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首页-小分子抑制剂&激动剂-Epigenetics-Histone Acetyltransferase (HAT)-CPTH6 hydrobromide
CPTH6 hydrobromide

Chemical Structure : CPTH6 hydrobromide

CAS No.: 2321332-57-2

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CPTH6 hydrobromide (Gcn5/pCAF inhibitor)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 386.736
    分子式 C15H17BrClN3S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

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

    参考文献

    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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