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CPTH6 hydrobromide

Chemical Structure : CPTH6 hydrobromide

CAS No.: 2321332-57-2

CPTH6 hydrobromide (Gcn5/pCAF inhibitor)

Catalog No.: PC-35321Not For Human Use, Lab Use Only.

CPTH6 hydrobromide is a thiazole derivative that can reduce histone acetylation and histone acetyltransferase (HAT) activity in human leukemia cells, CPTH6 is a specific Gcn5/pCAF inhibitor.

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

    Biological Activity

    CPTH6 hydrobromide is a thiazole derivative that can reduce histone acetylation and histone acetyltransferase (HAT) activity in human leukemia cells, CPTH6 is a specific Gcn5/pCAF inhibitor.
    CPTH6 exerts a significant inhibitory effect on HAT activity of both pCAF and Gcn5, whereas it does not affect p300 and CBP HAT activity.
    CPTH6 decrease acetylation of histone H3 specifically at lysine 18 in a dose-dependent fashion, does not affect H3 histone methylation at lysines 9 and 4.
    CPTH6 induces cell-cycle perturbation and apoptosis in AML cells, induces differentiation in AML and neuroblastoma cells。
    CPTH6 impairs autophagy and reduces autophagosome turnover through an impairment of their degradation pathway.

    Physicochemical Properties

    M.Wt 386.736
    Formula C15H17BrClN3S
    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

    (E)-4-(4-chlorophenyl)-2-(2-(3-methylcyclopentylidene)hydrazinyl)thiazole hydrobromide

    References

    1. Trisciuoglio D, et al. Clin Cancer Res. 2012 Jan 15;18(2):475-86.

    2. Ragazzoni Y, et al. Cell Death Dis. 2013 Mar 7;4:e524.

    3. Di Martile M, et al. Oncotarget. 2016 Mar 8;7(10):11332-48.

    4. Chimenti F, et al. J Med Chem. 2009 Jan 22;52(2):530-6.

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