ERK5-IN-3

Names

[ CAS No. ]:
1888305-85-8

[ Name ]:
ERK5-IN-3

Biological Activity

[Description]:

ERK5-IN-3 (compound 33j) is a potent and selective ERK5 (extracellular signal-related kinase 5) inhibitor, with an IC50 of 6 nM. ERK5-IN-3 shows antiproliferation activity against Hela cells, with an IC50 of 31 nM[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> MAPK/ERK Pathway >> ERK
Signaling Pathways >> Stem Cell/Wnt >> ERK

[Target]

ERK5:6 ± 1 nM (IC50)


[In Vivo]

ERK5-IN-3 (compound 33j) (10 mg/kg, i.v. and p.o, once) has low clearance (CL=20 mL/min/kg) and low oral bioavailability (F%=9%), with terminal elimination half-lives of 263 min[1].

[References]

[1]. Miller DC, et al. Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor. J Med Chem. 2022 May 12;65(9):6513-6540.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H23Cl2FN4O2

[ Molecular Weight ]:
489.37

Related Compounds