UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2.
UPGL00004 potently inhibits the growth of triple negative breast cancer cells, as well as tumor growth when combined with the anti-VEGF antibody bevacizumab[2].
UPGL00004 potently suppresses tumor growth in a patient-derived xenograft model for breast cancer, when combined with the anti-angiogenesis, anti-VEGF monoclonal antibody bevacizumab[2].
[1] McDermott LA, et al. Bioorg Med Chem. 2016, 24(8):1819-39. [2] Huang Q, et al. J Biol Chem. 2018, 293(10):3535-3545.