MEK

Choose Selective MEK Inhibitors

MEK Signaling Pathway Map

MEK Signaling Pathways

MEK Products

  • All (27)
  • MEK Inhibitors (23)
  • MEK Antibodies (3)
  • MEK Antagonists (1)
  • New MEK Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1008 Selumetinib (AZD6244) Selumetinib (AZD6244, ARRY-142886) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Selumetinib suppresses cell proliferation, migration and trigger apoptosis. Phase 3.
Nat Cell Biol, 2021, 23(4):377-390
J Extracell Vesicles, 2021, 10(8):e12091
Cancer Res, 2021, canres.1895.2020
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. PD184352 (CI-1040) selectively induces apoptosis. Phase 2.
Cell Syst, 2021, S2405-4712(21)00111-3
Elife, 2021, 10e66596
Elife, 2021, 10e73430
S1036 Mirdametinib (PD0325901) Mirdametinib (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, 2021, 10.1038/s41586-020-03085-8
Cell, 2021, 184(11):2843-2859.e20
Nat Genet, 2021, 53(12):1686-1697
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.
Nat Commun, 2020, 25;11(1):1556
Neuroscience, 2020, 430:1-11
Nat Commun, 2019, 10(1):2016
S1089 Refametinib (RDEA119) 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.
Genome Med, 2021, 13(1):116
Int J Mol Sci, 2021, 22(13)6727
J Transl Med, 2021, 19(1):184
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. U0126 inhibits autophagy and mitophagy with antiviral activity.
J Am Chem Soc, 2021, 10.1021/jacs.1c05386
Sci Adv, 2021, 7(36):eabi9787
Theranostics, 2021, 11(3):996-1015
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. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.
Biomed Pharmacother, 2022, 145:112437
Mol Med Rep, 2022, 25(2)56
Immunity, 2021, S1074-7613(20)30538-0
S1392 Pelitinib (EKB-569) Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Pelitinib (EKB-569) also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282 nM, 800 nM and 1255 nM, respectively. Phase2.
Mol Cancer Ther, 2020, 5;molcanther.1131.2019
Nat Cell Biol, 2019, 21(6):778-790
Korean J Parasitol, 2017, 55(5):491-503
S1475 Pimasertib (AS-703026) Pimasertib (AS-703026, MSC1936369B, SAR 245509) 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.
Sci Rep, 2021, 11(1):9161
STAR Protoc, 2021, 2(1):100300
Commun Biol, 2021, 4(1):1333
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.
Cell Stem Cell, 2021, 28(2):257-272.e11
Nat Immunol, 2018, 19(3):233-245
J Leukoc Biol, 2016, 99(1):143-52
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.
Cell Stem Cell, 2021, 28(2):257-272.e11
Cancers (Basel), 2021, 13(6)1205
Cell Death Dis, 2021, 12(12):1119
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.
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
Nat Commun, 2019, 10(1):2197
S2134 AZD8330 AZD8330 (ARRY704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
Curr Protoc, 2021, 1(6):e180
Int J Clin Oncol, 2020, 19
Nature, 2019, 569(7757):509-513
S2310 Honokiol (NSC 293100) Honokiol (NSC 293100) is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Honokiol causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. Honokiol inhibits hepatitis C virus (HCV) infection. Phase 3.
Cell Death Dis, 2021, 12(9):847
Front Cell Dev Biol, 2021, 9:619475
Am J Cancer Res, 2021, 11(6):3039-3054
S2326 Myricetin Myricetin, a natural flavonoid with antioxidant and anti tumor properties, is a novel inhibitor of MEK1 activity and transformation of JB6 P+ mouse epidermal cells. It also inhibits PI3Kγ with Kd of 0.17 μM.
Molecules, 2021, 26(5)1210
Front Med (Lausanne), 2020, 7:71
Int J Mol Sci, 2020, 21(14):5025
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.
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
Mol Cancer, 2019,
S2673 Trametinib (GSK1120212) Trametinib (GSK1120212, JTP-74057, Mekinist) 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. Trametinib activates autophagy and induces apoptosis.
Nature, 2021, 10.1038/s41586-021-03916-2
Cell, 2021, 184(25):6119-6137.e26
Nat Biotechnol, 2021, 10.1038/s41587-021-00837-3
S4484New Trametinib DMSO solvate Trametinib (GSK1120212, JTP-74057, Mekinist) DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis.
S7007 Binimetinib (MEK162) Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3.
Cell, 2021, 184(25):6119-6137.e26
Nat Commun, 2021, 12(1):3707
Neuro Oncol, 2021, 23(5):770-782
S7170 RO5126766 (CH5126766) RO5126766 (CH5126766, VS 6766, CKI-27, R-7304, RG-7304) 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.
EMBO Mol Med, 2021, e11814
Cancer Sci, 2021, 112(10):4026-4036
Nature, 2020, 588(7838):509-514
S7553 GDC-0623 GDC-0623 (G-868) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
Cell Rep, 2019, 29(3):573-588
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.
Sci Rep, 2021, 11(1):9161
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
S8041 Cobimetinib (GDC-0973) Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2660
EMBO Mol Med, 2021, e11814
EMBO Mol Med, 2021, e13466
A5009 MEK2 Rabbit Recombinant mAb

