2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
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.
