MEK2 Inhibitor

Hypothemycin, a fungal polyketide, is a multikinase inhibitor with K_is of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.

DS03090629 is an orally active, ATP-competitive MEK1/2 inhibitor. DS03090629 binds to the ATP-binding pocket of MEK, and this binding is unaffected by phosphorylation status. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with K_d values of 0.11 nM and 0.15 nM, respectively. DS03090629 inhibits the MEK1^F53L mutant while retaining activity relative to wild-type MEK1. DS03090629 suppresses the MAPK pathway, cell proliferation, and BRAF overexpression-mediated drug resistance in melanoma cells. DS03090629 can be used for research related to melanoma.

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.

(S)-N-trans-feruloyloctopamine is an isomer of N-trans-feruloyloctopamine (HY-N2232). N-trans-feruloyloctopamine is a natural hydroxycinnamic acid amide compound derived from garlic husk, possessing tyrosinase inhibitory, FGF2 inhibitory, anti-melanogenic, and anti-tumor activities, and is used in research related to hepatocellular carcinoma, pigmentation disorders, and UVB-induced skin damage.

RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC₅₀ of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research.

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.

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.

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.