MEK1/2

A neuropeptide with diverse biological activities

Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM.

PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader.

MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.

MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2.

GSK1790627 is the N-deacetylated metabolite of Trametinib. Trametinib is an orally active MEK inhibitor that activates autophagy and induces cell apoptosis.

Trametiglue is a derivative of Trametinib that binds to KSR-MEK and RAF-MEK with unprecedented potency and selectivity through a unique interface interaction.

3-droxy-4-carboxyalkylamidino-5-arylamino-isothiazoles is an inhibitor for bone morphogenetic protein 2 (BMP2) with an IC50 of 2.2 μM.

MEK-IN-6 (Example 69) is a MEK inhibitor.

MS934 is a novel improved VHL-recruiting MEK 1/2 degrader.

NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation.

SHY-867 is a pan RAS inhibitor.

SHY-855 is a pan RAS inhibitor.

KRAS G12D-IN-30 (Compound 4) is a KRAS inhibitor.

HDB-1 is a selective inhibitor of the P2Y14 receptor ( P2Y14R ) with an IC 50 of 26 pM.

KZ-02 is an orally active dual MEK1 / Pim-1 kinase inhibitor, with an IC 50 of 1.07 nM against MEK1 and an IC 50 of 1.34 μM against Pim-1.

IK-595 is a MEK1/MEK2 inhibitor with high affinity (7.39 nM).IK-595 blocks EGF-induced ERK1/2 phosphorylation in AsPC-1 cells with IC 50 value of 0.1 nM.

Hexestrol -d 4 is the deuterium labeled Hexestrol.

PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex.

APS-2-79 (Standard) is the analytical standard of APS-2-79.

Nedometinib is a MEK1 inhibitor (IC50 = 135 nM).

Isorhamnetin is a flavonoid compound extracted from the traditional Chinese medicine Hippophae rhamnoides L., possessing various biological activities including antioxidant, anti-inflammatory, anticancer, and neuroprotective effects.

Arctigenin,a natural lignan compound,has demonstrated anticancer activities in cancer. Arctigenin exhibits potent antioxidant, anti-inflammatory and antiviral (influenza A virus) activities.

MEK allosteric site inhibitor