MEK Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
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.	iScience, 2025, 28(11):113682 Int J Mol Sci, 2025, 26(17)8241 Int J Mol Sci, 2025, 26(16)7770
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.	Cell Rep Med, 2025, 6(11):102425 Signal Transduct Target Ther, 2023, 8(1):11 Nat Commun, 2023, 14(1):478
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
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.	Int J Nanomedicine, 2025, 20:3749-3764 Cell Death Dis, 2023, 14(11):715 Cell Death Dis, 2023, 10.1038/s41419-023-06229-6
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 Transl Psychiatry, 2024, 14(1):492 Int J Mol Sci, 2024, 25(10)5478
S7553	GDC-0623	GDC-0623 (G-868) is a potent and ATP-uncompetitive MEK1 inhibitor with K_i of 0.13 nM. Phase 1.	Cancer Res Commun, 2023, 3(10):2170-2181 Neurooncol Adv, 2023, 5(1):vdad132 Transplantation, 2022, 106-8:1589-1599
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.	Redox Biol, 2025, 86:103780 SLAS Discov, 2024, S2472-5552(24)00007-8 Evid Based Complement Alternat Med, 2022, 2022:3115312
S4484	Trametinib DMSO solvate (GSK1120212B)	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
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 Med Oncol, 2022, 39(10):144
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
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.
E1902	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).
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.
S0372	RO4987655	RO4987655(RG 7167,CH4987655) is an allosteric MEK inhibitor with IC50 of 5 nM. This compound exhibits a significant anti-proliferative and antitumor activity.
E6498^New	Atebimetinib (IMM-1-104)	Atebimetinib inhibits MEK tyrosine kinase and demonstrates antineoplastic effects.
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.
E1943^New	Tunlametinib	Tunlametinib (HL-085) is a highly selective and oral inhibitor of MEK1/2 with an IC50 of 1.9 nM for MEK1, with the potential to treat RAS/RAF mutant cancers. It also induces cell cycle arrest at the G0/G1 phase and promotes apoptosis in a dose-dependent manner. It also exhibits antitumor activity in patients with advanced NRAS-mutant melanoma.
E6024	Selumetinib sulfate	Selumetinib sulfate (AZD6244 sulfate, ARRY-142886 sulfate) is an oral, non-ATP-competitive inhibitor of MEK1/2, with an IC50 of 14 nmol/L against purified MEK1. It exhibits an anti-tumor effect in the HT-29 xenograft model and is used to treat cancer and inflammation.
S2310	Honokiol	Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. This compound causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. It inhibits hepatitis C virus (HCV) infection. Phase 3.	J Adv Res, 2025, S2090-1232(25)00062-1 J Nanobiotechnology, 2025, 23(1):414 Oncol Lett, 2025, 29(4):191
S1392	Pelitinib (EKB-569)	Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. This compound 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
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.
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.
E1965	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.