BOC Sciences provides a wide range of research chemicals and biochemicals including inhibitors, building blocks, GMP Products, impurities and metabolites, APIs for Veterinary, Natural Compounds, ADCs, Stem Cell Molecule and chiral compounds.
| Product | Description | |
|---|---|---|
| GRL0617 | GRL0617 is a potent and selective inhibitor of the protease enzyme papain-like protease (PLpro) with IC50 of 0.6 μM and Ki of 0.49 μM. It has been shown to inhibit SARS-CoV viral replication in vitro. Synonyms: GRL-0617; GRL 0617. Grade: 95%. CAS No. 1093070-16-6. Molecular formula: C20H20N2O. Mole weight: 304.39. |  |
| GRL-117C | GRL-117C is a CCR5 inhibitor that can inhibit the replication of wild-type R5-HIV-1. Synonyms: (4-Nitrophenyl)Methyl N-Allyl-N-[8-[4-[Benzenesulfonyl(Methyl)Amino]-3-Methyl-3-Phenyl-Butyl]-8-Azabicyclo[3.2.1]Octan-3-Yl]Carbamate; GRL117C; GRL 117C. Molecular formula: C36H44N4O6S. Mole weight: 660.8. | |
| Grp94 Inhibitor-1 | Grp94 Inhibitor-1 is a potent and selective inhibitor of Grp94 (IC50 = 2 nM), and over 1000-fold selectivity to Grp94 against Hsp90α. Synonyms: [1,1'-Biphenyl]-3-carboxamide, 4-[(trans-4-hydroxycyclohexyl)amino]-4'-(1-methylethyl)-; 4-[(trans-4-Hydroxycyclohexyl)amino]-4'-isopropyl-3-biphenylcarboxamide; rel-4-(((1R,4R)-4-hydroxycyclohexyl)amino)-4'-isopropyl-[1,1'-biphenyl]-3-carboxamide. Grade: ≥98%. CAS No. 2234897-35-7. Molecular formula: C22H28N2O2. Mole weight: 352.47. | |
| GRP (porcine) | GRP (porcine) is a mammalian bombesin-like peptide neurotransmitter that acts as an agonist for the gastrin-releasing peptide receptor (GRPR). It was shown to activate GABAergic interneurons in the amygdala resulting in an increase in GABA release and fear suppression in mice in vivo. Synonyms: Gastrin Releasing Peptide porcine. CAS No. 74815-57-9. Molecular formula: C126H198N38O31S2. Mole weight: 2805.31. | |
| GS 143 | GS 143 is a β-TrCP1 ligase inhibitor. GS 143 exhibits inhibitory effects on IκBα ubiquitination (IC50 = 5.2 μM), LPS-induced expression of inflammatory cytokines in human myelomonocytic cells, antigen-induced NFκB expression, inflammation and mucus production in airways of OVA-sensitized mice. Synonyms: GS-143; GS 143; GS143; 4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid. Grade: ≥98% by HPLC. CAS No. 916232-21-8. Molecular formula: C28H19FN2O4. Mole weight: 466.46. | |
| GS-283 | GS-283, an isoquinolin derivative, has been found to be histamine receptor and muscarinic receptor blocker. Synonyms: GS 283; GS-283; GS283; 6,7-Isoquinolinediol, 3,4-dihydro-1-((4-methoxyphenyl)methyl)-; 7-hydroxy-1-[(4-methoxyphenyl)methyl]-3,4-dihydro-2H-isoquinolin-6-one. Grade: 98%. CAS No. 149440-36-8. Molecular formula: C17H17NO3. Mole weight: 283.33. | |
| GS 389 | GS 389 is a novel tetrahydroisoquinoline analog which significantly increased cGMP levels in the rat aorta and inhibited cGMP phosphodiesterase from the rabbit brain. Uses: A novel tetrahydroisoquinoline analog. Synonyms: GS 389; GS-389; GS389. 6,7-dimethoxy-1-[(4-methoxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinoline. Grade: ≥98%. CAS No. 41498-37-7. Molecular formula: C19H23NO3. Mole weight: 313.39. | |
| GS 39783 | GS 39783 is an allosteric positive modulator of GABAB receptors, decreases cocaine self-administration, blocks the rewarding properties of nicotine and produces anxiolytic-like activity without the side effects associated with baclofen or benzodiazepines. Uses: Positive allosteric modulator of gabab receptor function. Synonyms: GS39783; GS-39783; GS 39783; N,N'-Dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine; 4-N,6-N-dicyclopentyl-2-methylsulfanyl-5-nitropyrimidine-4,6-diamine. Grade: ≥98%. CAS No. 39069-52-8. Molecular formula: C15H23N5O2S. Mole weight: 337.44. | |
| GS-441524 | GS-441524 is an analog nucleotide inhibitor against feline infectious peritonitis virus (FIPV). EC50 is 0.78?uM. GS-441524 is also a metabolite and intermediate of Remdesivir. Synonyms: 2-C-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-2,5-anhydro-D-altrononitrile; Remdesivir metabolite GS-441524; GS 441524; GS441524; (2R,3R,4S,5R)-2-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile. Grade: 97%. CAS No. 1191237-69-0. Molecular formula: C12H13N5O4. Mole weight: 291.26. | |
| GS-443902 | GS-443902 is a potent inhibitor of viral RNA-dependent RNA-polymerases (RdRp), with IC50s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. Uses: Antiviral agents. Synonyms: GS-441524 triphosphate; Remdesivir metabolite; RDV-TP. Grade: 99.87%. CAS No. 1355149-45-9. Molecular formula: C12H16N5O13P3. Mole weight: 531.20. | |
