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