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.

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.

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.

BAY-771 is a negative control and structural analog of BAY-069, exhibiting high permeability in Caco-2 cells with minimal inhibitory activity against BCAT1 and no activity against BCAT2. BAY-069 is a BCAT1/2 inhibitor and chemical probe for studying cancer and branched-chain amino acid metabolism.

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-252 is a potent inhibitor of branched-chain amino acid transaminases 1 (BCAT1) and BCAT2, with IC50 of 2 μM for both enzymes. In addition to its inhibitory properties, BAY-252 serves as a chemical probe in cancer research, aiding in the investigation of metabolic pathways involving branched-chain amino acids.

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 is a BCAT1 inhibitor that promotes oxidative phosphorylation (OXPHOS) in CD8+ T cells by selectively inhibiting the enzymatic activity of BCAT1, thereby increasing the cytotoxic capacity of CD8+ T cells. ERG245, when administered in combination with the anti-PD-1 antibody Pembrolizumab, induces tumor regression in preclinical settings, and it can be used as a research agent within the field of immuno-oncology.