CBFβ Inhibitor Inhibitor (CAS 493028-20-9)

CBFβ Inhibitor is a cell-permeable thiazolyl compound that binds to PEBP2beta (CBFbeta) and allosterically disrupts CBFalpha/Runx1 binding to PEBP2beta (CBFbeta). CBFbeta Inhibitor cellular studies indicate a good correlation between the inhibitor′s antiproliferative activity and the Runx1 expression level in the target cells. Core binding factors (CBFs) represent heterodimeric transcription factors comprising a DNA-binding component known as CBFα (a RUNX protein) and an enhancer of binding called CBFβ. The CBFβ inhibitor is a compact molecule designed to bind with CBFβ, effectively impeding its interaction with Runx1 (with an IC50 value of 3.2 µM). This inhibition disrupts the CBFβ-Runx1 interactions specifically in ME-1 cells, which are acute myeloid leukemia cells characterized by dysfunctional CBF. This targeted action results in reduced proliferation of these cells without causing any toxicity. The CBFβ Inhibitor is an inhibitor that can permeate cell membranes and functions by binding to the core binding factor beta. Its synthesis involves a series of steps, commencing with the condensation of 4-methoxybenzaldehyde with ethyl acetoacetate to produce 5-Ethyl-2,4-dimethoxy-3-oxo-hex-2-enal. Subsequently, this compound undergoes a reaction with thiosemicarbazide to form the thiazole ring. Finally, the resulting thiazol-2-ylamine undergoes alkylation with ethyl bromide to introduce the ethyl group.