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Message: CG-13250

http://www.sciencedirect.com/science/article/pii/S0006291X17301389

CG13250, a novel bromodomain inhibitor, suppresses proliferation of multiple myeloma cells in an orthotopic mouse model

  • a Department of Clinical and Translational Physiology, Kyoto Pharmaceutical University, Kyoto, Japan
  • b ConverGene LLC, Gaithersburg, MD, USA
  • c Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, USA
  • d Department of Clinical Oncology, Kyoto Pharmaceutical University, Kyoto, Japan
 
Received 12 January 2017, Accepted 18 January 2017, Available online 20 January 2017
 
 
•  A novel bromodomain inhibitor CG13250 suppresses MM cell proliferation.•  CG13250 decreases C-MYC expression, resulting in the induction of apoptosis.•  CG13250 prolongs the survivals of MM-bearing mice.In text: JQ-1 [12] and I-BET762 [13] were the first BET inhibitors to be described and these compounds suppress MM cell proliferation [14] ;  [15]. Other BET inhibitors described to date include PFI-1, RVX-208, and OTX015 [9] ;  [16]. By conducting chemical screening against BRD4 and subsequent chemical optimization, we developed a novel bromodomain inhibitor CG13250. Unlike previously described BET inhibitors, it has a quinolinone core and displayed high affinity and specificity to BET proteins. In this study, we investigated the inhibitory effects of CG13250 on the proliferation of MM cells.

Didn't see Zen-3694 mentioned in this one, though.

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