BAY-299 is an effecitve inhibitor of the bromodomain and PHD finger family member BRPF2 and the TATA box binding protein-associated factors TAF1 and TAF1L with IC50s of 67 nM, 8 nM, and 106 nM, respectively.

BRPF2 BD:67 nM, BRPF3 BD:5550 nM, BRPF1 BD:3150 nM, TAF1 BD2:8 nM, TAF1L BD2:106 nM

BAY-299 inhibits the cells proliferation of NCI-H526, CHL-1, MOLM-13, MV4-11, 769-P, Jurkat, and 5637 with GI50s of 6860, 7400, 1060, 2630, 3210, 3900, and 7980 nM, respectively. BAY-299 blocks the interaction of BRPF2 BD with H4 and H3.3 with IC50s of 575 and 825 nM, respectively[1].

The in vivo pharmacokinetic properties of BAY-299 in rats show are blood clearance is low (17% of hepatic blood flow), terminal half-life long to very long with t1/2 of 10 h, volume of distribution in steady-state high, and bioavailability high with F of 73%[1].