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GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity[1]. | [in vivo]
GLS1 Inhibitor-4 (50, 100 mg/kg; i.p.; twice a day for 21 consecutive days) shows antitumor activity in a dose-dependent manne[1]. | Animal Model: | Six-week-old BALB/c SPF nude mice (HCT116 tumor nude mouse xenograft model)[1] | | Dosage: | 50, 100 mg/kg | | Administration: | I.p.; twice a day for 21 consecutive days | | Result: | Inhibited the tumor growth at a dose-dependent manne with the tumor growth inhibition (TGI) values of 35.5% at 50 mg/kg and 47.5% at 100 mg/kg, respectively. |
| [References]
[1] Xu X, et al. Discovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles. Eur J Med Chem. 2022 Jun 5;236:114337. DOI:10.1016/j.ejmech.2022.114337 |
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