2,4(1H,3H)-Pyrimidinedione, 3-[4-chloro-3-(2-methylphenoxy)-1-naphthalenyl]-6-(trifluoromethyl)-, (3S)-

Uses

BAY-252 is a potent branched-chain amino acid transaminases 1 (BCAT1) and BCAT2 inhibitor with IC50s of 2 μM and 2 μM, respectively. BAY-069 also can be used as a chemical probe. BAY-069 can be used for the research of cancer[1].

Biological Activity

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.

References

[1] BCAT team. Dual BCAT1/2 Probe BAY-069. June, 2th 2020.