glutaminase

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

Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C (GLS1).

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

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.

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

GK921 is an inhibitor of transglutaminase 2 (TGase).

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

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

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

Sirpiglenastat (DRP-104), a glutamine antagonist and prodrug of DON, exhibits antitumor activity by inhibiting glutamine metabolism and stimulating both the innate and adaptive immune systems.

Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine inhibitor of the renal-type glutaminase (KGA) variant, exhibited antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model.

Glutaminase-IN-4 (compound 2a) is a glutaminase (GLS) inhibitor with an IC50 of 2.3 μM.

Glutaminase C Inhibitor 11 is a potent inhibitor specifically targeting Glutaminase C (GAC), demonstrating significant inhibition of GAC enzyme activity with an EC50 value of 10.64 nM. It effectively diminishes the viability of A549 non-small cell lung cancer (NSCLC) cells, presenting an IC50 of 4.025 nM. Moreover, at concentrations of 0.1 and 1 µM, it substantially impedes colony formation and reduces intracellular glutamate levels in A549 cells. Demonstrating efficacy in vivo, Glutaminase C Inhibitor 11 at a dosage of 100 mg/kg markedly curtails tumor growth in an A549 mouse xenograft model.

Transglutaminase (TG) is a thiolase that induces intermolecular cross-linking of proteins, by catalysing the formation of isopeptide bonds between the γ-carboxamide group of glutamine residues and the primary ε-amine group of other compounds. The enzyme plays a role in a variety of physiological processes including coagulation, antimicrobial immune responses and photosynthesis.

TG2-IN-3h is a transglutaminase (TGase) inhibitor used in the study of neurological and immune system disorders.

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.

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].

Zampilimab (UCB-7858) is a humanised monoclonal antibody targeting TGM2, which binds to and inhibits the cross-linking transamidase activity of TG2, and is used to improve renal fibrosis.

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].

TG-2-IN-4 (compound 8), an inhibitor of transglutaminase 2 (TG2) with an IC 50 value of less than 0.5 mM, is utilized in the study of inflammatory disorders [1].

IPN60090 is a novel, potent, orally bioavailable, renal-type glutaminase (GLS1)-specific inhibitor with an IC50 value of 31 nM for GLS1. IPN60090 has potential anticancer and immunostimulant immunomodulatory activity, selectively targets, binds, and inhibits human glutaminase, and can be used to study GLS1-mediated diseases.

JHU-083 is an orally available, blood-brain barrier-crossing, selective glutaminase antagonist that improves cognitive performance and normalizes abnormal hippocampal glutaminase activity in APOE4 mice.

Cystamine (2,2'-Disulfanediyldiethanamine) is an inhibitor of transglutaminase and inhibits caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used in studies about Huntington's diseases.

Cystamine dihydrochloride is a radiation-protective agent. It also protects against carbon tetrachloride liver damage.