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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.
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
Nat Commun, 2022, 13(1):1691
Bone Res, 2022, 10(1):27
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
Cell Rep, 2022, 38(11):110522
Elife, 2022, 11e76183
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 Lett, 2022, 541:215749
Neuropathol Appl Neurobiol, 2022, e12795
Front Pharmacol, 2022, 13:817596
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.
Sci Rep, 2022, 12(1):2928
Mol Cancer Ther, 2020, 5;molcanther.1131.2019
Nat Cell Biol, 2019, 21(6):778-790
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 Cell, 2022, S1535-6108(21)00662-0
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
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
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.
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
Nat Commun, 2022, 13(1):1691
Bone Res, 2022, 10(1):27
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
Cell Rep, 2022, 38(11):110522
Elife, 2022, 11e76183
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 Lett, 2022, 541:215749
Neuropathol Appl Neurobiol, 2022, e12795
Front Pharmacol, 2022, 13:817596
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.
Sci Rep, 2022, 12(1):2928
Mol Cancer Ther, 2020, 5;molcanther.1131.2019
Nat Cell Biol, 2019, 21(6):778-790
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 Cell, 2022, S1535-6108(21)00662-0
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
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
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.
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