glutaminase c-in-1

Glutaminase C-IN-1 (Compound 968) 是一种 Glutaminase C 变构抑制剂。

Telaglenastat (CB-839) hydrochloride is a first-in-class, reversible, and orally active inhibitor of glutaminase 1 (GLS1). It selectively inhibits the splice variants of GLS1, specifically KGA (kidney-type glutaminase) and GAC (glutaminase C), as compared to GLS2. Telaglenastat hydrochloride has an IC50 of 23 nM for endogenous glutaminase in mouse kidney and 28 nM in the brain. In addition, it induces autophagy and exhibits antitumor activity.

GlutaminaseC-IN-2（compound 11）为GAC变构抑制剂，IC50值为10.64 nM。该化合物通过干扰谷氨酰胺代谢，调控细胞代谢产物，进而提高ROS水平，并展现出抗癌活性。

Glutaminase C inhibitor 11是一种glutaminase C (GAC)的抑制剂。它能够抑制GAC酶的活性（EC50 = 10.64 nM），降低A549非小细胞肺癌(NSCLC)细胞的活力（IC50 = 4.025 nM）。在A549细胞中，Glutaminase C inhibitor 11（0.1和1 µM）能减少细胞集落形成并降低细胞内谷氨酸水平。在体内，Glutaminase C inhibitor 11（100 mg/kg）能够减缓A549小鼠异位瘤模型中的肿瘤生长。