| Cat.No. | Name | Information |
|---|---|---|
| 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). |
| M3626 | Cobimetinib (GDC-0973) | Cobimetinib (GDC-0973, RG7420) is an effective, selective, oral MEK1 inhibitor with an IC50 of 4.2 nM against MEK1. In addition, Cobimetinib is an inhibitor of Akt. |
| 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. |
| M1822 | PD98059 | PD98059 is a potent and selective inhibitor of mitogen-activated protein kinase kinase (MKK / MEK) with IC50 value of 2-7 μM. The expression of KAT2B protein in cells is significantly decreased after PD98059 inhibits ERK signaling pathway. |
| M1763 | Mirdametinib (PD0325901) | Mirdametinib (PD0325901) is a highly potent and selective MEK inhibitor with an IC50 in C26 cells of 0.33nM. |
| 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. |
| 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. |
| M1661 | AZD6244 | AZD6244 (ARRY-142886, Selumetinib) is a potent MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nM. |
| M27786 | U0126 | U0126 is a potent, non-ATP-competitive, selective inhibitor of MEK1 and MEK2 with IC50s of 72 nM and 58 nM, respectively.In addition, U0126 is an autophagy and mitophagy inhibitor and inhibits LPA-induced entosis. |
| 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. |
| 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. |
| M9014 | RO4987655 | RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM. |
| M7306 | SL 327 | SL 327 is a selective inhibitor of MEK1 and MEK2; brain penetrant. |
| 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. |
| 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. |
| 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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