| Description | UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM. Kd of UPGL00004 for GAC was 27 nM. UPGL00004 has a strong inhibitory effect on the proliferation of highly aggressive triple negative breast cancer cell lines. |
| In vitro | UPGL00004 inhibits MDA-MB-231, HS578T, and TSE cells (IC50s: 70, 129, and 262 nM, respectively).[1] |
| In vivo | In a triple-negative breast cancer patient-derived tumor graft model, the combination of UPGL00004 (1 mg/kg body weight) and Bevacizumab (2.5 mg/kg body weight) via intraperitoneal injection completely prevent any detectable increase in tumor size.[1] |
| Target activity | Glutaminase C:（kd）27 nM, Glutaminase C:29 nM, Glutaminase C:29 nM, Glutaminase C:27 nM（kd） |
| molecular weight | 534.66 |
| Molecular formula | C25H26N8O2S2 |
| CAS | 1890169-95-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 112.5 mg/mL (210.4 mM), Sonication is recommended. |
| 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. 2. McDermott LA,et al. Design and evaluation of novel glutaminase inhibitors. Bioorg Med Chem. 2016;24(8):1819-1839. |