MEK

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MEK Signaling Pathway Map

MEK Signaling Pathways

MEK Products

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  • New MEK Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0404New Zapnometinib (PD0184264) Zapnometinib (PD0184264, ATR-002), an major active metabolite of CI-1040, is a novel MEK inhibitor with an IC50 of 5.7 nM.
E2821New RGB-286638 free base RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
E3106New Dioscoreae Nipponicae Rhizoma Extract Dioscoreae Nipponicae Rhizoma Extract is extracted from the rhizome of Dioscorea nipponica, of which the main component decreases the phosphorylation in IGF-1R, which in turn inhibits the phosphorylation and activation of PI3K-AKT and Rap1-MEK signaling pathways, promoting cell apoptosis and Graves’ disease remission.
S0739New PD184161 PD184161, an orally active MEK inhibitor with IC50 of 10-100 nM in a time- and concentration-dependent manner, inhibits cell proliferation and induces apoptosis, and produces depressive-like behavior.
S0743 GW 284543 hydrochloride GW 284543 hydrochloride (UNC 10225170) is a selective inhibitor of MEK5.
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.
Cancer Cell, 2022, S1535-6108(21)00662-0
Blood, 2022, blood.2021014304
Nat Commun, 2022, 13(1):1691
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.
Cancer Cell, 2022, S1535-6108(22)00005-8
Signal Transduct Target Ther, 2022, 7(1):51
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
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, 2022, 604(7904):111-119
Cell Stem Cell, 2022, S1934-5909(22)00010-8
Mol Cell, 2022, 82(6):1169-1185.e7
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.
Eur J Neurosci, 2022, 55(6):1471-1482
Nat Commun, 2020, 25;11(1):1556
Neuroscience, 2020, 430:1-11
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
Mol Oncol, 2021, 10.1002/1878-0261.13153
Int J Mol Sci, 2021, 22(13)6727
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.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Redox Biol, 2022, 54:102384
Mol Syst Biol, 2022, 18(6):e10670
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.
Cancer Discov, 2022, candisc.1672.2021
Cell Death Dis, 2022, 13(7):626
Cancer Lett, 2022, 541:215749
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Sci Rep, 2022, 12(1):2928
Mol Cancer Ther, 2020, 5;molcanther.1131.2019
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.
Cancers (Basel), 2022, 14(6)1575
Front Oncol, 2021, 11:780654
Mol Oncol, 2021, 10.1002/1878-0261.13153
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
Front Cell Dev Biol, 2021, 9:742049
Nat Immunol, 2018, 19(3):233-245
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.
Cells, 2022, 11(9)1392
Cell Stem Cell, 2021, 28(2):257-272.e11
Front Cell Dev Biol, 2021, 9:742049
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.
Cancers (Basel), 2022, 14(6)1575
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
S2134 AZD8330 AZD8330 (ARRY704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
Cancers (Basel), 2022, 14(6)1575
Curr Protoc, 2021, 1(6):e180
Int J Clin Oncol, 2020, 19
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.
Br J Pharmacol, 2022, 10.1111/bph.15837
Cell Death Dis, 2021, 12(9):847
Front Cell Dev Biol, 2021, 9:619475
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.
Evid Based Complement Alternat Med, 2022, 2022:3115312
Molecules, 2021, 26(5)1210
Front Med (Lausanne), 2020, 7:71
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.
Cancers (Basel), 2022, 14(6)1575
Cells, 2022, 11(5)775
Curr Protoc, 2021, 1(6):e180
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, 2022, 603(7900):335-342
Cell, 2022, S0092-8674(22)00472-X
Cancer Discov, 2022, cd.22.0044
S4484 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.
Cell Rep, 2022, 38(7):110374
S6641New GW284543 (UNC10225170) GW284543 (UNC10225170), a MEK5-selective inhibitor, inhibits MEK5 in a dose-dependently way as determined by reductions in pERK5, and decreases endogenous MYC protein.
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, 2022, S0092-8674(22)00472-X
EMBO Mol Med, 2022, e14876
Cancer Res, 2022, canres.1397.2021
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.
Int J Endocrinol, 2021, 2021:5720145
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
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.
Cancer Cell, 2022, S1535-6108(21)00662-0
Signal Transduct Target Ther, 2022, 7(1):51
Nat Commun, 2022, 13(1):1100
A5009 MEK2 Rabbit Recombinant mAb

MEK2 Rabbit Recombinant mAb detects endogenous levels of MEK2.

A5019 MEK1 Rabbit Recombinant mAb

MEK1 Rabbit Recombinant mAb detects endogenous levels of total MEK1.

Am J Transl Res, 2018, 10(10):3068-3085
A5050 MEK3/MEK6 Rabbit Recombinant mAb

MEK3/MEK6 Antibody detects endogenous levels of MEK3/MEK6.

