REVIEW GW806742X is a nanomolar inhibitor of the protein kinase, VEGFR2 (2nm) and also binds to the pseudokinase domain of MLKL and blocks cell death by necroptosis. With regards to its role in necroptosis, GW806742X 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. GW806742X therefore appears 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.
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