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MEK Methyl Ethyl Ketone

Inhibitors

Cat.No.  Name Information
M1744 ARRY-162 (Binimetinib) ARRY-162 (MEK-162; Binimetinib) is a selective, potent inhibitor of MEK and cellular pERK with IC50 of 12 nM and 11 nM, respectively.
M1759 GSK1120212 (Trametinib) Trametinib (GSK1120212; Jtp-74057) is an orally effective MEK inhibitor with IC50 of 2 nM against MEK1 and MEK2, respectively. Trametinib can activate autophagy and induce apoptosis.
M1763 Mirdametinib (PD0325901) Mirdametinib (PD0325901) is a highly potent and selective MEK inhibitor with an IC50 in C26 cells of 0.33nM.
M1977 U0126-EtOH U0126-EtOH is a potent and highly selective non-competitive inhibitor of MAPK/ERK kinase with IC50 of 72 nM for MEK1 and 58 nM for MEK2.
M3626 Cobimetinib (GDC-0973) Cobimetinib (GDC-0973, RG7420) is an effective, selective, oral MEK1 inhibitor with an IC50 of 4.2 nM against MEK1.
M21071 MAP855 MAP855 is a potent, selective and orally effective ATP-competitive MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 inhibits wild-type and mutant MEK1/2 equally.
M20028 WAY-114228 WAY-114228 is a MEK1 inhibitor.
M14172 Trametinib (DMSO solvate) Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM.
M14171 Selumetinib sulfate Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
M14170 MEK inhibitor MEK inhibitor is a potent MEK inhibitor with antitumor potency.
M14169 GDC-0623 GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).
M14168 Cobimetinib hemifumarate Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM.
M14166 BIX02188 BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.
M11250 Zapnometinib Zapnometinib (PD0184264), an active metabolite of CI-1040, is an MEK inhibitor with an IC50 value of 5.7 nM. Zapnometinib has antiviral and antibacterial activity against influenza viruses.
M10503 GW284543 (UNC10225170) GW284543 (UNC10225170) is a selective MEK5 inhibitor, which reduces pERK5 and decreases endogenous MYC protein.
M10369 RO5126766 (VS-6766) RO5126766 (CH5126766, VS 6766) is a first-in-class dual MEK/RAF inhibitor with IC50 values of 8.2 nM, 19 nM, 56 nM and 160 nM for BRAF V600E, BRAF, CRAF and MEK1, respectively.
M9432 trans-Zeatin trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division.
M9014 RO4987655 RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM.
M5236 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.
M3767 Merestinib Merestinib (LY2801653) is a potent oral bioavailable c-Met inhibitor with antitumor activity (Ki=2 nM)。 Merestinib (LY2801653) 对 MST1R (IC50=11 nM)、FLT3 (IC50=7 nM)、AXL (IC50=2 nM)、MERTK (IC50=10 nM)、TEK (IC50=63 nM)、ROS1、DDR1/2 (IC50=0.1/7 nM) 和 MKNK1/2 (IC50=7 nM) also has strong activity.
M3633 Refametinib Refametinib (BAY 86-9766, RDEA119) is a potent, highly selective and ATP non-competitive inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.
M3626 Cobimetinib (GDC-0973) Cobimetinib (GDC-0973, RG7420) is an effective, selective, oral MEK1 inhibitor with an IC50 of 4.2 nM against MEK1.
M2915 PD 198306 PD 198306 is a cell-permeable and highly selective MEK inhibitor with IC50 of 8 nM.
M2316 BIX 02189 BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
M2177 BIX02188 BIX02188 is a novel specific inhibitor of MEK5 which inhibits catalytic function of purified, MEK5 enzyme.



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