GSK'872 (GSK2399872A)

InformationGSK'872 (GSK2399872A) GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.In vitroWhen assayed at 1 μM, GSK/'872 fails to inhibit most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase when tested directly. GSK/'872 blocks TNF-induced necroptosis in a concentration-dependent manner in HT-29 cells. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK/'872 also blocks necroptosis in primary human neutrophils isolated from whole blood. GSK/'872 inhibits TLR3- or DAI-induced death, two RIP1-independent pathways of necroptosis. It induces caspase activation followed by apoptotic cell death.In vivoGSK/'872 treatment significantly decreases HIF-1α expression compared with no treatment after ischemia injury in vivo.Cell Datacell lines：Concentrations：0.3, 1, 3 μMIncubation Time：18 hPowder Purity:≥99%. Specifications and Purity: 10mM in DMSO. Molecular Formula: C19H17N3O2S2. Molecular Weight: 383.49.