493028-20-9

Core binding factors (CBFs) are heterodimeric transcription factors consisting of a DNA-binding CBFα component (a RUNX protein) and an enhancer of binding, CBFβ. CBF dimers have central roles in hematopoiesis and, when dysfunctional, in leukemias. CBFβ inhibitor is a small molecule that binds to CBFβ and inhibits its association with Runx1 (IC₅₀ = 3.2 μM). It blocks CBFβ-Runx1 interactions in ME-1 cells, acute myeloid leukemia cells harboring dysfunctional CBF, reducing proliferation without toxicity.

Core binding factors (CBFs) are heterodimeric transcription factors consisting of a DNA-binding CBFα component (a RUNX protein) and an enhancer of binding, CBFβ. CBF dimers have central roles in hematopoiesis and, when dysfunctional, in leukemias. CBFβ inhibitor is a small molecule that binds to CBFβ and inhibits its association with Runx1 (IC50 = 3.2 μM). It blocks CBFβ-Runx1 interactions in ME-1 cells, acute myeloid leukemia cells harboring dysfunctional CBF, reducing proliferation without toxicity.

[1] KEVIN A. LINK  James C M  Fu Sheng Chou. Core binding factor at the crossroads: Determining the fate of the HSC?[J]. Journal of Cellular Physiology, 2009, 222 1: 50-56. DOI: 10.1002/jcp.21950
[2] GEMMA SWIERS  Nancy A S  Marella de Bruijn. Hematopoietic stem cell emergence in the conceptus and the role of Runx1.[J]. International Journal of Developmental Biology, 2010, 54 6-7: 1151-1163. DOI: 10.1387/ijdb.103106gs
[3] MICHAEL J GORCZYNSKI. Allosteric inhibition of the protein-protein interaction between the leukemia-associated proteins Runx1 and CBFbeta.[J]. Chemistry & biology, 2007, 14 10: 1186-1197. DOI: 10.1016/j.chembiol.2007.09.006