UPGL00004 Chemical Properties

Density 

1.460±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: 2mg/mL, clear

form 

Solid

pka

9.23±0.50(Predicted)

color 

Off-white to gray

UPGL00004 Usage And Synthesis

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

< td class="border-bottom: 1px dotted #ccc;padding: 5px;"> 29 nM

Target	Value
glutaminase C (Cell-free assay)

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