| GS-443902 trisodium | GS-443902 trisodium is a potent inhibitor of viral RNA-dependent RNA-polymerases (RdRp), with IC50s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. Synonyms: GS-441524 triphosphate trisodium; Remdesivir metabolite trisodium. Grade: 99%. CAS No. 1355050-21-3. Molecular formula: C12H12N5Na4O13P3. Mole weight: 619.13. | |
| GS-444217 | GS-444217 is an orally available and ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with IC50 of 2.87 nM. Synonyms: ASK1-IN-1. CAS No. 1262041-49-5. Molecular formula: C23H21N7O. Mole weight: 411.46. | |
| GS 6201 | GS 6201 is a selective A2B antagonist. Synonyms: CVT6883; CVT 6883; CVT-6883; GS6201; GS-6201; GS 6201; 3-Ethyl-3,9-dihydro-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-4-yl]-1H-purine-2,6-dione. CAS No. 752222-83-6. Molecular formula: C21H21F3N6O2. Mole weight: 446.43. | |
| GS-621763 | GS-621763 is an orally bioavailable prodrug of GS-441524. The nucleoside metabolite of remdesivir, GS-441524 displays potent anti-SARS-CoV-2 efficacy, and is being evaluated in clinical as an oral antiviral therapeutic for COVID-19. Synonyms: GS-441524 prodrug. Grade: 98%. CAS No. 2647442-13-3. Molecular formula: C24H31N5O7. Mole weight: 501.53. | |
| GS-7340 fumarate | Tenofovir alafenamide fumarate, also known as Tenofovir alafenamide hemifumarate; TAF, GS-7340, is a nucleotide reverse transcriptase inhibitor and a novel prodrug of tenofovir. It is under development by Gilead Sciences for use in the treatment of HIV infection. Closely related to the commonly used reverse-transcriptase inhibitor tenofovir disoproxil fumarate (Viread), Tenofovir alafenamide has greater antiviral activity and better distribution into lymphoid tissues than that agent. Gilead has announced a phase 3 clinical trial evaluating a single-tablet regimen combining GS-7340 with cobicistat, emtricitabine and elvitegravir and plans to coformulate the drug with cobicistat, emtricitabine and the protease inhibitor darunavir. In a 48 week study comparing Elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate to elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide fumarate, the results showed the prodrug to be non inferior to the established agent, but at much lower dosages and with lower incidence of adverse side effects such as impaired kidney function. Synonyms: GS-7340 fumarate; GS 7340 fumarate; GS7340 fumarate; (S)-isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate fumarate; TAF; GS734; GS-734; GS 7340; Tenofovir alafenamide fumarate; trade name: Genvoya. Grade: >98%. CAS No. 379270-38-9. Molecular formula: C25H33N6O9P. Mole weight: 59 | |
| GS-9219 | GS-9219 is a prodrug of the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)guanine (PMEG) with potential antineoplastic activity. Formulated to selectively accumulate in lymphocytes, nucleotide analogue GS 9219 is converted to its active metabolite, PMEG diphosphate (PMEGpp), via enzymatic hydrolysis, deamination, and phosphorylation; subsequently, PMEGpp is incorporated into nascent DNA chains by DNA polymerases, which may result in the termination of DNA synthesis, S-phase cell cycle arrest, and the induction of apoptosis in susceptible lymphoma cell populations. Synonyms: GS 9219; GS9219. CAS No. 859209-74-8. Molecular formula: C21H35N8O6P. Mole weight: 526.53. | |
| GS 9620 | GS 9620 is a potent and oral agonist of TLR7. Uses: Antiviral agents. Synonyms: 4-amino-2-butoxy-8-[[3-(pyrrolidin-1-ylmethyl)phenyl]methyl]-5,7-dihydropteridin-6-one; GS-9620; GS9620; Vesatolimod. Grade: 99.90%. CAS No. 1228585-88-3. Molecular formula: C22H30N6O2. Mole weight: 410.51. | |
| GS9667 | GS9667 is a new selective, partial agonist of the A(1) adenosine receptor (AR). It may be an effective therapy for Type 2 diabetes and dyslipidemia via lowering of free fatty acids (FFA). It was developed by Gilead and was in clinic phase 1 trials without progress. Uses: Gs966 may be an effective therapy for type 2 diabetes and dyslipidemia via lowering of free fatty acids (ffa). Synonyms: GS-9667; GS 9667; CVT-3619; CVT 3619; CVT3619. Grade: 98%. CAS No. 618380-90-8. Molecular formula: C21H24FN5O4S. Mole weight: 461.51. | |
| GS967 | GS967, also known as GS-458967, is a highly selective late sodium channel current blocker. The selective inhibition of late INa with GS967 can exert antiarrhythmic effects by suppressing EAD- and DAD-mediated extrasystolic activity in PFs and PV and SVC sleeve preparations. Synonyms: GS967; GS-967; GS 967; GS458967; GS 458967; GS-458967. Grade: 95%. CAS No. 1262618-39-2. Molecular formula: C14H7F6N3O. Mole weight: 347.22. | |
