MEK

Isoform-selective Products

Signaling Pathway

MEK Signaling Pathway

MEK Products

  • All (33)
  • MEK Inhibitors (32)
  • MEK Antagonist (1)
  • New MEK Products
Catalog No. Product Name Information Product Use Citations Product Validations
S2673 Trametinib (GSK1120212) Trametinib (GSK1120212, JTP-74057) 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, 2024, 629(8013):927-936
Cell, 2024, 187(3):712-732.e38
Cell, 2024, S0092-8674(24)00825-0
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, 2024, 10.1038/s41586-024-07706-4
Nature, 2024, 632(8027):1073-1081
Cell Stem Cell, 2024, 31(10):1501-1512.e8
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.
MedComm (2020), 2024, 5(5):e525
Int J Biol Sci, 2024, 20(6):2202-2218
Cell Death Dis, 2024, 15(1):31
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.
Nature, 2024, 629(8013):927-936
Nat Commun, 2024, 15(1):8002
Nat Commun, 2024, 15(1):6919
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
Cell Commun Signal, 2024, 22(1):473
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.
Nat Commun, 2024, 15(1):2132
Proc Natl Acad Sci U S A, 2024, 121(44):e2321305121
iScience, 2024, 27(3):109249
S8041 Cobimetinib (GDC-0973) Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, and showing no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.
Nature, 2024, 629(8013):927-936
Signal Transduct Target Ther, 2024, 9(1):293
Gastroenterology, 2024, S0016-5085(24)00062-3
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.
Nature, 2024, 629(8013):927-936
Signal Transduct Target Ther, 2024, 9(1):293
Gastroenterology, 2024, S0016-5085(24)00062-3
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.
Cancer Cell Int, 2024, 24(1):8
Nat Commun, 2023, 14(1):478
Br J Haematol, 2023, 10.1111/bjh.19018
S2310 Honokiol Honokiol 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.
Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
Nat Commun, 2023, 14(1):478
Cancers (Basel), 2022, 14(6)1575
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.
Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9
Neurooncol Adv, 2023, 5(1):vdad132
Nature, 2022, 604(7905):354-361
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
Neurooncol Adv, 2023, 5(1):vdad132
Cancer Res Commun, 2023, 3(10):2170-2181
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, 2024, 15(1):2539
Int J Mol Sci, 2024, 25(10)5478
Hum Mol Genet, 2023, 32(10):1722-1729
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.
Antibiotics (Basel), 2024, 13(9)909
JID Innov, 2024, 4(2):100248
Cell Rep, 2022, 38(7):110374
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
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.
E3106 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.
E1902New Nedometinib Nedometinib (NFX-179) is a highly specific and potent inhibitor of MEK1 with an IC50 of 135 nM. It also results in suppression of p-ERK levels and can be used in research and treatment of cutaneous neurofibromas (cNFs) associated with neurofibromatosis type 1 (NF1).
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.
E1965New NST-628 NST-628 is a potent and well-tolerated single-agent inhibitor of both RAF and MEK. It acts as a pan-RAF–MEK molecular glue that blocks the phosphorylation and activation of MEK by RAF.
S9740New U0126 U0126 is a highly potent and selective inhibitor of the dual-specificity kinases MEK1 and MEK2, with IC50 values of 72 nM and 58 nM, respectively. It also acts as a strong antioxidant, protecting cells from oxidative stress-induced cell death.
S2673 Trametinib (GSK1120212) Trametinib (GSK1120212, JTP-74057) 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, 2024, 629(8013):927-936
Cell, 2024, 187(3):712-732.e38
Cell, 2024, S0092-8674(24)00825-0
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, 2024, 10.1038/s41586-024-07706-4
Nature, 2024, 632(8027):1073-1081
Cell Stem Cell, 2024, 31(10):1501-1512.e8
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.
MedComm (2020), 2024, 5(5):e525
Int J Biol Sci, 2024, 20(6):2202-2218
Cell Death Dis, 2024, 15(1):31
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.
Nature, 2024, 629(8013):927-936
Nat Commun, 2024, 15(1):8002
Nat Commun, 2024, 15(1):6919
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
Cell Commun Signal, 2024, 22(1):473
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.
Nat Commun, 2024, 15(1):2132
Proc Natl Acad Sci U S A, 2024, 121(44):e2321305121
iScience, 2024, 27(3):109249
S8041 Cobimetinib (GDC-0973) Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, and showing no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.
Nature, 2024, 629(8013):927-936
Signal Transduct Target Ther, 2024, 9(1):293
Gastroenterology, 2024, S0016-5085(24)00062-3
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.
Nature, 2024, 629(8013):927-936
Signal Transduct Target Ther, 2024, 9(1):293
Gastroenterology, 2024, S0016-5085(24)00062-3
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.
Cancer Cell Int, 2024, 24(1):8
Nat Commun, 2023, 14(1):478
Br J Haematol, 2023, 10.1111/bjh.19018
S2310 Honokiol Honokiol 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.
Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
Nat Commun, 2023, 14(1):478
Cancers (Basel), 2022, 14(6)1575
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.
Nat Biomed Eng, 2024, 10.1038/s41551-024-01273-9
Neurooncol Adv, 2023, 5(1):vdad132
Nature, 2022, 604(7905):354-361
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
Neurooncol Adv, 2023, 5(1):vdad132
Cancer Res Commun, 2023, 3(10):2170-2181
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, 2024, 15(1):2539
Int J Mol Sci, 2024, 25(10)5478
Hum Mol Genet, 2023, 32(10):1722-1729
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.
Antibiotics (Basel), 2024, 13(9)909
JID Innov, 2024, 4(2):100248
Cell Rep, 2022, 38(7):110374
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.
E3106 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.
E1902New Nedometinib Nedometinib (NFX-179) is a highly specific and potent inhibitor of MEK1 with an IC50 of 135 nM. It also results in suppression of p-ERK levels and can be used in research and treatment of cutaneous neurofibromas (cNFs) associated with neurofibromatosis type 1 (NF1).
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.
E1965New NST-628 NST-628 is a potent and well-tolerated single-agent inhibitor of both RAF and MEK. It acts as a pan-RAF–MEK molecular glue that blocks the phosphorylation and activation of MEK by RAF.
S9740New U0126 U0126 is a highly potent and selective inhibitor of the dual-specificity kinases MEK1 and MEK2, with IC50 values of 72 nM and 58 nM, respectively. It also acts as a strong antioxidant, protecting cells from oxidative stress-induced cell death.
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
E1902New Nedometinib Nedometinib (NFX-179) is a highly specific and potent inhibitor of MEK1 with an IC50 of 135 nM. It also results in suppression of p-ERK levels and can be used in research and treatment of cutaneous neurofibromas (cNFs) associated with neurofibromatosis type 1 (NF1).
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.
E1965New NST-628 NST-628 is a potent and well-tolerated single-agent inhibitor of both RAF and MEK. It acts as a pan-RAF–MEK molecular glue that blocks the phosphorylation and activation of MEK by RAF.
S9740New U0126 U0126 is a highly potent and selective inhibitor of the dual-specificity kinases MEK1 and MEK2, with IC50 values of 72 nM and 58 nM, respectively. It also acts as a strong antioxidant, protecting cells from oxidative stress-induced cell death.

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