| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|