MEK2 Rabbit Recombinant mAb detects endogenous levels of MEK2.

A5165 MEK3 Rabbit Recombinant mAb MEK3 Rabbit Recombinant mAb detects endogenous level of MEK3.
A5191 Phospho-MEK1 (S298) Rabbit Recombinant mAb Phospho-MEK1 (S298) Rabbit Recombinant mAb detects endogenous level of total phospho-MEK1 (S298).
Mol Cancer Ther, 2021, molcanther.MCT-21-0395-A.2021
S8355 APS-2-79 HCl APS-2-79 is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK. IC50=120 ± 23 nM.
Sci Adv, 2019, 5(11):eaax4249
Exp Ther Med, 2018, 15(6):5269-5274
S1008 Selumetinib (AZD6244) Selumetinib (AZD6244, ARRY-142886) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Selumetinib suppresses cell proliferation, migration and trigger apoptosis. Phase 3.
Nat Cell Biol, 2021, 23(4):377-390
J Extracell Vesicles, 2021, 10(8):e12091
Cancer Res, 2021, canres.1895.2020
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. PD184352 (CI-1040) selectively induces apoptosis. Phase 2.
Cell Syst, 2021, S2405-4712(21)00111-3
Elife, 2021, 10e66596
Elife, 2021, 10e73430
S1036 Mirdametinib (PD0325901) Mirdametinib (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, 2021, 10.1038/s41586-020-03085-8
Cell, 2021, 184(11):2843-2859.e20
Nat Genet, 2021, 53(12):1686-1697
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.
Nat Commun, 2020, 25;11(1):1556
Neuroscience, 2020, 430:1-11
Nat Commun, 2019, 10(1):2016
S1089 Refametinib (RDEA119) 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.
Genome Med, 2021, 13(1):116
Int J Mol Sci, 2021, 22(13)6727
J Transl Med, 2021, 19(1):184
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. U0126 inhibits autophagy and mitophagy with antiviral activity.
J Am Chem Soc, 2021, 10.1021/jacs.1c05386
Sci Adv, 2021, 7(36):eabi9787
Theranostics, 2021, 11(3):996-1015
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. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.
Biomed Pharmacother, 2022, 145:112437
Mol Med Rep, 2022, 25(2)56
Immunity, 2021, S1074-7613(20)30538-0
S1392 Pelitinib (EKB-569) Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Pelitinib (EKB-569) also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282 nM, 800 nM and 1255 nM, respectively. Phase2.
Mol Cancer Ther, 2020, 5;molcanther.1131.2019
Nat Cell Biol, 2019, 21(6):778-790
Korean J Parasitol, 2017, 55(5):491-503
S1475 Pimasertib (AS-703026) Pimasertib (AS-703026, MSC1936369B, SAR 245509) 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.
Sci Rep, 2021, 11(1):9161
STAR Protoc, 2021, 2(1):100300
Commun Biol, 2021, 4(1):1333
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.
Cell Stem Cell, 2021, 28(2):257-272.e11
Nat Immunol, 2018, 19(3):233-245
J Leukoc Biol, 2016, 99(1):143-52
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.
Cell Stem Cell, 2021, 28(2):257-272.e11
Cancers (Basel), 2021, 13(6)1205
Cell Death Dis, 2021, 12(12):1119
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.
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
