ERK5-IN-2

1888305-96-1

388.19

DMSO : 250 mg/mL (644.01 mM; Need ultrasonic)

Stem Cell/Wnt; MAPK/ERK Pathway

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC₅₀s of 0.82 uM, 3 uM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis^[1]. IC50 & Target: IC50: 0.82 uM (ERK5) and 3 uM (ERK5 MEF2D)^[1] In Vivo: ERK5-IN-2 (compound 46) (p.o.; 100?mg/kg; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days) has an anti-angiogenic effect and low concentrations of haemoglobin^[1].
ERK5-IN-2 (i.v. or p.o.; 10?mg/kg for 0.083-24?hours) exhibits low intrinsic clearance and has high flux and a low efflux ratio (ER) in a caco-2?cell permeability assay in both human and mouse^[1].