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BET bromodomain inhibitor; blocks recruitment of BET to chromatin. Induces apoptosis and G0/G1 cell cycle arrest in MLL-fusion leukemic cell lines in vitro (IC50 values are 15, 26, 120 and 192 nM for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines respectively); reduces BCL2 expression in NOMO1 cells. Improves survival in two rodent models of MLL-fusion leukemia in vivo. Enhances differentiation of human iPSC into megakaryocytes. Also enhances fibroblast reprogramming to hiPSCs at low concentration.

Dawson et al (2011) Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature 478 529 PMID:21964340 |Feng et al (2014) Scalable generation of universal platelets from human induced pluripotent stem cells. Stem Cell Reports 3 817 PMID:25418726 |Shao et al (2016) Reprogramming by de-bookmarking the somatic transcriptional program through targeting of BET bromodomains. Cell Rep. 16 3138 PMID:27653680

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