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DRUG:

CINelim (terameprocol)

i
Other names: EM-1421, Tetra-O-Methyl Nordihydroguaiaretic Acid, M4N
Associations
Trials
Company:
Erimos Pharma
Drug class:
Survivin inhibitor, CDK1 inhibitor, Sp1 inhibitor
Associations
Trials
3ms
Molecular Insights into the Anticancer Activity of Withaferin-A: The Inhibition of Survivin Signaling. (PubMed, Cancers (Basel))
Several Survivin inhibitors, including YM-155, Debio1143, EM1421, LQZ-7I, and TL32711, have emerged as potential anticancer drugs awaiting validation in clinical trials. Furthermore, Wi-AREAL treatment activated apoptosis signaling, as evidenced by reduced PARP-1 and Bcl-2 levels, increased procaspase-3, and elevated Cytochrome C. Additionally, treating cells with a nontoxic low concentration (0.01%) of Wi-AREAL inhibited migration and invasion, as well as EMT (epithelial-mesenchymal transition) signaling. By combining computational and experimental approaches, we demonstrate the potential of Wi-A and Wi-AREAL as natural inhibitors of Survivin, which may be helpful in cancer treatment.
Journal • PARP Biomarker • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • BIRC5 (Baculoviral IAP repeat containing 5) • CASP3 (Caspase 3) • CDK1 (Cyclin-dependent kinase 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
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birinapant (IGM-9427) • xevinapant (Debio 1143) • CINelim (terameprocol)
over1year
Tetra-O-methyl-nordihydroguaiaretic acid inhibits energy metabolism and synergistically induces anticancer effects with temozolomide on LN229 glioblastoma tumors implanted in mice while preventing obesity in normal mice that consume high-fat diets. (PubMed, PLoS One)
Tetra-O-methyl-nordihydroguaiaretic acid (terameprocol; M4N), a global transcription inhibitor, in combination with a second anticancer drug induces strong tumoricidal activity and has the ability to suppress energy metabolism in cultured cancer cells...Meanwhile, the ability of M4N to suppress energy metabolism prevented obesity in mice consuming HF diets, indicating that M4N has beneficial effects on normal tissues. The dual ability of combination treatment with M4N to suppress both energy metabolism and oncometabolites shows that it is potentially an effective therapy for cancer.
Preclinical • Journal
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LDHA (Lactate dehydrogenase A) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • ATF4 (Activating Transcription Factor 4) • NAMPT (Nicotinamide Phosphoribosyltransferase) • TCF4 (Transcription Factor 4)
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temozolomide • CINelim (terameprocol) • terameprocol oral (EM-1421 oral)