I-CBP112

  • Chemical Properties
CAS No. 1640282-31-0 Cat. No. BCP20774
Name I-CBP112
Synonyms
Formula C27H36N2O5 M. Wt 468.59
  • Biological Activity
Description 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.
Pathways Epigenetics 
Targets Histone Acetyltransferase Epigenetic Reader Domain 

Structure

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