Nat Commun, 2019, 10(1):2197
S2134 AZD8330 AZD8330 (ARRY704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
Curr Protoc, 2021, 1(6):e180
Int J Clin Oncol, 2020, 19
Nature, 2019, 569(7757):509-513
S2310 Honokiol (NSC 293100) Honokiol (NSC 293100) is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Honokiol causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. Honokiol inhibits hepatitis C virus (HCV) infection. Phase 3.
Cell Death Dis, 2021, 12(9):847
Front Cell Dev Biol, 2021, 9:619475
Am J Cancer Res, 2021, 11(6):3039-3054
S2326 Myricetin Myricetin, a natural flavonoid with antioxidant and anti tumor properties, is a novel inhibitor of MEK1 activity and transformation of JB6 P+ mouse epidermal cells. It also inhibits PI3Kγ with Kd of 0.17 μM.
Molecules, 2021, 26(5)1210
Front Med (Lausanne), 2020, 7:71
Int J Mol Sci, 2020, 21(14):5025
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.
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
Mol Cancer, 2019,
S2673 Trametinib (GSK1120212) Trametinib (GSK1120212, JTP-74057, Mekinist) 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. Trametinib activates autophagy and induces apoptosis.
Nature, 2021, 10.1038/s41586-021-03916-2
Cell, 2021, 184(25):6119-6137.e26
Nat Biotechnol, 2021, 10.1038/s41587-021-00837-3
S4484New Trametinib DMSO solvate Trametinib (GSK1120212, JTP-74057, Mekinist) DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis.
S7007 Binimetinib (MEK162) Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3.
Cell, 2021, 184(25):6119-6137.e26
Nat Commun, 2021, 12(1):3707
Neuro Oncol, 2021, 23(5):770-782
S7170 RO5126766 (CH5126766) RO5126766 (CH5126766, VS 6766, CKI-27, R-7304, RG-7304) 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.
EMBO Mol Med, 2021, e11814
Cancer Sci, 2021, 112(10):4026-4036
Nature, 2020, 588(7838):509-514
S7553 GDC-0623 GDC-0623 (G-868) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
Cell Rep, 2019, 29(3):573-588
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.
Sci Rep, 2021, 11(1):9161
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
S8041 Cobimetinib (GDC-0973) Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2660
EMBO Mol Med, 2021, e11814
EMBO Mol Med, 2021, e13466
A5009 MEK2 Rabbit Recombinant mAb

MEK2 Rabbit Recombinant mAb detects endogenous levels of MEK2.

A5165 MEK3 Rabbit Recombinant mAb MEK3 Rabbit Recombinant mAb detects endogenous level of MEK3.
A5191 Phospho-MEK1 (S298) Rabbit Recombinant mAb Phospho-MEK1 (S298) Rabbit Recombinant mAb detects endogenous level of total phospho-MEK1 (S298).
Mol Cancer Ther, 2021, molcanther.MCT-21-0395-A.2021
S8355 APS-2-79 HCl APS-2-79 is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK. IC50=120 ± 23 nM.
Sci Adv, 2019, 5(11):eaax4249
Exp Ther Med, 2018, 15(6):5269-5274
S4484New Trametinib DMSO solvate Trametinib (GSK1120212, JTP-74057, Mekinist) DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis.
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