CB-839
Glutaminase inhibitor / CB-839 is a potent (IC50 = 24 nM), selective and orally bioavailable inhibitor of glutaminase (KGA and GAC).1 CB-839 displayed an antiproliferative effect in the triple-negative breast cancer cell line, HCC-1806, but no activity in the estrogen receptor-positive cell line T47D. CB-839 was able to cause proliferation arrest and apoptosis in acute myeloid leukemia cells without causing cytotoxicity against normal human CD34(+) progenitors.2 Aspartate-glutamate carrier 1 (AGC1) inhibition can synergize with CB-839 to limit tumor growth.3
Biochemicals & reagents
1439399-58-2
Telaglenastat
1) Gross et al. (2014), Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer; Mol. Cancer Ther.,13 890 2) Jacque et al. (2015), Targeting glutaminolysis has antileukemic activity in acute myeloid leukemia and synergizes with BCL-2 inhibition; Blood 126 1346 3) Alkan et al. (2018) Cytosolic Aspartate Availability Determines Cell Survival When Glutamine is Limiting; Cell Metabolism 28 1
-20°C
TARGET: Glutaminase; Energy production -- PATHWAY: Apoptosis inducer; Amino acid metabolism; Proliferation; Cell cycle -- RESEARCH AREA: Cell death; Neuroscience -- DISEASE AREA: Cancer