产品描述:
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).{49425} 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-α 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-1β and IL-6 levels in intestinal mucosa tissue isolated from patients with ulcerative colitis. It increases survival in a mouse model of TNF-α-induced lethal shock when administered at doses of 3, 10, and 50 mg/kg.