BAY-069 is a non-cytotoxic (anti-proliferation IC50 >47 μM using 6 cell lines), potent and selective branched chain amino acid (BCAA) transaminase (BCAT) inhibitor (BCAT1/2 IC50 = 27/130 nM; glutamic-oxaloacetic transaminase GOT1/2 IC50 >50 μM) with good selectivity over a panel of 30 kinases, 30 proteases and 77 other targets. BAY-069 upregulates BCAAs in high BCAT1-expressing U-87 MG and high BCAT2-expressing MDA-MB-231 (IC50 = 358 and 874 nM, respectively) with good pharmacokinetics and oral bioavailability in rats in vivo.
