AK-2292 (AK2292) is a first, potent and selective small-molecule degrader of both STAT5A (Ki=210 nM) and STAT5B (Ki=308 nM) isoforms.
AK-2292 effectively induces degradation of STAT5A, STAT5B, and phosphorylated STAT5 proteins in a concentration- and time-dependent manner in acute myeloid leukemia (AML) cell lines.
AK-2292 demonstrates excellent degradation selectivity for STAT5 over all other STAT members.
AK-2292 exerts potent and specific cell growth inhibitory activity in AML cell lines with high levels of phosphorylated STAT5.
AK-2292 effectively induces STAT5 depletion in normal mouse tissues and human chronic myeloid leukemia (CML) xenograft tissues and achieves tumor regression in CML xenograft mouse models.
