ERK1/2 inhibitor 1

Biological Activity

ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively[1]. ERK1/2 inhibitor 1 (Compound 27) shows excellent antiproliferative potency with IC50s of 4.9 and 7.5 nM in A375 and Colo205 cells, respectively[1].

References

[1]. Heightman TD, et al. Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2. J Med Chem. 2018 Jun 14;61(11):4978-4992.