I-CBP112
CAS号 | 1640282-31-0 | 货号 | BCP20774 |
中文名 | I-CBP112 | ||
英文名 | I-CBP112 | ||
中文别名 | |||
英文别名 | |||
分子式 | C27H36N2O5 | 分子量 | 468.59 |
生物活性 | I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.142 and 0.625 μM, respectively). I-CBP112 has little activity against other bromodomains at concentrations up to 1 mM. I-CBP112 targets the CBP/p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. Interestingly, I-CBP112 increased the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin. | ||
信号通路 | Epigenetics | ||
靶 点 | Histone Acetyltransferase Epigenetic Reader Domain |
结构式
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