MEK

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MEK Inhibitors (19)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1008 Selumetinib (AZD6244) Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM in cell-free assays, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.
  • Nature, 2012, 487(7408):505-9
  • Nature, 2010, 468(7326):968-72
  • Cell, 2012, 151(5):937-50
S1036 PD0325901 PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2.
  • Nature, 2015, 10.1038/nature14413
  • Nature, 2015, 517(7534):391-5
  • Cell, 2015, 160(1-2):161-76
S2673 Trametinib (GSK1120212) Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2.
  • Nature, 2015, 517(7534):391-5
  • Nature, 2014, 510(7504):283-7
  • Nature, 2014, 508(7494):118-22
S1102 U0126-EtOH U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059.
  • Cell, 2013, 153(4):840-54
  • Nat Genet, 2011, 44(2):133-9
  • J Natl Cancer Inst, 2012, 104(21):1673-9
S1020 PD184352 (CI-1040) PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. Phase 2.
  • Science, 2011, 331(6019):912-6
  • Nat Genet, 2011, 44(2):133-9
  • Cancer Cell, 2016, 10.1016/j.ccell.2016.01.006
S7553 GDC-0623 GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
S1177 PD98059 PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2.
  • J Natl Cancer Inst, 2012, 104(21):1673-9
  • Hepatology, 2013, 59(4):1262-72
  • Clin Cancer Res, 2016, 10.1158/1078-0432.CCR-15-2242
S1531 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.
  • Neurobiol Aging, 2014, 35(3):669-79
  • Am J Pathol, 2013, 183(6):1758-68
  • J Biol Chem, 2014, 289(9):6311-22
S1475 Pimasertib (AS-703026) Pimasertib (AS-703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines. Phase 2.
  • FASEB J, 2014, 10.1096/fj.13-247924
  • Br J Haematol, 2014, 10.1111/bjh.13200
  • Endocrinology, 2013, 154(9):3219-27
S1530 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.
  • Cardiovasc Res, 2015, 105(1):86-95
  • Exp Neurol, 2012, 238(2):209-17
  • Mol Cancer, 2014, 13:40
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Oncotarget, 2014, 5(20):9609-18
  • Mol Cancer Ther, 2014, 13(2):353-63
  • Int J Clin Exp Pathol, 2013, 6(10):2082-91
S2134 AZD8330 AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
  • Cell, 2012, 32(34):4034-42
S7007 Binimetinib (MEK162, ARRY-162, ARRY-438162) Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Phase 3.
  • Stem Cells, 2015, 10.1002/stem.1990
  • Mol Oncol, 2014, 8(3):544-54
  • Tumour Biol, 2015, 10.1007/s13277-015-3244-2
S1568 PD318088 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.
S2310 Honokiol Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Phase 3.
  • Sensor actuat B-chem, 2012, Jin Akagi
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.
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.
  • J Neurosci, 2012, 32(14):4887-900
S8041 Cobimetinib (GDC-0973, RG7420) Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM. Phase 3.
  • Cancer Discov, 2015, 10.1158/2159-8290.CD-15-0913
S7843 BI-847325 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.
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All MEK Products

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1008 Selumetinib (AZD6244) <1 mg/mL 91 mg/mL <1 mg/mL
S1036 PD0325901 <1 mg/mL 96 mg/mL 40 mg/mL
S2673 Trametinib (GSK1120212) <1 mg/mL 22 mg/mL <1 mg/mL
S1102 U0126-EtOH <1 mg/mL 85 mg/mL <1 mg/mL
S1020 PD184352 (CI-1040) <1 mg/mL 96 mg/mL 14 mg/mL
S7553 GDC-0623 <1 mg/mL 91 mg/mL 5 mg/mL
S1177 PD98059 <1 mg/mL 14 mg/mL <1 mg/mL
S1531 BIX 02189 <1 mg/mL 60 mg/mL 80 mg/mL
S1475 Pimasertib (AS-703026) <1 mg/mL 86 mg/mL <1 mg/mL
S1530 BIX 02188 <1 mg/mL 43 mg/mL 3 mg/mL
S2617 TAK-733 <1 mg/mL 101 mg/mL <1 mg/mL
S2134 AZD8330 <1 mg/mL 92 mg/mL 92 mg/mL
S7007 Binimetinib (MEK162, ARRY-162, ARRY-438162) <1 mg/mL 88 mg/mL <1 mg/mL
S1568 PD318088 <1 mg/mL 112 mg/mL 14 mg/mL
S2310 Honokiol <1 mg/mL 53 mg/mL <1 mg/mL
S1066 SL-327 <1 mg/mL 67 mg/mL 7 mg/mL
S1089 Refametinib (RDEA119, Bay 86-9766) <1 mg/mL 100 mg/mL 100 mg/mL
S8041 Cobimetinib (GDC-0973, RG7420) <1 mg/mL 100 mg/mL 47 mg/mL
S7843 BI-847325 <1 mg/mL 19 mg/mL 1 mg/mL
Tags: MEK inhibition | MEK pathway | MEK activation | MEK inhibitor cancer | MEK phosphorylation | MEK activity | MEK inhibitor clinical trial | MEK inhibitor side effects | MEK inhibitor drugs | MEK inhibitor review
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