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首页-小分子抑制剂&激动剂-Epigenetics-Histone Acetyltransferase (HAT)-iP300w
iP300w

Chemical Structure : iP300w

CAS No.: 1889284-33-6

iP300w (CP-C27, CBP and p300 inhibitor compound 27)

货号: PC-73089Not For Human Use, Lab Use Only.

iP300w (CP-C27) is a potent, selective, orally bioavailable inhibitor of p300/CBP histone acetyltransferases with IC50 of 19 nM (p300), H3K27Ac EC50 of 5 nM, does not inhibitor other HATs.

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

    生物&药学活性

    iP300w (CP-C27) is a potent, selective, orally bioavailable inhibitor of p300/CBP histone acetyltransferases with IC50 of 19 nM (p300), H3K27Ac EC50 of 5 nM, does not inhibitor other HATs.
    iP300w is a potent p300/CBP inhibitor, inhibits p300-mediated H3K9 acetylation with IC50 of 33 nM in HTRF assay.
    iP300w diminishes DUX4-induced toxicity and inhibits DUX4-mediated transcription.
    iP300w blocks DUX4-induced H3 acetylation and prevents the increase in expression of DUX4 target genes, erases the DUX4-mediated transcriptional fingerprint in FSHD myoblasts.
    iP300w impairs DUX4-mediated transcription in vivo in the iDUX4pA FSHD mouse model.

    物理化学性质&存储条件

    分子量 618.565
    分子式 C29H27F5N6O4
    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

    (1'S,3'R)-3'-Fluoro-N-[(4-fluorophenyl)methyl]-2',3'-dihydro-5'-[1-[2-(methylamino)-2-oxoethyl]-1H-pyrazol-4-yl]-2,5-dioxo-N-[(1S)-2,2,2-trifluoro-1-methylethyl]spiro[imidazolidine-4,1'-[1H]indene]-1-acetamide

    参考文献

    1. Bosnakovski D, et al. Sci Adv. 2019 Sep 11;5(9):eaaw7781.

    2. Bosnakovski D, et al. Oncogenesis. 2021 Oct 12;10(10):68.

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