579515-63-2

GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X has activity against VEGFR2 (IC50=2 nM). GW806742X retards MLKL membrane translocation and inhibits necroptosis[1][2].

GW806742X, an ATP mimetic, is a potent MLKL inhibitor that binds the MLKL pseudokinase domain with a Kd of 9.3μM. It has anti-VEGFR2 activity (IC50=2 nM). It delays MLKL membrane translocation and inhibits necrosis.

MLKL 9.3 μM (Kd)

VEGFR2 2 nM (IC 50 < /sub> )

MLKL: 9.3 μM (Kd); VEGFR2: 2 nM (IC₅₀)

Store at -20°C

[1] Hildebrand JM, et al. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014 Oct 21;111(42):15072-7. DOI:10.1073/pnas.1408987111
[2] Sammond DM, et al. Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase. Bioorg Med Chem Lett. 2005;15(15):3519-3523. DOI:10.1016/j.bmcl.2005.05.096