MEK1 Inhibitor

KZ-02 is an orally active dual MEK1/Pim-1 kinase inhibitor, with an IC₅₀ of 1.07 nM against MEK1 and an IC₅₀ of 1.34 μM against Pim-1. KZ-02 reduces the phosphorylation levels of ERK and Cdc25C, and promotes the proteasomal degradation of Pim-1 protein. KZ-02 inhibits cancer cell growth and exerts anti-tumor effects. KZ-02 can be used in the research of colorectal cancer.

MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC₅₀ values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines.

MEK-IN-10 is an orally active pan-MEK/RAF non-degrading molecular glue with an IC₅₀ of 782 nM against human MEK1. MEK-IN-10 blocks the phosphorylation of MEK and ERK, induces and stabilizes the MEK1-RAF complex, and disrupts the RAS-MAPK signaling pathway. MEK-IN-10 induces apoptosis in cancer cells and arrests cells at the G0/G1 phase. MEK-IN-10 induces tumor growth inhibition in mouse xenograft models. MEK-IN-10 can be used in the research of RAS-driven cancers, such as colorectal cancer and pancreatic cancer.

(E/Z)-Chk2-IN-1 ((E/Z)-Hymenialdisine analogue-1) (Compound 1) is a potent and selective cell cycle kinase Chk2 inhibitor with an IC₅₀ of 8 nM. (E/Z)-Chk2-IN-1 exhibits low inhibitory activity against other kinases (such as CK1δ, MEK1, and PKCα/βⅡ) with IC₅₀ values both >89 nM. (E/Z)-Chk2-IN-1 can be used for the research of cancer.

MEK4 IN-4 is a MEK4 inhibitor (IC₅₀ = 0.041 μM) that inhibits the kinase catalytic activity of MEK4 via competitive blockade of ATP binding. MEK4 IN-4 can be used to investigate cell proliferative diseases and disorders associated with MEK4 activity, including cancer.

Isorhamnetin (Standard) is the analytical standard of Isorhamnetin. This product is intended for research and analytical applications. Isorhamnetin is a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L.. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and PI3K.

MEK1-IN-1 (Compound M15) is a MEK1 inhibitor with an IC₅₀ of 10.29 nM. MEK1-IN-1 can inhibit the proliferation and migration, induce apoptosis of tumor cells. MEK1-IN-1 has good liver microsomal stability. MEK1-IN-1 can be used for the research of solid tumors.

GIT1-IN-1 is an inhibitor of ARF GTPase-activating protein 1 (GIT1) with a K_D of 6.2 μM. GIT1-IN-1 induces apoptosis (apoptosis) in liver and colon cancer cells, arrests the cell cycle at the G2/M phase, and inhibits cell proliferation, colony formation and migration. GIT1-IN-1 inhibits the activities of MEK and ERK, reduces the expression level of cyclin D1, and stabilizes cyclin B1 protein in liver and colon cancer cells. GIT1-IN-1 can be used in the research of liver cancer and colon cancer.

MEK ligand-2, a MEK1 and MEK2 inhibitor, is a ligand for target protein for PROTAC of MS934 (HY-153863). MS934 is a VHL-recruiting MEK 1/2 PROTAC degrader.

ST-168 is an orally active MEK/PI3K inhibitor with an IC₅₀ of 182 nM against MEK1 and IC₅₀ values ​​of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research.

Nuvrumetinib (PAS-004) is a macrocyclic MEK inhibitor. Nuvrumetinib functionally inhibits MEK1/2, thereby suppressing pERK in tumors. Nuvrumetinib inhibits the proliferation of NRAS-mutant cancer cells. Nuvrumetinib can be used in studies related to NRAS^G12C-mutant solid tumors, neurofibromatosis type 1 (NF1), RASopathies and laminopathies.

CI-1040 (PD 184352) hydrochloride is an orally active, highly specific inhibitor of MEK, with an IC₅₀ of 17 nM for MEK1.

G-963 is an allosteric inhibitor of mitogen-activated protein kinase kinase (MEK) with a MEK1 IC₅₀ of 0.012 μM. G-963 interacts with Ser212 of MEK and exhibits potent antiproliferative activity against HCT116 colon cancer cells (EC₅₀ = 0.120 μM) and A375 melanoma cells (EC₅₀ = 0.025 μM). G-963 can be used for the research of colon cancer, melanoma.

Lixisenatide (Leu-¹³C₆,¹⁵N) TFA is the ¹³C- and ¹⁵N-labeled Lixisenatide (HY-P0119). Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis.

CInQ-03 is an allosteric inhibitor of MEK1/2, with IC₅₀ values of 5 μM and 10 μM against MEK1 and MEK2, respectively. CInQ-03 inhibits the kinase activity of MEK1/2 and reduces the phosphorylation levels of downstream ERK1/2 and RSK. CInQ-03 suppresses both anchorage-dependent and anchorage-independent growth of colon cancer cells, the activity of AP-1 reporter gene in colon cancer cells, as well as EGF-induced growth, transformation and AP-1 reporter gene activity in HaCaT keratinocytes. CInQ-03 can be used in studies related to colon cancer.