GW-806742X

Soluble in DMSO. Potent protein kinase VEGFR2 inhibitor (2nm range). Binds to the pseudokinase domain of MLKL and blocks cell death by necroptosis, as well. With regards to its role in necroptosis, it is an ATP-mimetic that was shown to bind recombinant mouse MLKL pseudokinase domain, which showed inhibited TSQ-induced death of mouse dermal fibroblasts by delaying MLKL translocation to the membrane. Appears therefore to be a valuable reagent to inhibit necroptosis. It also provides an important proof-of-principle that targeting catalytically-dead pseudoenzymes represents a feasible, emerging therapeutic avenue.