63053-14-5

AI-4-57 Hydrochloride is a ligand to the CBF? portion of the CBF?-SMMHC fusion protein. AI-4-57 Hydrochloride inhibits its binding to the Runt domain of RUNX proteins, and is also a modest potency inhibitor of the binding of wildtype CBF? to the RUNX1 Runt domain.

AI-4-57 is an allosteric inhibitor for CBFβ SMMHC-RUNX1 (core binding factor β and the smooth-muscle myosin heavy chain) interaction with an IC50 of 22 μM[1].

[1] Illendula A, et al., A small-molecule inhibitor of the aberrant transcription factor CBFβ-SMMHC delays leukemia in mice. Science. 2015 Feb 13;347(6223):779-84. DOI:10.1126/science.aaa0314