glutaminase-in-1

Glutaminase-IN-1 (CB839 derivative)，是一种新型 1,3,4-硒二氮基肾型谷氨酰胺酶(KGA) 的变构抑制剂，在侵袭性 H22 肝癌异种移植模型中显示出抗肿瘤活性。

IPN60090是一种新型、强效、口服生物利用度高的 肾型谷氨酰胺酶（GLS1）特异性抑制剂，对GLS1的IC50值为31 nM。IPN60090 具有潜在的抗癌和免疫刺激 免疫调节活性，可选择性地靶向、结合并抑制人谷氨酰胺酶，可用于研究 GLS1 介导的疾病。

GLS1 inhibitor is an inhibitor of glutaminase 1 (GLS1; IC50= 0.021 μM).1It inhibits the growth of NCI H1703 non-small cell lung cancer (NSCLC) cellsin vitro(GI50= 0.011 μM). GLS1 inhibitor (100 mg/kg) reduces tumor growth, increases tumor levels of glutamine, and decreases tumor levels of glutamate and aspartate in an NCI H1703 mouse xenograft model. 1.Finlay, M.R.V., Anderton, M., Bailey, A., et al.Discovery of a thiadiazole-pyridazine-based allosteric glutaminase 1 inhibitor series that demonstrates oral bioavailability and activity in tumor xenograft modelsJ. Med. Chem.62(14)6540-6560(2019)

Glutaminase-IN-3 是一种有效的的 Glutaminase 1 抑制剂，具有潜在的抗肿瘤活性，对 GLS1 具有抑制作用，可用于研究癌症。

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.

IPN-60090 dihydrochloride is a potent and specific inhibitor of glutaminase 1 (GLS1) with a remarkable inhibition constant (IC50) of 31 nM. It does not exhibit any inhibitory activity against GLS-2. Furthermore, IPN-60090 dihydrochloride possesses outstanding physicochemical properties and pharmacokinetic characteristics in vivo. Therefore, it is a valuable compound for researching solid tumors, including lung and ovarian cancers.

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

LWG-301是一种针对Glutaminase1(GLS1)的变构抑制剂，具有(IC50=7 nM)。通过显著阻断谷氨酰胺代谢并增加细胞内ROS，LWG-301能够诱导细胞凋亡(apoptosis)。在HCT116异种移植模型中，LWG-301展示出中等抗肿瘤活性。

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。