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.

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.

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.

GK921 is an inhibitor of transglutaminase 2 (TGase).

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

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

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

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

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

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).

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.

Irbesartan-d4 (Irbesartan D4), a deuterated compound of Irbesartan, is an angiotensin receptor blocker that is used in the study of cardiovascular disease.

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].

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].

TGase2-IN-1 (Compound 22) is an orally effective TGase2 inhibitor with an IC50 of 1.12 µM. It inhibits TGase2 in human retinal microvascular endothelial cells with a strikingly lower IC50 of 0.07 µM. The oral bioavailability of TGase2-IN-1 is 74.6%. Additionally, it can suppress retinal vascular leakage in a mouse model of diabetes induced by Streptozotocin.

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].