Drug intelligence / Profile preview

dehydroxymethylepoxyquinomicin

Development stage
Preclinical
Lead developer
Keio University
Modality
Small Molecules
Administration
Intraperitoneal (preclinical/research Context)
01

Overview

Dehydroxymethylepoxyquinomicin (DHMEQ) is a synthetic small molecule that acts as a selective inhibitor of the transcription factor nuclear factor kappa B (NF-κB), a protein complex central to inflammatory signaling and survival in various diseases including cancer and inflammatory conditions. DHMEQ is derived from the structure of the antibiotic epoxyquinomicin C and inhibits NF-κB activation by binding covalently to specific cysteine residues of RelA (p65) and RelB subunits, thereby preventing their translocation to the nucleus and subsequent gene activation. DHMEQ has demonstrated anti-inflammatory and anti-neoplastic activity in various preclinical models, showing efficacy in ameliorating asthma, suppressing glioblastoma cell proliferation, and reducing inflammatory cytokine production in activated cells. It is primarily being investigated as a research tool and for potential therapeutic development against inflammation-driven diseases, cancer, and immune-related pathologies[1][4][5][7].

Other names
(-)-DHMEQ(+)-DHMEQepoxyquinomicin C derivative
02

Targets

RELB (Nuclear factor kappa-light-chain-enhancer of activated B cells subunit RelB)RELA (Nuclear Factor Kappa B Subunit p65)

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