Glutaminase

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.

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.

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

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.

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

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.

GK921 is an inhibitor of transglutaminase 2 (TGase).

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.

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

L-Methionine-DL-sulfoximine (MSO) inhibits glutamine synthetase and metabolically and morphologically primarily affects astroglia. L-Methionine-DL-sulfoximine can be used in convulsant studies.

LDN-27219 is a potent hTGase inhibitor with IC50 of 0.6 uM.

TG-2-IN-1 is a potent transglutaminase-2 (TGM-2) inhibitor.TG-2-IN-1 is used in the study of cancer, neurological disorders, and immune system disorders.

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

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

Decanoic Acid (Caprynic acid) acts as a non-competitive AMPA receptor antagonist.

ZM39923 hydrochloride (JAK3 Inhibitor IV) is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.

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

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.

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

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).

N-Phenylacrylamide inhibit human recombinant TGM2 by fluorescent transamidation assay.

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.

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.

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.