||MEK Inhibitor TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.
||BIX02188 is a specific MEK5 inhibitor (IC50: 4.3 nM), also inhibits ERK5 catalytic activity (IC50: 810 nM), and does not inhibit closely related kinases MEK1/2, JNK2, and ERK2.
||BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
||GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
||U0126-EtOH, a non-ATP competitive specific inhibitor of MEK1/2, with the IC50 for MEK1/2 is 0.07 μM/0.06 μM. The affinity of U0126-EtOH for ΔN3-S218E/S222D MEK is100-fold higher over PD98059.
||BI-847325 is a selective dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.
||URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
||Pimasertib is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.
||PD98059 is a non-ATP competitive MEK inhibitor (IC50: 2 μM) in a cell-free assay; no direct inhibition of ERK1/2.
||PD184352 (CI-1040, an ATP non-competitive MEK1/2 inhibitor (IC50=17 nM), has been used in trials studying the treatment of lung cancer, breast cancer, breast neoplasms, pancreatic cancer, and colorectal cancer.
||Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
||SL327 is a selective inhibitor for MEK1/2 with IC50 of 0.18 μM/0.22 μM; able to transport through the blood-brain barrier.
||ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.
||Honokiol is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2.
||PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
||PD0325901(IC50=0.33 nM) is a specific and non-ATP-competitive MEK inhibitor, probably 500-fold more efficiency activity than CI-1040 on phosphorylation of ERK1 and ERK2.
||BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.
||Selumetinib (AZD6244), an effective, greatly specific MEK1 and ERK1/2 phosphorylation inhibitor, is with IC50 of 14 nM and 10 nM, respectively.
||Binimetinib (MEK162, ARRY-162, ARRY-438162)
||Binimetinib (MEK162, ARRY-162, ARRY-438162) is an orally available inhibitor of MEK1/2 (IC50: 12 nM) in a cell-free assay.
||BMS-599626 has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
||AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
||TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.
||Trametinib is a dual-kinase inhibitor that is used in the treatment of advanced malignant melanoma. Trametinib therapy is associated with transient elevations in serum aminotransferase and alkaline phosphatase levels during therapy, but has yet to be linked cases of clinically apparent acute liver i
||Refametinib (RDEA119, Bay 86-9766)
||Refametinib (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC50: 19/47 nM).
||Cobimetinib is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) (IC50: 0.9 nM). Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tu
||SCH772984 is a new-type, selective inhibitor of ERK1(IC50=4 nM)，ERK2(IC50=1 nM).
||RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM,19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.