For research use only. Not for therapeutic Use.
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-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].
| Catalog Number | I018671 |
| CAS Number | 1888305-96-1 |
| Synonyms | 4-(2-bromo-6-fluorobenzoyl)-N-pyridin-3-yl-1H-pyrrole-2-carboxamide |
| Molecular Formula | C17H11BrFN3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H11BrFN3O2/c18-12-4-1-5-13(19)15(12)16(23)10-7-14(21-8-10)17(24)22-11-3-2-6-20-9-11/h1-9,21H,(H,22,24) |
| InChIKey | ATKCERYALDNMPL-UHFFFAOYSA-N |
| SMILES | C1=CC(=C(C(=C1)Br)C(=O)C2=CNC(=C2)C(=O)NC3=CN=CC=C3)F |
| 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. |
