GSK2982772

GSK2982772 is an inhibitor of receptor interacting serine/threonine kinase 1 (RIPK1, IC50s = 16 and 2,500 nM for the human and mouse enzymes, respectively). It is greater than 10,000-fold selective for RIPK1 over a panel of 339 kinases at 10 µM. GSK2982772 inhibits necrotic cell death induced by a combination of TNF-alpha and the caspase inhibitor QVD-OPh in U937 human monocytic and L929 murine fibrosarcoma cells (IC50s = 6.3 and 1,300 nM, respectively). GSK2982772 (3-300 nM) decreases IL-1beta and IL-6 levels in intestinal mucosa tissue isolated from patients with ulcerative colitis. It increases survival in a mouse model of TNF-alpha-induced lethal shock when administered at doses of 3, 10, and 50 mg/kg.Formal Name: 3-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-5-carboxamide. CAS Number: 1622848-92-3. Molecular Formula: C20H19N5O3. Formula Weight: 377.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10mg/mL, DMSO: 15mg/mL, DMSO:PBS (pH 7.2) (1:5): 0.16mg/mL, Ethanol: 5mg/mL. SMILES: CN1C2=CC=CC=C2OC[C@H](NC(C3=NN=C(CC4=CC=CC=C4)N3)=O)C1=O. InChi Code: InChI=1S/C20H19N5O3/c1-25-15-9-5-6-10-16(15)28-12-14(20(25)27)21-19(26)18-22-17(23-24-18)11-13-7-3-2-4-8-13/h2-10,14H,11-12H2,1H3,(H,21,26)(H,22,23,24)/t14-/m0/s1. InChi Key: LYPAFUINURXJSG-AWEZNQCLSA-N.