BAY-069 (BAY069) is a potent, selective branched-chain amino acid transaminase BCAT1/2 inhibitor with IC50 of 31/153 nM, respectively.
BAY-069 is highly selective for BCAT1/2, and shows no activity against aspartate transaminases (GOT1 and GOT2, glutamate-oxaloacetate transaminase, IC50>50 μM), also is inactive against an protease panel (30 proteases) and kinase panel (30 kinases).
BAY-069 increases cellular branched-chain amino acid (BCAA) in tumor cell lines (U-87 MG and MDA-MB-231) with IC50 of 358 and 874 nM, respectively.
BAY-069 does not inhibit cell proliferation of U-87 MG (high BCAT1 expression) and MDA-MB-231 (high BCAT2 expression) cells.
BAY-069 is a valuable tool to better understand the biology and pharmacology of BCAT inhibition in the field of tumor metabolism.
