MEK1/2 - MAPK Signaling

Cat.No. Product Name Information

BCC4587 TAK-733 TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM. TAK-733

BCC7200 U0124 U0124

BCC2550 BIX 02188 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.

BCC2549 BIX 02189 BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 59 nM in cell-free assays, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

BCC4150 GDC-0623 GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).

BCC1066 U0126-EtOH U0126-EtOH is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126-EtOH is an autophagy and mitophagy inhibitor.

BCC2013 Trametinib DMSO solvate Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.

BCC6511 BI-847325 BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.

BCC2529 Pimasertib (AS-703026) Pimasertib (AS703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2, used for cancer treatment.

BCC6371 GDC-0994 Ravoxertinib (GDC-0994) is an orally bioavailable ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.

BCC1098 PD98059 PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits autophagy. PD98059

BCC7428 PD 198306 Selective inhibitor of MEK1/2

BCC1112 PD184352 (CI-1040) CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.

BCC1123 SL-327 SL327 inhibits MEK1 and MEK2, with IC50 values of 180 nM and 220 nM, respectively. SL-327

BCC1738 MEK inhibitor MEK inhibitor is a potent MEK inhibitor with antitumor potency.

BCC2539 PD318088 PD318088 is an allosteric MEK inhibitor.

BCC1277 PD0325901 PD0325901 is a selective and cell permeable MEK inhibitor with an IC50 of 0.33 nM.

BCC6300 PD 334581

BCC3624 AZD6244 (Selumetinib) Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

BCC1148 MEK162 (ARRY-162, ARRY-438162) Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.

BCC5773 10Z-Hymenialdisine

BCC3733 AZD8330 AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 nM. AZD8330

BCC1282 Trametinib (GSK1120212) Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.

BCC5135 RO4987655 RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.

BCC4276 Refametinib Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.

BCC4055 Refametinib R enantiomer Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM.

BCC1491 Cobimetinib Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.

BCC1493 Cobimetinib (R-enantiomer) Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.

BCC1492 Cobimetinib (racemate) Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.

BCC1935 SCH772984 SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.

BCC6374 RO5126766(CH5126766) Ro 5126766 is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAFV600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).

Products for MEK1/2