GLS1 Inhibitor

GLS1 inhibitor is an inhibitor of glutaminase 1 (GLS1; IC₅₀ = 0.021 μM). It inhibits the growth of NCI H1703 non-small cell lung cancer (NSCLC) cells in 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.

GLS1 Inhibitor-1 (Compound 27) is an orally active inhibitor for glutaminase 1 (GLS1) with an IC50 of 0.021 μM. GLS1 Inhibitor-1 inhibits the proliferation of PC-3 with an IC50 of 0.3 nM. GLS1 Inhibitor-1 exhibits antitumor efficacy against NCI-H1703 with GI50 of 0.011 μM. GLS1 Inhibitor-1 exhibits moderate pharmacokinetic characteristics[1].

[1] Finlay MRV, et al., Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models. J Med Chem. 2019 Jul 25;62(14):6540-6560. DOI:10.1021/acs.jmedchem.9b00260