I-CBP112 hydrochloride is a selective inhibitor of CBP and EP300, acting through direct binding to their bromodomains with dissociation constants of 142 nM and 625 nM, respectively. This compound has been shown to significantly diminish the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells both in vitro and in vivo, demonstrating dose-dependent efficacy. Additionally, I-CBP112 enhances the cytotoxic effects of the BET bromodomain inhibitor JQ1 and doxorubicin, making it a valuable tool for research in cancer therapeutics and epigenetic regulation.
I-CBP112 hydrochloride is a selective inhibitor of CBP and EP300, acting through direct binding to their bromodomains with dissociation constants of 142 nM and 625 nM, respectively. This compound has been shown to significantly diminish the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells both in vitro and in vivo, demonstrating dose-dependent efficacy. Additionally, I-CBP112 enhances the cytotoxic effects of the BET bromodomain inhibitor JQ1 and doxorubicin, making it a valuable tool for research in cancer therapeutics and epigenetic regulation.
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