| GS-9822 | GS-9822 is one of novel non-catalytic site integrase inhibitors (NCINIs), which is a potential class of antiretroviral (ARV) agents. GS-9822 exhibits a potent effect against the T174I mutant (EC50: 3.0 ± 0.9 nM) and IN polymorphic variants (fold shift: 0.4 to 1.3). Studies showed that it has excellent pharmacokinetic properties and metabolic stability. Uses: Antiretroviral (arv) agent. Synonyms: 2219362-41-9; GS-9822; (S)-2-(tert-Butoxy)-2-(7-(4-chlorophenyl)-5-methyl-2-(1-methyl-3-(1-(oxetan-3-yl)piperidin-4-yl)-1H-indazol-5-yl)benzo[d]thiazol-6-yl)acetic acid; SCHEMBL20030699; DA-63908; HY-122229; CS-0082907; (2S)-2-tert-butoxy-2-[7-(4-chlorophenyl)-5-methyl-2-[1-methyl-3-[1-(oxetan-3-yl)-4-piperidyl]indazol-5-yl]-1,3-benzothiazol-6-yl]acetic acid. CAS No. 2219362-41-9. Molecular formula: C10H13N5O3. Mole weight: 251.24. | |
| GSA 10 | GSA 10 is a quinolinecarboxamide derivative that acts as a Smoothened/Smo receptor agonist (EC50 = 1.2 μM). GSA 10 can promote differentiation of multipotent mesenchymal progenitor cells into osteoblasts. Uses: Smoothened (smo) receptor agonist. Synonyms: GSA-10; propyl 4-[(1-hexyl-4-hydroxy-2-oxoquinoline-3-carbonyl)amino]benzoate. Grade: >98%. CAS No. 300833-95-8. Molecular formula: C26H30N2O5. Mole weight: 450.53. | |
| GS-CA-1 | GS-CA-1 is a novel HIV capsid inhibitor developed by Gilead, which is a promisingly long-acting antiretroviral (ARV) agent. The preclinical study showed that GS-CA-1 could inhibit HIV-1 replication in human peripheral blood mononuclear cells (PBMCs) (EC50 = 140 pM). Uses: Long-acting antiretroviral (arv) agent. Synonyms: GS CA 1. Grade: 99.94%. CAS No. 2189684-45-3. Molecular formula: C41H36ClF8N7O5S2. Mole weight: 958.34. | |
| GSI-136 | GSI-136 is an amyloid precursor protein secretase inhibitor. Uses: Γ-secretase inhibitor. Synonyms: GSI-136; GSI 136; GSI136. (S)-5-chloro-N-(3-ethyl-1-hydroxypentan-2-yl)thiophene-2-sulfonamide. Grade: ≥98%. CAS No. 443989-01-3. Molecular formula: C11H18ClNO3S2. Mole weight: 311.83. | |
| GSK046 | GSK046 is a potent, selective and orally active inhibitor of BET with immunomodulatory activity. GSK046 reduces the recruitment of BET proteins to interferon (IFN) target genes following IFN-γ stimulation. Synonyms: iBET-BD2; GSK 046; GSK-046. CAS No. 2474876-09-8. Molecular formula: C23H27FN2O4. Mole weight: 414.47. | |
| GSK0660 | GSK0660 is a selective PPARδ antagonist. GSK0660 blocks the effect of TNFα on the expressions of cytokines involved in leukocyte recruitment, including CCL8, CCL17, and CXCL10, and it may block TNFα-induced retinal leukostasis. Synonyms: GSK0660; GSK-0660; GSK 0660. Grade: 96%. CAS No. 1014691-61-2. Molecular formula: C19H18N2O5S2. Mole weight: 418.48. | |
| GSK097 | GSK097, a potent and selective inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins, shows 2000-fold selectivity for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media. Synonyms: 2,4-Pyridinedicarboxamide, 6-[(S)-hydroxyphenylmethyl]-N2-methyl-N4-[(1S,2S)-2-methylcyclopropyl]-. CAS No. 2159137-02-5. Molecular formula: C19H21N3O3. Mole weight: 339.39. | |
| GSK-1014802 hydrochloride | GSK-1014802 hydrochloride is the hydrochloride form of GSK-1014802, which is a novel analgesic for the treatment of lumbosacral radiculopathy (sciatica) and trigeminal neuralgia. It acts as a selective, small-molecule, state-dependent Nav1.7 voltage-gated sodium channel blocker. It received orphan-drug designation from the US Food and Drug Administration in July 2013. It was developed by Convergence Pharmaceuticals. It is currently in phase II studies in bipolar depression. Uses: Gsk-1014802 hydrochloride is a novel analgesic for the treatment of lumbosacral radiculopathy (sciatica) and trigeminal neuralgia. it received orphan-drug designation from the us food and drug administration in july 2013. Synonyms: GSK-1014802 hydrochloride; GSK 1014802 hydrochloride; GSK1014802 hydrochloride; (2S,5R)-5-(4-((2-Fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide hydrochloride; (5R)-5-(4-{[(2-fluorophenyl)methyl]oxy}phenyl)-L-prolinamide hydrochlorideCNV1014802 hydrochloride; CNV-1014802 hydrochloride; Raxatrigine hydrochloride. Grade: >98%. CAS No. 934240-31-0. Molecular formula: C18H20ClFN2O2. Mole weight: 350.82. | |
