Glutaminase

Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.

BJJF078, an aminopiperidine derivative, is a potent inhibitor of recombinant human and mouse glutamine aminotransferase (TG2) activity, with IC50 values of 41 and 54 nM for human and mouse glutamine aminotransferase, respectively.BJJF078 inhibits TG1 enzyme, with an IC50 of 0.16 μM.BJJF078 can be used to study multiple sclerosis (MS). BJJF078 can be used to study multiple sclerosis (MS).

Glutaminase C-IN-2 (compound 11), an allosteric inhibitor of glutaminase C (GAC), exhibits potent inhibitory activity with an IC50 of 10.64 nM. By disrupting glutamine metabolism, this compound modulates cellular metabolites and elevates reactive oxygen species (ROS), exerting anticancer effects [1].

ZED-1227 (TAK-227) is an orally active, selective and potent transglutaminase 2 (TG2) inhibitor with anticancer activity that blocks inflammation-induced TG2 expression and activation for the treatment of Celiac Disease.

GK921 is a transglutaminase 2 (TGase) inhibitor.

Glutaminase C-IN-1 (Compound 968) is a Glutaminase C allosteric inhibitor.

UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM. Kd of UPGL00004 for GAC was 27 nM. UPGL00004 has a strong inhibitory effect on the proliferation of highly aggressive triple negative breast cancer cell lines.

Sirpiglenastat (DRP-104) is a glutamine antagonist, a prodrug of DON, with antitumor activity that acts by inhibiting glutamine metabolism and stimulating the innate and adaptive immune system.

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

BPTES(IC50 of 0.16 μM) is an effective and specific GlutamiN/Ase GLS1 (KGA) inhibitor.

GLS1 Inhibitor-4 (compound 41e) is a powerful GLS1 inhibitor, demonstrating an IC50 of 11.86 nM. It exhibits antiproliferative effects, substantial metabolic stability, and strong GLS1 binding affinity. Furthermore, it interrupts glutamine metabolism, induces ROS production, and triggers apoptosis, culminating in notable antitumor activity [1].

Glutaminase-IN-3 is a potent Glutaminase 1 inhibitor with potential antitumor activity and inhibits GLS1 for cancer research.

6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine) is an antagonist of glutaminases (Ki : 6 μM). It is an antineoplastic antibiotic produced by an unidentified species of Streptomyces from Peruvian soil.

L-Albizziin (L-beta-Ureidoalanine) is a glutamase inhibitor and is a glutaminyl-tRNA synthetase inhibitor.