. CAS No. 869499-38-7. Molecular formula: C22H19ClNNaO3. Mole weight: 403.83. | |
| GSK-356278 | GSK-356278 is a selective Type 4 cyclic nucleotide phosphodiesterase inhibitor. It shows anxiolytic and cognition-enhancing effects and it has the ability to elevate cAMP in various cell types of the central nervous system. No development was reported for phase-I development in Major depressive disorder and Huntington's-disease. Uses: Huntington's disease; major depressive disorder. Synonyms: GSK-356278; GSK356278; GSK 356278; 5-(5-((2,4-dimethyl-5-thiazolyl)methyl)-1,3,4-oxadiazol-2-yl)-1-ethyl-n-(tetrahydro-2H-pyran-4-yl)-1H-Pyrazolo(3,4-b)pyridin-4-amine. Grade: 98%. CAS No. 720704-34-7. Molecular formula: C21H25N7O2S. Mole weight: 439.54. | |
| GSK3685032 | GSK3685032 is a non-time-dependent, non-covalent, first-in-class reversible and selective inhibitor of DNMT1, with IC50 of 0.036 μM. GSK3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition. Synonyms: GSK-3685032; GSK 3685032. CAS No. 2170137-61-6. Molecular formula: C22H24N6OS. Mole weight: 420.53. | |
| 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. | |
| GSK376501A | GSK376501A is a bio-active chemical compound used for the treatment of type 2 diabetes and hypercholesterolemia. It was developed by GlaxoSmithKline and was once in clinic phase 1, but now it has been terminated. Uses: Gsk376501a is used for the treatment of type 2 diabetes and hypercholesterolemia. Synonyms: GSK-376501A; GSK376501; GSK-376501; 1-[[3,5-bis(2-methoxyethoxy)phenyl]methyl]-3-(4-tert-butylphenyl)indole-2-carboxylic acid; 1H-Indole-2-carboxylic acid, 1-((3,5-bis(2-methoxyethoxy)phenyl)methyl)-3-(4-(1,1-dimethylethyl)phenyl)-. Grade: >98 %. CAS No. 1010412-80-2. Molecular formula: C32H37NO6. Mole weight: 531.64. | |
| GSK-3787 | GSK-3787 is a potent and selective ligand for PPARdelta with good pharmacokinetic properties. Synonyms: GSK-3787; GSK3787; GSK 3787. CAS No. 188591-46-0. Molecular formula: C15H12ClF3N2O3S. Mole weight: 392.78059. | |
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