tcsc0035358 GNE 220

GNE-220 is a potent and selective inhibitor of MAP4K4 with an IC₅₀ of 7 nM.

IC50 & Target: IC50: 7 nM (MAP4K4), 9 nM (MINK/MAP4K6), 476 nM (DMPK), 1.06 μM (MELK), 1.1 μM (KHS1/MAP4K5), 1.13 μM (TBK1), 2.02 μM (Flt3), 2.06 μM (Rse)^[1]

In Vitro: GNE-220 also inhibits a few other kinases with IC₅₀s of 9 nM, 476 nM and 1.1 μM for MINK (MAP4K6), DMPK and KHS1 (MAP4K5), respectively. GNE-220 alters human umbilical vein endothelial cells (HUVEC) sprout morphology. GNE-220 also reduces pERM⁺ retraction fibres in a dose-dependent manner. GNE-220 also dose-dependently increased the number of active-INTβ1⁺ long focal adhesions (FAs)^[1].