BAY-184 is a potent, selective and in vivo-active KAT6A/B inhibitor with IC50 of 71/83 nM respectively.
BAY-184 displays an overall good selectivity, with high selectivity against the close members of the MYST family, with only a residual low micromolar activity for KAT7 (11-fold), and with no activity against the more distantly related histone acetyltransferase p300 (IC50 > 10 μM).
BAY-184 also shows high selectivity against a full kinase panel at a concentration of 10 μM (366 kinases) at Eurofins.
BAY-184 (1 uM) elicited a swift decline in H3K23ac levels in ZR-75-1 cells, shows IC50 of 670 nM for H3K23 acetylation in HTRF assays, and IC50 of 168 nM in ER target gene reporter assay.
BAY-184 inhibits cell growth of ZR-75-1 breast cancer cells with IC50 of 130 nM, shows IC50 values of <1 uM against ER-positive breast cancer subtypes.
BAY-184 (50-150 mg/kg, po, twice daily (2 qd)) induced a dose-dependent inhibition of tumor growth in ZR-75-1 xenografts.