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
E0404New Zapnometinib (PD0184264) Zapnometinib (PD0184264, ATR-002), an major active metabolite of CI-1040, is a novel MEK inhibitor with an IC50 of 5.7 nM.
E2821New RGB-286638 free base RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
E3106New Dioscoreae Nipponicae Rhizoma Extract Dioscoreae Nipponicae Rhizoma Extract is extracted from the rhizome of Dioscorea nipponica, of which the main component decreases the phosphorylation in IGF-1R, which in turn inhibits the phosphorylation and activation of PI3K-AKT and Rap1-MEK signaling pathways, promoting cell apoptosis and Graves’ disease remission.
S0739New PD184161 PD184161, an orally active MEK inhibitor with IC50 of 10-100 nM in a time- and concentration-dependent manner, inhibits cell proliferation and induces apoptosis, and produces depressive-like behavior.
S0743 GW 284543 hydrochloride GW 284543 hydrochloride (UNC 10225170) is a selective inhibitor of MEK5.
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.
Cancer Cell, 2022, S1535-6108(21)00662-0
Blood, 2022, blood.2021014304
Nat Commun, 2022, 13(1):1691
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.
Cancer Cell, 2022, S1535-6108(22)00005-8
Signal Transduct Target Ther, 2022, 7(1):51
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
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, 2022, 604(7904):111-119
Cell Stem Cell, 2022, S1934-5909(22)00010-8
Mol Cell, 2022, 82(6):1169-1185.e7
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.
Eur J Neurosci, 2022, 55(6):1471-1482
Nat Commun, 2020, 25;11(1):1556
Neuroscience, 2020, 430:1-11
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
Mol Oncol, 2021, 10.1002/1878-0261.13153
Int J Mol Sci, 2021, 22(13)6727
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.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Redox Biol, 2022, 54:102384
Mol Syst Biol, 2022, 18(6):e10670
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.
Cancer Discov, 2022, candisc.1672.2021
Cell Death Dis, 2022, 13(7):626
Cancer Lett, 2022, 541:215749
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Sci Rep, 2022, 12(1):2928
Mol Cancer Ther, 2020, 5;molcanther.1131.2019
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.
Cancers (Basel), 2022, 14(6)1575
Front Oncol, 2021, 11:780654
Mol Oncol, 2021, 10.1002/1878-0261.13153
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
Front Cell Dev Biol, 2021, 9:742049
Nat Immunol, 2018, 19(3):233-245
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.
Cells, 2022, 11(9)1392
Cell Stem Cell, 2021, 28(2):257-272.e11
Front Cell Dev Biol, 2021, 9:742049
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.
Cancers (Basel), 2022, 14(6)1575
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
S2134 AZD8330 AZD8330 (ARRY704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
Cancers (Basel), 2022, 14(6)1575
Curr Protoc, 2021, 1(6):e180
Int J Clin Oncol, 2020, 19
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.
Br J Pharmacol, 2022, 10.1111/bph.15837
Cell Death Dis, 2021, 12(9):847
Front Cell Dev Biol, 2021, 9:619475
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.
Evid Based Complement Alternat Med, 2022, 2022:3115312
Molecules, 2021, 26(5)1210
Front Med (Lausanne), 2020, 7:71
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.
Cancers (Basel), 2022, 14(6)1575
Cells, 2022, 11(5)775
Curr Protoc, 2021, 1(6):e180
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, 2022, 603(7900):335-342
Cell, 2022, S0092-8674(22)00472-X
Cancer Discov, 2022, cd.22.0044
S4484 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.
Cell Rep, 2022, 38(7):110374
S6641New GW284543 (UNC10225170) GW284543 (UNC10225170), a MEK5-selective inhibitor, inhibits MEK5 in a dose-dependently way as determined by reductions in pERK5, and decreases endogenous MYC protein.
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, 2022, S0092-8674(22)00472-X
EMBO Mol Med, 2022, e14876
Cancer Res, 2022, canres.1397.2021
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.
Int J Endocrinol, 2021, 2021:5720145
Curr Protoc, 2021, 1(6):e180
Nature, 2019, 569(7757):509-513
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.
Cancer Cell, 2022, S1535-6108(21)00662-0
Signal Transduct Target Ther, 2022, 7(1):51
Nat Commun, 2022, 13(1):1100
A5009 MEK2 Rabbit Recombinant mAb

MEK2 Rabbit Recombinant mAb detects endogenous levels of MEK2.

A5019 MEK1 Rabbit Recombinant mAb

MEK1 Rabbit Recombinant mAb detects endogenous levels of total MEK1.

Am J Transl Res, 2018, 10(10):3068-3085
A5050 MEK3/MEK6 Rabbit Recombinant mAb

MEK3/MEK6 Antibody detects endogenous levels of MEK3/MEK6.

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
E0404New Zapnometinib (PD0184264) Zapnometinib (PD0184264, ATR-002), an major active metabolite of CI-1040, is a novel MEK inhibitor with an IC50 of 5.7 nM.
E2821New RGB-286638 free base RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
E3106New Dioscoreae Nipponicae Rhizoma Extract Dioscoreae Nipponicae Rhizoma Extract is extracted from the rhizome of Dioscorea nipponica, of which the main component decreases the phosphorylation in IGF-1R, which in turn inhibits the phosphorylation and activation of PI3K-AKT and Rap1-MEK signaling pathways, promoting cell apoptosis and Graves’ disease remission.
S0739New PD184161 PD184161, an orally active MEK inhibitor with IC50 of 10-100 nM in a time- and concentration-dependent manner, inhibits cell proliferation and induces apoptosis, and produces depressive-like behavior.
S6641New GW284543 (UNC10225170) GW284543 (UNC10225170), a MEK5-selective inhibitor, inhibits MEK5 in a dose-dependently way as determined by reductions in pERK5, and decreases endogenous MYC protein.
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