MEK

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MEK製品

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  • MEK阻害剤 (27)
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S1036 Mirdametinib (PD0325901) ミルダメチニブ (Mirdametinib (PD0325901)) は選択的非 ATP 競合性 MEK 阻害剤です。Cell-free assay における IC50 は0.33 nM で、ERK1 および ERK2 のリン酸化に対して CI-1040 よりも約 500 倍の活性を有しています。臨床第2相試験中
Nat Commun, 2024, 15(1):668
J Adv Res, 2024, S2090-1232(24)00073-0
Cell Rep, 2024, 43(1):113614
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.
Cell Death Dis, 2024, 15(1):31
Cell Mol Life Sci, 2024, 81(1):59
mBio, 2024, e0313623.
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.
iScience, 2024, 27(1):108696
Nat Cancer, 2023, 4(3):419-435
Nat Cancer, 2023, 4(3):419-435
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.
Nat Commun, 2024, 15(1):987
Adv Sci (Weinh), 2024, 11(4):e2304987
Cancer Cell Int, 2024, 24(1):54
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.
iScience, 2024, 27(3):109249
Front Cell Infect Microbiol, 2024, 14:1275940
PLoS One, 2023, 18(5):e0285707
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.
Gastroenterology, 2024, S0016-5085(24)00062-3
Cell Rep Med, 2023, 4(10):101200
Cell Rep Med, 2023, S2666-3791(23)00367-1
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.
Gastroenterology, 2024, S0016-5085(24)00062-3
Oncologist, 2024, 29(1):15-24
Cell Rep Med, 2023, 4(4):101002
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.
PLoS One, 2024, 19(1):e0295629
Nat Commun, 2023, 10.1038/s41467-023-43369-x
Exp Mol Med, 2023, 55(6):1247-1257
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.
Nat Commun, 2023, 14(1):478
Br J Haematol, 2023, 10.1111/bjh.19018
J Cell Commun Signal, 2023, 17(3):975-989
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.
Int J Nanomedicine, 2023, 18:4313-4327
Exp Gerontol, 2023, 173:112091
Cell Death Differ, 2022, 10.1038/s41418-022-01053-5
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.
Signal Transduct Target Ther, 2023, 8(1):11
Nat Commun, 2023, 14(1):478
Cell Rep Med, 2023, S2666-3791(23)00367-1
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.
Nat Commun, 2023, 14(1):478
mediaTUM, 2023,
Br J Cancer, 2022, 10.1038/s41416-022-01973-6
S2134 AZD8330 AZD8330 (ARRY704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
Nat Commun, 2023, 14(1):478
Cancers (Basel), 2022, 14(6)1575
Int J Tryptophan Res, 2022, 15:11786469221138456
S7170 Avutometinib Avutometinib(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.
Nature, 2022, 604(7905):354-361
Br J Cancer, 2022, 10.1038/s41416-022-01973-6
Cell Mol Life Sci, 2022, 80(1):12
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 Death Dis, 2023, 14(11):715
Cell Death Dis, 2023, 10.1038/s41419-023-06229-6
Cell Stem Cell, 2021, 28(2):257-272.e11
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
Cancer Discov, 2022, 12(5):1378-1395
Cell Oncol (Dordr), 2022, 45(4):601-619
S7553 GDC-0623 GDC-0623 (G-868) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
Cancer Res Commun, 2023, 3(10):2170-2181
Cancer Res Commun, 2023, 3(10):2170-2181
Transplantation, 2022, 106-8:1589-1599
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.
bioRxiv, 2023, 10.1101/2023.12.12.571297
Nat Cardiovasc Res, 2023, 2:2023530-549
Metab Brain Dis, 2022, 37(4):1057-1070
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.
SLAS Discov, 2024, S2472-5552(24)00007-8
Evid Based Complement Alternat Med, 2022, 2022:3115312
Molecules, 2021, 26(5)1210
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.
Nat Commun, 2023, 14(1):478
Cancer Res Commun, 2023, 3(10):2170-2181
Cancer Res Commun, 2023, 3(10):2170-2181
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.
iScience, 2022, 25(10):105182
Cancers (Basel), 2022, 14(6)1575
Curr Protoc, 2021, 1(6):e180
S4484 Trametinib DMSO solvate Trametinib 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.
JID Innov, 2024, 4(2):100248
Cell Rep, 2022, 38(7):110374
Mol Cell Proteomics, 2022, 21(6):100240
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.
Sci Adv, 2019, 5(11):eaax4249
Exp Ther Med, 2018, 15(6):5269-5274
S0739 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.
E2821 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.
S6641 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.
S0372New RO4987655 RO4987655(RG 7167,CH4987655) is an allosteric MEK inhibitor with IC50 of 5 nM. RO4987655 exhibits a significant anti-proliferative and antitumor activity.
E0404 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.
