A potent, orally-active MEK1/2 inhibitor with IC50 of 10-100 nM.

APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM

APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM

AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM.

AZD8330(ARRY-424704; ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM.

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. Phase 1.

BIX02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

CI-1040 (PD 184352) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM.

GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase, also known as MEK, a serine/threonine kinase that is a component of the RAS/RAF/MEK/ERK pathway.

OTS964 is a novel TOPK(T–lymphokine-activated killer cell–originated protein kinase) inhibitor.

PD 98059 is a selective inhibitor of MEK and blocker of MAPK

PD0325901 (PD325901) is selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM.

PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.

RO5126766(CH5126766) is a Raf/MEK dual kinase inhibitor.

TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.

Trametinib is a highly specific and potent MEK1 and MEK2 inhibitor with IC50 of 0.92 nM and 1.8 nM, respectively.

U0126-EtOH(U-0126) is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD098059.

Vacquinol-1 is an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells.

AS703026(Pimasertib) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines.

RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.