tcsc1436 XMD17-109

XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC₅₀ of 162 nM.

IC50 & Target: IC50: 162 nM (ERK-5)^[1]

In Vitro: XMD17-109 (Compound 26) inhibits ERK5 biochemically with an IC₅₀ of 0.162 ± 0.006 μM, and blocks pidermal growth factor induced ERK5 autophosphorylation with an EC₅₀ of 0.09 ± 0.03 μM in cells. XMD17-109 also inhibits LRRK2[G2019S] with an IC₅₀ of 339 nM^[1]. XMD17-109 demonstrats low nanomolar cellular activity judged by the significant dose-dependent reduction of mobility shifted phosphorylated ERK5 bands from sorbitol stimulated cells. XMD17-109 completely inhibits the ERK5-mediated AP1 transcriptional activity at 30 μM and has an EC₅₀ of 4.2 μM^[2].