S1036 Mirdametinib (PD0325901) ミルダメチニブ (Mirdametinib (PD0325901)) は選択的非 ATP 競合性 MEK 阻害剤です。Cell-free assay における IC50 は0.33 nM で、ERK1 および ERK2 のリン酸化に対して CI-1040 よりも約 500 倍の活性を有しています。臨床第2相試験中
Nat Commun, 2024, 15(1):668
J Adv Res, 2024, S2090-1232(24)00073-0
Cell Rep, 2024, 43(1):113614
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.
Cell Death Dis, 2024, 15(1):31
Cell Mol Life Sci, 2024, 81(1):59
mBio, 2024, e0313623.
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.
iScience, 2024, 27(1):108696
Nat Cancer, 2023, 4(3):419-435
Nat Cancer, 2023, 4(3):419-435
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.
Nat Commun, 2024, 15(1):987
Adv Sci (Weinh), 2024, 11(4):e2304987
Cancer Cell Int, 2024, 24(1):54
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.
iScience, 2024, 27(3):109249
Front Cell Infect Microbiol, 2024, 14:1275940
PLoS One, 2023, 18(5):e0285707
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.
Gastroenterology, 2024, S0016-5085(24)00062-3
Cell Rep Med, 2023, 4(10):101200
Cell Rep Med, 2023, S2666-3791(23)00367-1
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.
Gastroenterology, 2024, S0016-5085(24)00062-3
Oncologist, 2024, 29(1):15-24
Cell Rep Med, 2023, 4(4):101002
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.
PLoS One, 2024, 19(1):e0295629
Nat Commun, 2023, 10.1038/s41467-023-43369-x
Exp Mol Med, 2023, 55(6):1247-1257
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.
Nat Commun, 2023, 14(1):478
Br J Haematol, 2023, 10.1111/bjh.19018
J Cell Commun Signal, 2023, 17(3):975-989
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.
Int J Nanomedicine, 2023, 18:4313-4327
Exp Gerontol, 2023, 173:112091
Cell Death Differ, 2022, 10.1038/s41418-022-01053-5
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.
Signal Transduct Target Ther, 2023, 8(1):11
Nat Commun, 2023, 14(1):478
Cell Rep Med, 2023, S2666-3791(23)00367-1
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.
Nat Commun, 2023, 14(1):478
mediaTUM, 2023,
Br J Cancer, 2022, 10.1038/s41416-022-01973-6
S2134 AZD8330 AZD8330 (ARRY704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
Nat Commun, 2023, 14(1):478
Cancers (Basel), 2022, 14(6)1575
Int J Tryptophan Res, 2022, 15:11786469221138456
S7170 Avutometinib Avutometinib(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.
Nature, 2022, 604(7905):354-361
Br J Cancer, 2022, 10.1038/s41416-022-01973-6
Cell Mol Life Sci, 2022, 80(1):12
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 Death Dis, 2023, 14(11):715
Cell Death Dis, 2023, 10.1038/s41419-023-06229-6
Cell Stem Cell, 2021, 28(2):257-272.e11
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
Cancer Discov, 2022, 12(5):1378-1395
Cell Oncol (Dordr), 2022, 45(4):601-619
S7553 GDC-0623 GDC-0623 (G-868) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
Cancer Res Commun, 2023, 3(10):2170-2181
Cancer Res Commun, 2023, 3(10):2170-2181
Transplantation, 2022, 106-8:1589-1599
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.
bioRxiv, 2023, 10.1101/2023.12.12.571297
Nat Cardiovasc Res, 2023, 2:2023530-549
Metab Brain Dis, 2022, 37(4):1057-1070
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.
SLAS Discov, 2024, S2472-5552(24)00007-8
Evid Based Complement Alternat Med, 2022, 2022:3115312
Molecules, 2021, 26(5)1210
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.
Nat Commun, 2023, 14(1):478
Cancer Res Commun, 2023, 3(10):2170-2181
Cancer Res Commun, 2023, 3(10):2170-2181
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.
iScience, 2022, 25(10):105182
Cancers (Basel), 2022, 14(6)1575
Curr Protoc, 2021, 1(6):e180
S4484 Trametinib DMSO solvate Trametinib 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.
JID Innov, 2024, 4(2):100248
Cell Rep, 2022, 38(7):110374
Mol Cell Proteomics, 2022, 21(6):100240
S0739 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.
E2821 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.
S6641 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.
S0372New RO4987655 RO4987655(RG 7167,CH4987655) is an allosteric MEK inhibitor with IC50 of 5 nM. RO4987655 exhibits a significant anti-proliferative and antitumor activity.
E0404 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.
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.
Sci Adv, 2019, 5(11):eaax4249
Exp Ther Med, 2018, 15(6):5269-5274
S0372New RO4987655 RO4987655(RG 7167,CH4987655) is an allosteric MEK inhibitor with IC50 of 5 nM. RO4987655 exhibits a significant anti-proliferative and antitumor activity.

MEK阻害剤の選択性比較

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