ERK5-IN-2_product_DataBase

Bioactivity	ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM 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].
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]. Animal Model:
Name	ERK5-IN-2
CAS	1888305-96-1
Formula	C17H11BrFN3O2
Molar Mass	388.19
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Reference	[1]. Myers SM, et al. Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4. Eur J Med Chem. 2019 May 25;178:530-543.

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