UH15-38

UH15-38 is an inhibitor of receptor-interacting serine/threonine kinase 3 (RIPK3, IC50 = 0. µM). It is selective for RIPK3 over a panel of 50 receptors and enzymes at 1 µM and a panel of 77 kinases at 0. µM but does inhibit RIPK1 (IC50 = 0. µM) and 13 other kinases by greater than 90% at 0. µM. UH15-38 inhibits LPS-induced necroptosis in RAW 264. macrophages and isolated mouse bone marrow-derived macrophages (BMDMs, IC50s = 17 and 22 nM, respectively) and TNF-alpha-induced necroptosis in recombinant human RIPK3-expressing HeLa cells, Fas-associated death domain protein knockout (FADD-/-) Jurkat cells, and U937 cells (IC50s = 722, 205, and 329 nM, respectively). In vivo, UH15-38 (30 mg/kg) increases survival, decreases lung injury and immune cell bronchoalveolar fluid (BALF) infiltration, and inhibits decreases in arterial oxygen saturation in a mouse model of severe influenza A infection.. Solulibility: DMSO: Soluble: =10 mg/ml: Ethanol: Sparingly soluble: 1-10 mg/ml.