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Diazepinomicin

Chemical Structure : Diazepinomicin

CAS No.: 733035-26-2

Diazepinomicin (TLN 4601, ECO-4601)

Catalog No.: PC-62205Not For Human Use, Lab Use Only.

Diazepinomicin (TLN 4601, ECO-4601) is a brain penetrant inhibitor of Ras-RAF-MAPK pathway post Ras prenylation and prior to MEK activation, binds the central and/or peripheral benzodiazepine receptors (PBR, TSPO).

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    Biological Activity

    Diazepinomicin (TLN 4601, ECO-4601) is a brain penetrant inhibitor of Ras-RAF-MAPK pathway post Ras prenylation and prior to MEK activation, binds the central and/or peripheral benzodiazepine receptors (PBR, TSPO).
    Diazepinomicin prevents EGF-induced phosphorylation of Raf-1, MEK, and ERK1/2.
    Diazepinomicin reduces Ras-GTP levels and induces apoptosis.
    Diazepinomicin shows antitumor activity and decreases tumor Raf-1 protein levels in MIA PaCa-2 tumor-bearing mice.

    Physicochemical Properties

    M.Wt 462.58
    Formula C28H34N2O4
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    4,6,8-trihydroxy-10-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one

    References

    1. Campbell PM, et al. J Mol Signal. 2010 Nov 2;5:18.

    2. Quah SY, et al. Pharmacol Ther. 2016 Jun;162:35-57.

    3. Boufaied N, et al. Anticancer Drugs. 2010 Jun;21(5):543-52.

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