VX-11e is a potent, selective, and orally bioavailable ERK2 inhibitor with Ki of <2 nM, over 200-fold selective over other kinases tested.
SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Pluripotin is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP with Kd values of 98 nM and 212 nM respectively. It maintains embryonic stem cell (ESC) self-renewal.
Pexmetinib is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line.
BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively.
DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of 0.5 μM.
Lifirafenib potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.