BAY-069 is an inhibitor. BAY-069 inhibited branched-chain amino acid transaminase 1 (BCAT1) at IC50:31 nM and branched-chain amino acid transaminase 2 (BCAT2) at IC50:153 nM. BAY-069 is a novel (trifluoromethyl) pyrimidine dione chemical probe, which can be used for anticancer research.

BCAT1:31 nM, BCAT2:153 nM

BAY-069, inhibits the proliferation of U-87 and MDA-MB-231 cells. The compound is tested at concentrations ranging from 70 nM to 50 μM, with a duration of 72 hours. In U-87 cells, the IC50 is determined to be 358 nM, while in MDA-MB-231 cells, the IC50 is 874 nM [1].

BAY-069 demonstrates high metabolic stability when incubated with human liver microsomes, with a blood clearance of 0.11 L/h/kg. It also shows moderate metabolic stability when incubated with rat hepatocytes, with a blood clearance of 1.8 L/h/kg. BAY-069 exhibits high permeability through Caco-2 cell monolayers without any signs of efflux [1].