bcat1

ERG240 is an inhibitor of branched-chain amino acid aminotransferase 1 (BCAT1). ERG240 can be used for the research of rheumatoid arthritis, cancer, and bone disease.

Gue1654 is a selective OXE-R inhibitor that attenuates coronary artery ligation-induced ischemic myocardial injury and cardiomyocyte oxygen glucose deprivation-induced injury in mice through activation of BCAT1.Gue1654 inhibits OXE-R-inhibited protein kinase C-ε (PKC-ε) nuclear factor κB (NF-κB) signaling and apoptosis in cardiomyocytes. Gue1654 can be used to study cardiovascular disease.

BCATc Inhibitor 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. BCATc Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective e

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.

BAY-771 is a negative control of BAY-069, BAY-069 is a BCAT1 2 Inhibitor and Chemical Probe. BAY-069 displays high cellular activity and very good selectivity. BAY-069 displays high cellular activity. Its overall in vivo pharmacokinetic profile and its selectivity in various in vitro panels suggest that BAY-069 is suitable for in vivo experiments.

BAY-252 is a potent inhibitor of branched-chain amino acid transaminases 1 (BCAT1) and BCAT2, demonstrating inhibitory concentration (IC50) values of 2 μM for both enzymes. Additionally, BAY-069 serves as a chemical probe and is applicable in cancer research [1].

WQQ-345, a BCAT1 inhibitor, exhibits an IC50 of 10.8 mM. In 67R cells, it reduces α-KG levels and upregulates H3K27me3 expression while downregulating the expression of glycolytic enzymes (PFKP and LDHA), leading to impaired glycolytic activity. Additionally, WQQ-345 demonstrates tumor-suppressive activity in a 67R subcutaneous xenograft model.

ERG245, a BCAT1 inhibitor, specifically targets BCAT1 activity to enhance oxidative phosphorylation (OXPHOS) in CD8+ T cells, boosting their cytotoxicity. Additionally, when used alongside Pembrolizumab (anti-PD-1), ERG245 aids in promoting tumor regression. This compound is valuable in immuno-oncology research.