GLS1 Inhibitor

Description: 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. Target: Others. Smiles: N([C@H]1CN(CC1)C2=CC=CN=N2)C=3SC(NC([C@@H](OC)C4=CC=CC=C4)=O)=NN3. References: 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)