GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a K d of 9.3 μM. GW806742X has activity against VEGFR2 ( IC 50 =2 nM). GW806742X retards MLKL membrane translocation and inhibits necroptosis
In Vitro
GW806742X (0.1-10000 nM) inhibits necroptotic death of wild-type mouse dermal fibroblasts (MDFs) stimulated with TSQ (1 ng/mL TNF, 500 nM compound A (Smac mimetic), 10 μM Q-VD-OPh) in a dose-dependent manner. GW806742X shows inhibition of VEGF induced proliferation of HUVECs with an IC50 of 5 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
