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Core binding factors (CBFs) are heterodimeric transcription factors consisting of a DNA-binding CBFα component (a RUNX protein) and an enhancer of binding, CBFβ.1 CBF dimers have central roles in hematopoiesis and, when dysfunctional, in leukemias.1,2 CBFβ inhibitor is a small molecule that binds to CBFβ and inhibits its association with Runx1 (IC50 = 3.2 µM).3 It blocks CBFβ-Runx1 interactions in ME-1 cells, acute myeloid leukemia cells harboring dysfunctional CBF, reducing proliferation without toxicity.3
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1. Core binding factor at the crossroads: Determining the fate of the HSC. J. Cell. Physiol. 222(1), 50-56 (2010).
2. Hematopoietic stem cell emergence in the conceptus and the role of Runx1. Int. J. Dev. Biol. 54(6-7), 1151-1163 (2010).
3. Allosteric inhibition of the protein-