Description
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.
Uses
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].
References
[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