| GSK1016790A | GSK1016790A is a novel and potent transient receptor potential vanilloid 4 (TRPV4) agonist. It has been used to demonstrate a role for TRPV4 in regulating urinary bladder activity and endothelial control of vascular tone. It elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells with EC50 values of 18 and 2.1 nM, respectively. It also evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM, which is 300 fold more potent than 4a-PDD. It was developed by GlaxoSmithKline. Uses: Gsk1016790a regulats urinary bladder activity and endothelial control of vascular tone. Synonyms: GSK1016790A; GSK-1016790A; GSK 1016790A. N-((S)-1-(4-((S)-2-(2,4-dichlorophenylsulfonaMido)-3-hydroxypropanoyl)piperazin-1-yl)-4-Methyl-1-oxopentan-2-yl)benzo[b]thiophene-2-carboxaMide. Grade: >98 %. CAS No. 942206-85-1. Molecular formula: C28H32Cl2N4O6S2. Mole weight: 655.61. | |
| GSK1059615 | GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. Synonyms: GSK-1059615; GSK 1059615; GSK1059615. Grade: >98%. CAS No. 958852-01-2. Molecular formula: C18H11N3O2S. Mole weight: 333.36. | |
| GSK106 hydrochloride | GSK106 is a useful inactive control for the selective PAD4 inhibitors GSK484 and GSK199. Synonyms: (3-amino-1-piperidinyl)[2-(1-ethyl-1H-indol-2-yl)-1-methyl-1H-benzimidazol-6-yl]-methanone, monohydrochloride. Grade: ≥98%. CAS No. 1652591-82-6. Molecular formula: C24H27N5O·HCl. Mole weight: 437.97. | |
| GSK-1070916A | GSK-1070916A is an ATP-competitive inhibitor of the serine/threonine kinases Aurora B and C with potential antineoplastic activity. Aurora B/C kinase inhibitor GSK1070916A binds to and inhibits the activity of Aurora kinases B and C, which may result in inhibition of cellular division and a decrease in the proliferation of tumor cells that overexpress the Aurora kinases B and C. Aurora kinases play essential roles in mitotic checkpoint control during mitosis, and are overexpressed by a wide variety of cancer cell types. Synonyms: GSK 1070916; GSK-1070916; GSK 1070916; GSK1070916A; GSK 1070916A; NMI-900; NMI 900; NMI900; N'-[4-[4-[2-[3-[(Dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethyl-1H-pyrazol-3-yl]phenyl]-N,N-dimethylurea. Grade: 98%. CAS No. 942918-07-2. Molecular formula: C30H33N7O. Mole weight: 507.63. | |
| GSK-1071306 | GSK-1071306 is one of the metabolites of pazopanib which is a inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity as a approved drug. Synonyms: GSK-1071306; GSK1071306; GSK 1071306; Pazopanib metabolite M27; 5-((4-((2,3-dimethyl-2H-indazol-6-yl)amino)-2-pyrimidinyl)amino)-2-methyl-Benzenesulfonamide. Grade: 98%. CAS No. 1252927-47-1. Molecular formula: C20H21N7O2S. Mole weight: 423.49. | |
| GSK-114 | GSK-114 is a selective TNNI3 Interacting Kinase (TNNI3K) inhibitor with IC50 of 25nM. GSK-114 shows significant bias for TNNI3K over B-Raf, exceptional broad spectrum kinase selectivity and adequate oral exposure to enable its use in cellular and in vivo studies. Ralated studies has shown that TNNI3 Interacting Kinase has been linked to the progression of dilated cardiomyopathy, cardiac hypertrophy, and ischemia/reperfusion injury using models that employ TNNI3K overexpressing or TNNI3K knockout animals. Synonyms: GSK-114; GSK 114; GSK114; 3-((6,7-dimethoxyquinazolin-4-yl)amino)-4-(dimethylamino)-N-methylbenzenesulfonamide; 1301760-19-9 (2HCl). Grade: 98%. CAS No. 1301761-96-5. Molecular formula: C19H23N5O4S. Mole weight: 417.48. | |
| GSK-114 2Hcl | GSK-114 is a potent and selective TNNI3K inhibitor (TNNI3 IC50 = 25nM; B-RafV600E IC50 = 1000 nM). GSK-114 displays significant bias (40-fold) for TNNI3K over B-Raf, exceptional broad spectrum kinase selectivity, and adequate oral exposure to enable its use in cellular and in vivo studies. Synonyms: GSK-114 2Hcl; GSK114 2Hcl; GSK 114 2Hcl. CAS No. 1301760-19-9. Molecular formula: C19H23N5O4S.2HCl. Mole weight: 495.484. | |
| GSK121 trifluoroacetate salt | GSK121 is an inhibitor for protein arginine deiminase 4 (PAD4), which has been shown to inhibit the citrullination of PAD4 target proteins in a functional assay with an IC50 value of 3.2 μM. Synonyms: (3-amino-1-piperidinyl)[1-methyl-2-(1-methyl-1H-indol-2-yl)-1H-benzimidazol-5-yl]-methanone, 2,2,2-trifluoroacetate. Grade: ≥98%. CAS No. 1652591-80-4. Molecular formula: C23H25N5O·CF3COOH. Mole weight: 501.5. | |
| GSK124576A | GSK124576A is a biochemical. Synonyms: N-Benzyl-2-(6-bromo-2-methyl-quinolin-4-yloxy)-acetamide; N-benzyl-2-(6-broMo-2-Methylquinolin-4-yloxy)acetamide; N-Benzyl-2-((6-bromo-2-methylquinolin-4-yl)oxy)acetamide. Grade: 98% by HPLC. CAS No. 1443139-14-7. Molecular formula: C19H17BrN2O2. Mole weight: 385.3. | |
| GSK126 | GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity. GSK126 decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice. Together, these data demonstrate that pharmacological inhibition of EZH2 activity may provide a promising treatment for EZH2 mutant lymphoma. Synonyms: GSK2816126; GSK-2816126; GSK 2816126; GSK-126; GSK 126; (S)-1-(sec-Butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide. Grade: 98%. CAS No. 1346574-57-9. Molecular formula: C31H38N6O2. Mole weight: 526.69. | |
| GSK-1268992 | GSK-1268992 is one of a metabolite of Pazopanib which is a selective multi-targeted receptor tyrosine kinase inhibitor that blocks tumour growth and inhibits angiogenesis. Synonyms: GSK-1268992; GSK1268992; GSK 1268992; Pazopanib metabolite M24; 5-((4-((3-(Hydroxymethyl)-2-methyl-indazol-6-yl)-methyl-amino)pyrimidin-2-yl)amino)-2-methyl-benzenesulfonamide. Grade: 98%. CAS No. 1414375-49-7. Molecular formula: C21H23N7O3S. Mole weight: 453.52. | |
| GSK-1268997 | GSK-1268997 is one of a metabolite of Pazopanib which is a selective multi-targeted receptor tyrosine kinase inhibitor that blocks tumour growth and inhibits angiogenesis. Synonyms: GSK-1268997; GSK1268997; GSK 1268997; Pazopanib metabolite M26; 5-((4-((2,3-Dimethylindazol-6-yl)-methyl-amino)pyrimidin-2-yl)amino)-2-(hydroxymethyl)benzenesulfonamide. Grade: 98%. CAS No. 1414375-50-0. Molecular formula: C21H23N7O3S. Mole weight: 453.52. | |
| GSK-1292263 | GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes. Synonyms: GSK1292263; GSK 1292263l; GSK-1292263. Grade: 0.98. CAS No. 1032823-75-8. Molecular formula: C23H28N4O4S. Mole weight: 456.561. | |
| GSK1324726A | GSK1324726A is a novel, potent and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50 = 41 nM), BRD3 (IC50 = 31 nM), and BRD4 (IC50 = 22 nM). Synonyms: I-BET-726; I-BET 726; I-BET726; GSK-1324726A; GSK 1324726A. Grade: >98%. CAS No. 1300031-52-0. Molecular formula: C25H23ClN2O3. Mole weight: 434.91. | |
| GSK137647A | GSK137647A, a diarylsulfonamide, is an agonist of the free fatty acid receptor 4 [GPR120 (pEC50s = 6.3, 6.2, and 6.1 at human, mouse, and rat receptors, respectively)]. Uses: A selective ffa4 agonist. Synonyms: GSK137647A; GSK-137647A; GSK 137647A; GSK137647; GSK-137647; GSK 137647; 4-methoxy-N-(2,4,6-trimethylphenyl)-benzenesulfonamide. Grade: ≥98%. CAS No. 349085-82-1. Molecular formula: C16H19NO3S. Mole weight: 305.4. | |
| GSK143 | GSK143 is a selective SYK inhibitor, which abrogates survival signals in chronic lymphocytic leukaemia. Synonyms: 2-{[(3r,4r)-3-Aminotetrahydro-2h-Pyran-4-Yl]amino}-4-[(4-Methylphenyl)amino]pyrimidine-5-Carboxamide. CAS No. 1240390-27-5. Molecular formula: C17H22N6O2. Mole weight: 342.40. | |
| GSK143 dihydrochloride | GSK143 dihydrochloride is a highly selective SYK inhibitor, which abrogates survival signals in chronic lymphocytic leukaemia. Synonyms: GSK143 (dihydrochloride). Grade: 98%. CAS No. 2341796-81-2. Molecular formula: C17H24Cl2N6O2. Mole weight: 415.32. | |
| GSK-1440115 | GSK-1440115 is an orally active urotensin II receptor antagonist. It is used for the treatment of asthma. Uses: Gsk-1440115 is used for the treatment of asthma. Synonyms: GSK 1440115; GSK-1440115; GSK1440115. 4'-(1-(((6,7-Dichloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetyl)(methyl)amino)-2-(4-morpholinyl)ethyl)-4-diphenylcarboxylic acid; 4-[4-[(1R)-1-[[2-(6,7-dichloro-3-oxo-1,4-benzoxazin-4-yl)acetyl]-methylamino]-2-morpholin-4-ylethyl]phenyl]benzoic acid. Grade: >98 %. CAS No. 1003878-16-7. Molecular formula: C30H29Cl2N3O6. Mole weight: 598.47. | |
| GSK1521498 | GSK-1521498 is a novel μ-Opioid receptor antagonist. It shows to attenuate reward-driven compulsive behaviours, such as stimulant drug seeking or binge eating in animals and humans. It is mainly used for the treatment of obesity and alcohol dependence. It was developed by GlaxoSmithKline and in clinic phase 2. Uses: Gsk-1521498 is mainly used for the treatment of obesity and alcohol dependence. Synonyms: GSK-1521498; GSK1521498; GSK 1521498; GSK-1521498B; N-[[2,6-difluoro-4-[3-(1H-1,2,4-triazol-5-yl)phenyl]phenyl]methyl]-2,3-dihydro-1H-inden-2-amine; N-((3,5-difluoro-3'-(1H-1,2,4-triazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-2,3-dihydro-1H-inden-2-amine. Grade: >98 %. CAS No. 1007573-18-3. Molecular formula: C24H20F2N4. Mole weight: 402.44. | |
| GSK1521498 free base (hydrochloride) | GSK1521498 free base (hydrochloride) is a selective μ-opioid receptor (MOR) antagonist. It is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs. Synonyms: GSK1521498 hydrochloride. CAS No. 1007578-24-6. Molecular formula: C24H21ClF2N4. Mole weight: 438.90. | |
| GSK 1562590 hydrochloride | GSK 1562590 hydrochloride is a high affinity and selective urotensin II (UT) receptor antagonist (pKi = 9.14, 9.28, 9.34, 9.64 and 9.66 at monkey, human, mouse, cat and rat recombinant receptors, respectively). It displays selectivity for UT receptors over a range of GPCRs, ion channels, enzymes and neurotransmitter transporters. GSK 1562590 has been shown to inhibit human urotensin-II (hU-II)-induced contraction of isolated rat aorta in vitro and ex vivo. Synonyms: GSK 1562590 hydrochloride; GSK1562590 hydrochloride; GSK-1562590 hydrochloride; N-[(1R)-1-[3'-(Aminocarbonyl)[1,1'-biphenyl]-4-yl]-2-(1-pyrrolidinyl)ethyl]-6,7-dichloro-2,3-dihydro-N-methyl-3-oxo-4H-1,4-benzoxazine-4-acetamide hydrochloride; 3-[4-[(1R)-1-[[2-(6,7-dichloro-3-oxo-1,4-benzoxazin-4-yl)acetyl]-methylamino]-2-pyrrolidin-1-ylethyl]phenyl]benzamide hydrochloride. Grade: ≥98% by HPLC. CAS No. 1003878-07-6. Molecular formula: C30H30Cl2N4O4.HCl. Mole weight: 617.95. | |
| GSK163090 | GSK163090 is Potent, selective, and orally active 5-HT1A/B/D receptor antagonist. Synonyms: 1-(3-(2-(4-(2-methylquinolin-5-yl)piperazin-1-yl)ethyl)phenyl)imidazolidin-2-one; GSK163090; GSK-163090; GSK 163090. Grade: 98%. CAS No. 844903-58-8. Molecular formula: C25H29N5O. Mole weight: 415.54. | |
| GSK 1702934A | GSK 1702934A is a potent and selective TRPC3/6 activator (EC50 = 80 and 440 nM for TRPC3 and 6, respectively). However, it exhibits no activity at TRPV4, TRPA1, M1, M4, CaV1.2, hERG, NaV1.5, or CXCR5 receptors at concentrations <10 μM. Synonyms: 1,3-Dihydro-1-[1-[(5,6,7,8-tetrahydro-4H-cyclohepta[b]thien-2-yl)carbonyl]-4-piperidinyl]-2H-benzimidazol-2-one; 3-[1-(5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-2-carbonyl)piperidin-4-yl]-1H-benzimidazol-2-one; GSK-2934A. Grade: ≥98% by HPLC. CAS No. 924377-85-5. Molecular formula: C22H25N3O2S. Mole weight: 395.52. | |
| GSK172981 | This molecular is a novel non-peptide tachykinin NK3 receptor antagonist and it has a very high affinity for native guinea pig (pK(I) value 7.8) tachykinin NK(3) receptors and recombinant human (pK(I) value 7.7). Meanwhile, GSK172981 also exhibited a competitive profile in antagonizing neurokinin B-stimulated neuronal activity recorded from the guinea pig medial habenula slices (apparent pK(B)=8.1). In the near future, this active molecular may be promising drug candidate in the treatment of schizophrenia. Uses: Treatment of schizophrenia. Synonyms: GSK172981; GSK-172981; GSK 172981. (S)-3-amino-N-(cyclopropyl(phenyl)methyl)-2-(3-fluorophenyl)quinoline-4-carboxamide. Grade: 98%. CAS No. 1133705-99-3. Molecular formula: C26H22FN3O. Mole weight: 411.48. | |
| GSK180736A | GSK180736A is a potent and selective inhibitor of GRK2 (IC50 = 0.77 μM) and ROCK1 (IC50 = 14 nM). Synonyms: GSK-180736A; 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-3,4-dihydro-1H-pyrimidine-5-carboxamide. Grade: >98%. CAS No. 817194-38-0. Molecular formula: C19H16FN5O2. Mole weight: 365.37. | |
| GSK1838705A | GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and IR (insulin receptor) with IC50s of 2.0 and 1.6 nM, respectively. GSK1838705A blocks the in vitro proliferation of cell lines derived from solid and hematologic malignancies, including multiple myeloma and Ewing's sarcoma, and retards the growth of human tumor xenografts in vivo. Despite the inhibitory effect of GSK1838705A on insulin receptor, minimal effects on glucose homeostasis were observed at efficacious doses. GSK1838705A also inhibits the anaplastic lymphoma kinase (ALK), which drives the aberrant growth of anaplastic large-cell lymphomas, some neuroblastomas, and a subset of non-small cell lung cancers. GSK1838705A inhibits ALK, with an IC(50) of 0.5 nmol/L, and causes complete regression of ALK-dependent tumors in vivo at well-tolerated doses. GSK1838705A is therefore a promising antitumor agent for therapeutic use in human cancers. Synonyms: GSK1838705A; GSK-1838705A; GSK-1838705A. Grade: 0.98. CAS No. 1116235-97-2. Molecular formula: C27H29FN8O3. Mole weight: 532.57. | |
| GSK1842799 | GSK1842799 is a selective S1P1 receptor agonist for multiple sclerosis. It showed subnanomole S1P1 agonist activity with >1000× selectivity over S1P3 upon phosphorylation. It has good oral bioavailability. It was selected as a candidate for further clinical on the basis of the favorable in vitro ADME and in vivo PK/PD properties as well as broad toxicology evaluations. Uses: Gsk1842799 was selected as a candidate for further clinical. Synonyms: (S)-2-amino-2-(5-(4-(octyloxy)-3-(trifluoromethyl)phenyl)-1,3,4-thiadiazol-2-yl)propan-1-ol; GSK1842799; GSK 1842799; GSK 1842799. Grade: >98 %. CAS No. 1005407-76-0. Molecular formula: C20H28F3N3O2S. Mole weight: 431.52. | |
| GSK 189254A | GSK-189,254 is a H3 histamine receptor inverse agonist. It has subnanomolar affinity for the H3 receptor with Ki of 0.2nM. It possesses stimulant and nootropic effects and analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord. No development was reported about Phase-II clinical trials for Narcolepsy in Europe. Uses: Narcolepsy. Synonyms: 6-((3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-N-methyl-3-Pyridinecarboxamide. Grade: 98%. CAS No. 720690-73-3. Molecular formula: C21H25N3O2. Mole weight: 351.44. | |
| GSK-189254 hydrochloride | GSK-189,254 is a potent and selective H3-receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H3 receptor (Ki 0.2nM) and selectivity of over 10,000x for H3 over other histamine receptor subtypes.Animal studies have shown it to possess not only stimulant and nootropic effects, but also analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord. GSK-189,254 and several other related drugs are currently being investigated as a treatment for Alzheimer's disease and other forms of dementia, as well as possible use in the treatment of conditions such as narcolepsy, or neuropathic pain which do not respond well to conventional analgesic drugs. Synonyms: GSK189254; GSK-189254; GSK-189,254. CAS No. 945493-87-8. Molecular formula: C21H26ClN3O2. Mole weight: 387.91. | |
| GSK-1904529a | GSK-1904529A is an IGF-1R Inhibitor, is is a promising candidate for therapeutic use in IGF-IR-dependent tumors. GSK1904529A selectively inhibits IGF-IR and IR with IC50s of 27 and 25 nmol/L, respectively. GSK1904529A blocks receptor autophosphorylation and downstream signaling, leading to cell cycle arrest. It inhibits the proliferation of cell lines derived from solid and hematologic malignancies, with multiple myeloma and Ewing's sarcoma cell lines being most sensitive. Oral administration of GSK1904529A decreases the growth of human tumor xenografts in mice, consistent with a reduction of IGF-IR phosphorylation in tumors. Despite the potent inhibitory activity of GSK1904529A on IR in vitro and in vivo, minimal effects on blood glucose levels are observed in animals at doses that show significant antitumor activity. Synonyms: GSK 4529; GSK4529; GSK-4529; GSK1904529a; GSK 1904529; GSK-1904529a. CAS No. 1089283-49-7. Molecular formula: C44H47F2N9O5S. Mole weight: 851.975. | |
| GSK1997132B | PPARγ is a ligand-activated nuclear receptor and was reported to plays a role in energy metabolism, glucose homeostasis and microglia-mediated neuroinflammation. GSK1997132B is a metabolically stable, highly potent centrally penetrant PPARγ partial agonist. Synonyms: GSK 1997132B; GSK-1997132B; GSK1997132B; GSK1997132; GSK-1997132; GSK 1997132. (R)-1-((3,5-difluoropyridin-2-yl)methyl)-2-methyl-N-(1-phenylpropyl)-1H-benzo[d]imidazole-5-carboxamide. Grade: 98%. CAS No. 1168138-37-1. Molecular formula: C24H22F2N4O. Mole weight: 420.46. | |
| GSK199 hydrochloride | GSK199 is a potent and reversible inhibitor of PAD4 with an IC50 value of 200 nM) which is less potent than the related PAD4 inhibitor GSK484 (IC50 = 50 nM). Synonyms: [(3R)-3-amino-1-piperidinyl][2-(1-ethyl-1H-pyrrolo[2,3-b]pyridin-2-yl)-7-methoxy-1-methyl-1H-benzimidazol-5-yl]-methanone, monohydrochloride. Grade: ≥98%. CAS No. 1549811-53-1. Molecular formula: C24H28N6O2·HCl. Mole weight: 469. | |
| GSK-2018682 | GSK-2018682 is a potent and selective agonist of sphingosine-1-phosphate receptor (S1PR) subtype 1 that has the potential to treat multiple sclerosis (MS). Synonyms: GSK2018682; GSK 2018682; GSK-2018682. UNII-NJL503AIJA; NJL503AIJA; 4-(4-(5-(5-chloro-6-isopropoxypyridin-3-yl)-1,2,4-oxadiazol-3-yl)-1H-indol-1-yl)butanoic acid. Grade: ≥98%. CAS No. 1034688-30-6. Molecular formula: C22H21ClN4O4. Mole weight: 440.884. | |
| GSK-2033 | This active molecular is a cell permeable, potent LXR (liver-X-receptor) antagonist. pIC50 values is 7.0 for LXRα and 7.4 for LXRβ. GSK2033 enhances T-cell proliferation and Th1/Th2/Th17 differentiation when treatment of murine CD41 T cells. Synonyms: GSK-2033; GSK2033; GSK 2033; CHEMBL1093266; GTPL8690; SCHEMBL13280409; 2,4,6-trimethyl-N-[[4-(3-methylsulfonylphenyl)phenyl]methyl]-N-[[5-(trifluoromethyl)furan-2-yl]methyl]benzenesulfonamide. Grade: 98%. CAS No. 1221277-90-2. Molecular formula: C29H28F3NO5S2. Mole weight: 591.66. | |
