ERK5-IN-2 |
| Catalog No.GC36002 |
ERK5-IN-2는 ERK5 및 ERK5 MEF2D에 대해 각각 0.82μM, 3μM의 IC50을 갖는 경구 활성, 서브마이크로몰, 선택적 ERK5 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1888305-96-1
Sample solution is provided at 25 µL, 10mM.
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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]. ERK5|0.82 μM (IC50)|ERK5 MEF2D|3 μM (IC50)
ERK5-IN-2 (compound 46) (p.o.; 100mg/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.; 10mg/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: Female CD1 mice (8-10 weeks old) with Matrigel inoculation and female CD1 nude (nu/nu) mice (8-10 weeks old) bearing A2780 human ovarian carcinoma xenografts[1]
[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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