| Bioactivity | LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model[1]. |
| Invitro | LWG-301 (compound 41a) inhibits HCT116 cancer cells growth with an IC50 value of 61 nM[1].LWG-301 has great metabolic stability in human liver microsomes with T1/2=108 min, CL=32 μL/min/mg[1].LWG-301 (10 μM; 6 h) interacts with GLS1 protein in a dose- and time-dependent manner[1].LWG-301 (0.03-3 μM; 14 d) inhibits the colony formation of HCT116 cells in a concentration-dependent manner[1].LWG-301 (0.2 μM, 1 μM, 5 μM; 24 h) blocks the metabolism of glutamine thus results a decrease of glutamate, glutathione, and fumaric acid[1].LWG-301 (1-10 μM; 24 h) induces ROS production and (0.1-10 μM; 24 h) induces apoptosis in HCT116 cells[1]. Western Blot Analysis[1] Cell Line: |
| Name | LWG-301 |
| Formula | C28H38N8O3S |
| Molar Mass | 566.72 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |