gls-1 inhibitor

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. 1.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)

GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor (IC50: 27.98 nM) with anti-proliferative effects.

GLS1 Inhibitor-5 (compound 24y) is a selective, orally active glutaminase 1 (GLS1) inhibitor (IC50: 68 nM) that induces apoptosis and exhibits anti-tumor effects.

GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM, exhibiting antiproliferative effects, substantial metabolic stability, and strong GLS1 binding affinity. It disrupts glutamine metabolism, induces ROS production, triggers apoptosis, and demonstrates notable antitumor activity [1].

GLS1 Inhibitor-6 inhibitor ( IC 50 =68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis .

GLS1 Inhibitor-7 (compound 4d) is a GLS1 antagonist with an IC50 value of 46.7 μM, showing potential applications in anticancer, antiaging, and antiobesity therapies [1].

JNK-IN-23 (Compound K12) is an inhibitor of JNK. It effectively inhibits the proliferation of MDA-MB-231 cells with a GIC50 of 30 nM. In vivo, JNK-IN-23 blocks metastatic growth of triple-negative breast cancer (TNBC). Additionally, it suppresses the growth of lung metastases by dual targeting of glutaminase-1 (GLS) and the pyruvate dehydrogenase complex (PDHC).

IPN-60090 dihydrochloride is a potent and specific inhibitor of glutaminase 1 (GLS1) with a remarkable inhibition constant (IC50) of 31 nM. It does not exhibit any inhibitory activity against GLS-2. Furthermore, IPN-60090 dihydrochloride possesses outstanding physicochemical properties and pharmacokinetic characteristics in vivo. Therefore, it is a valuable compound for researching solid tumors, including lung and ovarian cancers.

GLS-1-IN-1 (compound 1d) is a GLS-1 inhibitor effective against Hep G2, MCF 7, and MCF 10A cells.