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首页-小分子抑制剂&激动剂-Epigenetics-Histone Acetyltransferase (HAT)-DS-9300
DS-9300

Chemical Structure : DS-9300

CAS No.: 2259641-46-6

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DS-9300 (DS9300)

货号: PC-49530Not For Human Use, Lab Use Only.

DS-9300 (DS9300) is a highly potent, selective and orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with IC50 of 28 nM, inhibits cellular acetylation of histone H3K27 (H3K27Ac) with IC50 of 54 nM.

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

    生物&药学活性

    DS-9300 (DS9300) is a highly potent, selective and orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with IC50 of 28 nM, inhibits cellular acetylation of histone H3K27 (H3K27Ac) with IC50 of 54 nM.
    DS-9300 inhibits VCaP cell growth with GI50 of 0.6 nM, and DS-9300 (3 mg/kg, once daily, oral) demonstrated potent antitumor effects in a castrated VCaP xenograft mouse model without significant body weight loss.

    物理化学性质&存储条件

    分子量 501.510
    分子式 C25H26F3N5O3
    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

    (2R,4R)-1-(4,4-difluoro-1-(4-methoxyphenyl)cyclohexane-1-carbonyl)-4-fluoro-N-(1H-pyrazolo[4,3-b]pyridin-5-yl)pyrrolidine-2-carboxamide

    参考文献

    1. Kanada R, et al. J Med Chem. 2022 Dec 26. doi: 10.1021/acs.jmedchem.2c01641.

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