Chemical Properties | Back Directory | [density ]
1.450±0.06 g/cm3(Predicted) | [storage temp. ]
-70°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
6.02±0.40(Predicted) | [color ]
Off-white to light yellow |
Hazard Information | Back Directory | [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 kinases30 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 nMrespectively) with good pharmacokinetics and oral bioavailability in rats in vivo. | [References]
[1] BCAT team. Dual BCAT1/2 Probe BAY-069. June, 2th 2020. |
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Company Name: |
Merck KGaA
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Tel: |
21-20338288 |
Website: |
www.sigmaaldrich.cn |
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