ERK - ERK2

VRT752271 is a pyrrole inhibitors of ERK protein kinase.

TCS ERK 11e (VX-11e) is a potent and selective extracellular signal-related kinase 2 (ERK2) inhibitor (Ki values are <2, 395, 540 and 852 nM for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively). Potently blocks proliferation of HT29 cells (IC50 = 48 nM).

GDC-0994 is a potent and selective Erk1/2 inhibitor. GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways.

CC-90003 is an irreversible inhibitor of ERK1/2 with IC50s in the 10-20 nM range and shows good kinase selectivity in a 258-kinase biochemical assay.

AG-126 is a ERK2 inhibitor that selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM.

Rineterkib (ERK-IN-1) (compound B) is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway.

ERK2 IN-1 is a selective ERK2 inhibitor with an IC50 of 7 nM.

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.

KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential clinical utility in MAPK pathway dysregulated tumors.