IACS-16559

IACS-16559 is a potent and selective small molecule inhibitor of the CREBBP (CBP) and EP300 (p300) bromodomains. Developed by the Institute for Applied Cancer Science (IACS) at The University of Texas MD Anderson Cancer Center, it is designed to disrupt the transcriptional programs hijacked by aberrant factors in specific leukemias. Preclinical studies have demonstrated its efficacy in acute myeloid leukemia (AML) models, particularly those characterized by MLL rearrangements or NPM1 mutations. Unlike many cytotoxic agents, IACS-16559 does not primarily induce apoptosis but instead promotes differentiation and growth arrest. It has also shown synergistic potential when combined with Menin-MLL inhibitors.