Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11412 |
IPN60090
GLS1-IN-1 |
Others; transporter | Metabolism; Others |
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。 | |||
T37385 |
Glutaminase-IN-3
|
Glutaminase | Proteases/Proteasome |
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。 | |||
T37222 |
GLS1 Inhibitor
|
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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 demons... | |||
T72679 |
GLS1 Inhibitor-4
|
Glutaminase | Proteases/Proteasome |
GLS1 Inhibitor-4 (compound 41e)作为一种高效的GLS1抑制剂,具有11.86 nM的IC50值。该化合物展现了抗增殖效果、优秀的代谢稳定性以及强大的GLS1结合亲和力。它通过阻断谷氨酰胺代谢和诱导ROS生成,能够引发细胞凋亡并表现出对抗肿瘤的活性。 | |||
T39309 |
Telaglenastat hydrochloride
CB-839 hydrochloride |
||
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. | |||
T79340 |
GLS1 Inhibitor-7
|
Glutaminase | Proteases/Proteasome |
GLS1 Inhibitor-7 (compound 4d) 作为一种GLS1 抑制剂,表现出抑制浓度50%所需浓度(IC50)为46.7 μM,潜在用途涉及抗癌、抗衰老和抗肥胖。 | |||
T39544 |
IPN60090 dihydrochloride
IPN60090 dihydrochloride |
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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. | |||
T73458 |
LWG-301
|
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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。 |