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Glutaminase inhibitors/antagonist

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Cat.No. Product Name Information Product Use Citations Product Validations
S7655 Telaglenastat (CB-839) Telaglenastat (CB-839) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. It induces autophagy and has antitumor activity. Phase 1.
Signal Transduct Target Ther, 2025, 10(1):271
Bone Res, 2025, 13(1):62
Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0694
Verified customer review of Telaglenastat (CB-839)
S8620 6-Diazo-5-oxo-L-norleucine (Diazooxonorleucine) 6-Diazo-5-oxo-L-norleucine (Diazooxonorleucine, L-6-Diazo-5-oxonorleucine, DON), an antibiotic isolated from Streptomyces, is a glutaminase antagonist with IC50 of ~1  mM for cKGA (kidney-type glutaminase). 6-Diazo-5-oxo-L-norleucine exhibits analgesic, antibacterial, antiviral and anticancer properties.
bioRxiv, 2025, 2025.07.14.664742
Int J Mol Sci, 2024, 25(18)10183
iScience, 2023, 26(10):107790
E1203 Sirpiglenastat (DRP-104) Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. It has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response with immunomodulatory and antineoplastic activities.
S7753 BPTES BPTES is a potent and selective Glutaminase GLS1 (KGA) inhibitor with IC50 of 0.16 μM. It has no effect on glutamate dehydrogenase activity and causes only a very slight inhibition of γ-glutamyl transpeptidase activity.
Signal Transduct Target Ther, 2025, 10(1):27
Biomed Pharmacother, 2025, 191:118492
STAR Protoc, 2025, 6(1):103518
Verified customer review of BPTES
S8891 JHU-083 JHU-083 (Ethyl 2-(2-Amino-4-methylpentanamido)-DON) is a novel prodrug of DON. This compound selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.Solutions are unstable and should be fresh-prepared.
Cell Rep, 2025, 44(5):115596
iScience, 2023, 26(10):107790
S6417 GK921 GK921 is a transglutaminase 2 (TGase 2) inhibitor with an IC50 of 8.93 μM under a modified assay condition.
J Immunol Res, 2021, 2021:4754454
E0373New LDN-27219 LDN-27219 is a potent, reversible, slow-binding inhibitor of Tissue transglutaminase (TGase), which exhibits IC50 of 0.6 μM against human hTGase. It likely binds at the GTP-binding or regulatory site rather than the enzyme’s active site. It lowers blood pressure and improves endothelium-dependent vasodilation in resistance arteries in an age-dependent manner.
S8892 JHU395 JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. This compound delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and significantly inhibits tumor growth without observed toxicity.
S8778 UPGL00004 UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2.
S8998 IACS-6274 IACS-6274 (IPN60090), is a potent, selective and orally active glutaminase inhibitor with potential antineoplastic and immunostimulating activities.