| GSK205 | GSK205 is a potent and selective antagonist of TRPV4 with an IC50 of 4.19 μM for inhibiting TRPV4-mediated Ca2+ influx. Synonyms: N-(4-(2-(benzyl(methyl)amino)ethyl)phenyl)-5-(pyridin-3-yl)thiazol-2-amine hydrobromide; N-(4-{2-[Benzyl(methyl)amino]ethyl}phenyl)-5-(3-pyridinyl)-1,3-thiazol-2-amine hydrobromide (1:1); 2-Thiazolamine, N-[4-[2-[methyl(phenylmethyl)amino]ethyl]phenyl]-5-(3-pyridinyl)-, hydrobromide (1:1). Grade: ≥98%. CAS No. 1263068-83-2. Molecular formula: C24H25BrN4S. Mole weight: 481.45. | |
| GSK2110183 | GSK2110183 is an orally bioavailable pan-Akt inhibitor with IC50s of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively. Synonyms: GSK2110183; GSK 2110183; GSK-2110183. Grade: >98%. CAS No. 1047634-63-8. Molecular formula: C18H16Cl2F2N4OS. Mole weight: 445.31. | |
| GSK2110183 hydrochloride | GSK2110183 is an orally bioavailable pan-Akt inhibitor with IC50s of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively. Synonyms: Afuresertib-F HCl; GSK2110183 analog 1 (hydrochloride). Grade: 99%. CAS No. 2070009-64-0. Molecular formula: C18H17Cl3F2N4OS. Mole weight: 481.77. | |
| GSK2141795 hydrochloride | GSK2141795 Hcl is a potent and selective pan-Akt inhibitor with IC50s of 180/328/38 nM for Akt1/Akt2/Akt3 respectively. Synonyms: GSK-2141795 Hydrochloride; GSK 2141795 Hydrochloride; GSK2141795 Hydrochloride; GSK2141795 HCl; Uprosertib. Grade: >98%. CAS No. 1047635-80-2. Molecular formula: C18H17Cl3F2N4O2. Mole weight: 465.71. | |
| GSK215 | GSK215, a potent and selective PROTAC focal adhesion kinase (FAK) degrader, is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. It induces rapid and prolonged degradation of FAK, with a long-lasting effect on FAK levels and a significant disconnect in pharmacokinetic/pharmacodynamics (PK/PD). Synonyms: (2S,4R)-4-Hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-((4-((2-(methylcarbamoyl)phenyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide. Grade: ≥95%. CAS No. 2743427-26-9. Molecular formula: C50H59F3N10O6S. Mole weight: 985.13. | |
| GSK215083 | GSK215083 is a PET radioligand for the 5-hydroxytrypamine-6 (5HT6) receptor. It is a quinoline based compounds that acts by antagonising the 5-HT6 receptor. It binds to receptors 5HT6 in the striatum and 5-hydroxytryptamine-2A (5HT2A) in the frontal cortex. It is used for the treatment of Alzheimer's disease and used as a PET ligand for identification of occupancy of the 5HT6 receptor coupled with 11C. Uses: Gsk215083 is used for the treatment of alzheimer's disease and used as a pet ligand for identification of occupancy of the 5ht6 receptor coupled with 11c. Synonyms: GSK-215083; GSK 215083; GSK215083; 3-(3-Fluoro-benzenesulfonyl)-8-(4-Methyl-piperazin-1-yl)-quinoline; GSK-215083; Quinoline, 3-((3-fluorophenyl)sulfonyl)-8-(4-methyl-1-piperazinyl)-. Grade: 98%. CAS No. 607742-80-3. Molecular formula: C20H20FN3O2S. Mole weight: 385.46. | |
| GSK2190915 | GSK2190915 is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor. It exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. It also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model. It increased survival time in mice exposed to a lethal intravenous injection of platelet activating factor (PAF). Synonyms: AM-803; AM 803; AM803; 3Fiboflapon; GSK2190915; GSK 2190915; GSK-2190915. Grade: >98%. CAS No. 936350-00-4. Molecular formula: C38H43N3O4S. Mole weight: 637.83. | |
| GSK2190915 sodium salt | GSK2190915(AM-803; Fiboflapon) sodium salt is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM. Synonyms: GSK2190915 sodium salt; GSK 2190915 sodium salt; GSK-2190915 sodium salt; GSK-2190915A; GSK 2190915A; GSK2190915A; Fiboflapon sodium; AM-803 sodium; AM 803 sodium; AM803 sodium. Grade: >98%. CAS No. 1196070-26-4. Molecular formula: C38H42N3NaO4S. Mole weight: 659.81. | |
| GSK2193874 | GSK2193874 is a potent, orally active and specific antagonist of TRPV4 ion channels (IC50 values 2 and 40 nM for rat and human receptors, respectively). GSK2193874 is selective over a panel of ~200 human receptors, channels and enzymes. Synonyms: GSK2193874; GSK 2193874; GSK-2193874; GSK2193874A; GSK 2193874A; GSK-2193874A; 7-bromo-N-(1-phenylcyclopropyl)-3-[(4-piperidin-1-ylpiperidin-1-yl) methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide. CAS No. 1336960-13-4. Molecular formula: C37H38BrF3N4O. Mole weight: 691.62. | |
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