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IRBM6

Chemical Structure : IRBM6

CAS No.: 1561819-01-9

IRBM6 (Class I HDAC-IN-6)

Catalog No.: PC-72886Not For Human Use, Lab Use Only.

IRBM6 (Class I HDAC-IN-6) is a potent, class I selective HDAC inhibitor with EC50 of 50 nM (HeLa cellular), HDAC1/2/3 IC50 of 1.7/2.8/1.1 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    IRBM6 (Class I HDAC-IN-6) is a potent, class I selective HDAC inhibitor with EC50 of 50 nM (HeLa cellular), HDAC1/2/3 IC50 of 1.7/2.8/1.1 nM.
    IRBM6 weakly inhibits HDAC6 (IC50=177 nM) and is inactive at 5 uM against HDACs 4-7.
    IRBM6 showed a potent inhibitory effect on the growth TC-797s and two additional NUT carcinoma (NC) cell lines, PER-403, and 10-15.
    IRBM6 induces a transcriptional program of differentiation in NC cells, demonstrated large-scale changes in gene expression that were significantly enriched with differentiation gene sets and depleted of pro-growth gene sets, including those of MYC and E2F targets.
    IRBM6 repressed growth and induced differentiation of NUT carcinoma (NC) cells in proportion to inhibition of NUT transcriptional activity.

    Physicochemical Properties

    M.Wt 478.593
    Formula C27H34N4O4
    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

    (S)-N-(1-(5-(2-methoxyquinolin-3-yl)oxazol-2-yl)-7-oxononyl)-1-methylazetidine-3-carboxamide

    References

    1. Alberto Bresciani, et al. ACS Med Chem Lett. 2018 Nov 27;10(4):481-486.

    2. Hitoshi Shiota, et al. Mol Cancer Res. 2021 Nov;19(11):1818-1830.

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