产品名称

GSK 2982772

产品货号

Axon 2713 CAS [1622848-92-3] MF C20H19N5O3MW 377.40 Purity: 99% Optical purity: Optically pure Soluble in DMSO Description GSK2982772 potently binds to RIP1 with exquisite kinase specificity (IC50 value of 1.0 nM; ADP-Glo activity assay) and has excellent activity in blocking many TNF-dependent cellular responses (IC50 value of 6.3 nM; human monocytic U937 cellular assay). The inhibitor was also able to reduce spontaneous production of cytokines from human ulcerative colitis explants. First-in-class RIP1 inhibitor to enter clinical trials for psoriasis, rheumatoid arthritis, and ulcerative colitis. KEYWORDS: GSK 2982772 | supplier | RIP1 inhibitor | GSK-2982772 | GSK2982772 | CAS [1622848-92-3] | Non Selective (Phosphorylation Substrates) | RIP | Inhibitor | Enzymes

产品价格

现货询价，电话：010-67529703

产品规格

产品品牌

axonmedchem

产品概述

产品详情

GSK 2982772

Based on 1 reference(s) in Google Scholar 8 10 1

Axon 2713

CAS [1622848-92-3]

MF C20H19N5O3
MW 377.40

Purity: 99%
Optical purity: Optically pure
Soluble in DMSO

GSK 2982772

Description

GSK2982772 potently binds to RIP1 with exquisite kinase specificity (IC50 value of 1.0 nM; ADP-Glo activity assay) and has excellent activity in blocking many TNF-dependent cellular responses (IC50 value of 6.3 nM; human monocytic U937 cellular assay). The inhibitor was also able to reduce spontaneous production of cytokines from human ulcerative colitis explants. First-in-class RIP1 inhibitor to enter clinical trials for psoriasis, rheumatoid arthritis, and ulcerative colitis.

PA Harris et al. Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J Med Chem. 2017 Feb 23;60(4):1247-1261.

Specific inhibitor of RIP1 kinase

Chemical name

(S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-1H-1,2,4-triazole-3-carboxamide

Parent CAS No.

[1622848-92-3]

产品资料