MEK1 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S2617 TAK-733

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. Phase 1.

Selective MEK1, IC50: 3.2 nM
S1008 Selumetinib (AZD6244)

Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.

Selective MEK1, IC50: 14 nM
S1177 PD98059

PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2.

Selective MEK1, IC50: 2 μM
S2673 Trametinib (GSK1120212)

Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2.

Pan MEK1, IC50: 0.92 nM
S1020 PD184352 (CI-1040)

PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM, 100-fold more selective for MEK1/2 than MEK5. Phase 2.

Pan MEK1, IC50: 17 nM
S1089 Refametinib (RDEA119, Bay 86-9766)

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.

Pan MEK1, IC50: 19 nM
S1102 U0126-EtOH

U0126-EtOH 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 PD98059.

Pan MEK1, IC50: 0.07 μM
S1066 SL-327

SL327 is a selective inhibitor for MEK1/2 with IC50 of 0.18 μM/ 0.22 μM, no activity towards Erk1, MKK3, MKK4, c-JUN, PKC, PKA, or CamKII;capable of transport through the blood-brain barrier.

Pan MEK1, IC50: 0.18 μM