GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10\u2009000-fold selective for RIP1 over 339 other kinases.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of receptor interacting serine/threonine kinase 1
Product Description
Information
GSK'963 GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.
Targets
RIP1 kinase (Cell-free assay) 29 nM
In vitro
GSK\'963 inhibits RIP1-dependent cell death with an IC50 of between 1 and 4\u2009nM in human and murine cells.
In vivo
GSK\'963 is a potent inhibitor of a TNF+zVAD-mediated lethal shock. At 2\u2009mg/kg, GSK\'963 would maintain blood concentrations above the concentration required for 90% inhibition of RIP1 activity for an extended period of time compared with Nec-1.
J2213760