I-CBP112 hydrochloride

Description: I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. 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. Target: Epigenetic Reader Domain. Smiles: O(C[C@@H]1CN(C)CCC1)C2=C3C(=CC(=C2)C4=CC(OC)=C(OC)C=C4)CN(C(CC)=O)CCO3.Cl. References: Zucconi BE, et al. Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain LigandI-CBP112. Biochemistry. 2016 Jul 12,55(27):3727-34.