ERK

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).

SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively.

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.

MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK inhibitor that inhibits activated ERK1 and ERK2 in vitro, with IC50 values of 23.0 nM and 8.8 nM, respectively (IMAP kinase assay), and nonactivated ERK2, with an IC50 of 0.5 nM (MEK1-ERK2-coupled assay).

AZD0364 is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.

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

AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.

Omtriptolide (PG490-88) is a water soluble derivative prodrug of triptolide purified from the Chinese herb