GSK-962

Description: GSK-962 (also known as GSK'962 or GSK962) is a negative control for GSK'963 (also known as GSK'963 or GSK963). GSK-963 is a potent and selective RIP1 kinase inhibitor. GSK'963 is significantly more potent than Nec-1 (a known RIP1 kinase inhibitor ) in both biochemical and cellular assays, inhibiting RIP1-dependent cell death with an IC50 of between 1 and 4?nM in human and murine cells. GSK'963 is > 10?000-fold selective for RIP1 over 339 other kinases, lacks measurable activity against IDO and has an inactive enantiomer, GSK'962, which can be used to confirm on-target effects. The increased in vitro potency of GSK'963 also translates in vivo, where GSK'963 provides much greater protection from hypothermia at matched doses to Nec-1, in a model of TNF-induced sterile shock. Together, we believe GSK'963 represents a next-generation tool for examining the function of RIP1 in vitro and in vivo, and should help to clarify our current understanding of the role of RIP1 in contributing to disease pathogenesis.

References: Cell Death Discov. 2015 Jul 27; 1:15009.

Related CAS #: 2049868-46-2 (GSK-963)