| 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 |
MEK2, IC50: 1.8 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 |
MEK2, 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 |
MEK2, IC50: 47 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 |
MEK2, IC50: 0.06 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 |
MEK2, IC50: 0.22 μM |