化合物I-CBP112 hydrochloride T4247

Product Introduction
Bioactivity


英文名: I-CBP112 hydrochloride

描述: I-CBP112 hydrochloride 是含溴结构域转录因子的选择性抑制剂，靶向 CBP/p300 溴结构域。在体内外，它以剂量依赖性方式显着降低 MLL-AF9(+) 急性髓细胞白血病细胞的白血病起始潜力，还增加 BET 溴结构域抑制剂 JQ1 以及阿霉素的细胞毒活性。

体外活性: I-CBP112 markedly increases acetylation by p300 at the histone H3K18 and H3K23 sites. I-CBP112 stimulated H3K18ac by ~3-fold, and induced enhances acetylation of these same sites by CBP as well as at H4K5. The EC50s of activation of I-CBP112 on CBP- and p300-mediated H3K18 acetylation are ~2 μM[1]. In mouse and human leukemia cell lines, I-CBP112 causes substantially impaired colony formation and induces cellular differentiation without significant cytotoxicity. In BioMAP primary cell panel, I-CBP112 results in a unique response on cytokine and marker protein expression[2].

体内活性: I-CBP112 markedly and dose-dependently reduces the leukemia-initiating potential of mLL-AF9+ AmL cells in vitro and in vivo. The synergistic effects of I-CBP112 and current standard therapy (doxorubicin), as well as emerging treatment strategies (BET inhibition), provide new possibilities for combinatorial treatment of leukemia and potentially other cancers[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (118.8 mM)


关键字: inhibit | Inhibitor | I CBP112 hydrochloride | I-CBP 112 Hydrochloride | I-CBP-112 hydrochloride | I-CBP112 | I-CBP112 Hydrochloride | I-CBP-112 Hydrochloride | ICBP112 hydrochloride | Epigenetic Reader Domain

相关产品: J-147 | TPOP146 | RVX-297 | BRD4 Inhibitor-20 | BRD4-BD1-IN-2 | Hexamethylene bisacetamide | GNE-207 | DBr-1 | BY27 | 666-15

相关库: Transcription Factor-Targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Epigenetics Compound Library | Hematonosis Compound Library | PPI Inhibitor Library | Histone Modification Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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