Uses
UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines[1].
Biological Activity
UPGL00004 is a potent glutaminase C (GAC) inhibitor with IC50 of 29 nM, more selective for GAC than GLS2.
in vitro
Administration of UPGL00004 in combination with the anti-VEGF antibody bevacizumab effectively inhibited triple-negative breast cancer cell growth and tumor growth.
in vivo
Administration of UPGL00004 in combination with the anti-VEGF antibody bevacizumab inhibited tumor growth in a human xenograft model of breast cancer.
target
| Target | Value |
glutaminase C
(Cell-free assay) | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> 29 nM
References
[1] Huang Q, et al. Characterization of the interactions of potent allosteric inhibitors with glutaminase C, a key enzyme in cancer cell glutamine metabolism. J Biol Chem. 2018 Mar 9;293(10):3535-3545. DOI:
10.1074/jbc.M117.810101
