| Bioactivity | 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]. |
| Invitro | GLS1 Inhibitor-4 (compound 41e) shows antiproliferative activity with IC50s of 0.051, 0.37, 0.32, 1.34 µM for HCT116 and MDA-MB-436, CT26, H22 cells, respectively[1].GLS1 Inhibitor-4 shows good plasma and liver microsomal stability with 96% stability in Human plasma[1].GLS1 Inhibitor-4 shows robust binding affinity with GLS1 protein, the dissociation constants (Kd) of 52 nM[1].GLS1 Inhibitor-4 (0.1, 0.5, 1 µM) inhibits the colony formation of HCT116 cells in a dose-dependent manner[1].GLS1 Inhibitor-4 (100, 300 nM, 12 h) reduces the concentration of a number of key metabolites downstream of glutamate within 12 h[1].GLS1 Inhibitor-4 (30, 50, 200 nM; 6 h) increases the ROS levels in a dose-dependent manner in HCT116 cells[1].GLS1 Inhibitor-4 (1 mmol/L; 12 h) significantly decreases the ATP production basal and maximal OCRs (oxygen consumption rates) after 12 h, suppresses the aerobic glycolysis in HCT116 cancer cells[1].GLS1 Inhibitor-4 (30, 50, 200 nM; 24 h) induces apoptosis in a dose-dependent manner[1]. Apoptosis Analysis[1] Cell Line: |
| Name | GLS1 Inhibitor-4 |
| Formula | C29H27F3N10O2S2 |
| Molar Mass | 668.72 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |