UPGL00004是一种有效的谷氨酰胺酶C(GAC)抑制剂(IC50=29nM;Kd=27nM)。UPGL00004强烈抑制高度侵袭性三阴性乳腺癌细胞系的增殖。
货号:ajcx31634
CAS:1890169-95-5
分子式:C25H26N8O2S2
分子量：534.66
溶解度:DMSO: 125 mg/mL (233.79 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

UPGL00004 inhibits MDA-MB-231, HS578T and TSE cells with IC50s of 70, 129, and 262 nM, respectively[1].

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 in a triple-negative breast cancer patient-derived tumor graft model[1].

[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.