Glutaminase

Glutaminase製品

All (11)
Glutaminase阻害剤 (7)
Glutaminase拮抗剤(4)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
S7655	Telaglenastat (CB-839)	CB-839 (Telaglenastat) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1.	Nat Commun, 2024, 15(1):9820 Nat Commun, 2024, 15(1):5620 EBioMedicine, 2024, 102:105090
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.	Gastroenterology, 2024, S0016-5085(24)00062-3 Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0 Exp Mol Med, 2024, 10.1038/s12276-024-01214-1
S8620	6-Diazo-5-oxo-L-norleucine	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.	Int J Mol Sci, 2024, 25(18)10183 iScience, 2023, 26(10):107790 Cancer Cell, 2022, 40(10):1207-1222.e10
S8891	JHU-083	JHU-083 (Ethyl 2-(2-Amino-4-methylpentanamido)-DON) is a novel prodrug of DON.JHU-083 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.	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
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. JHU395 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.
E2365	Glutaminase C-IN-1	Glutaminase C-IN-1 is an allosteric inhibitor of Glutaminase C (GAC) that inhibits cancer cell growth without affecting their normal cellular counterparts.
E1203	Sirpiglenastat	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.
E0134	L-Albizziin	L-albizziin (L-alpha-amino-beta-ureidopropionic acid) is a potent inhibitor of glutamase. L-albizziin interferes with the utilisation of L-glutamine by the Debaryomyces spp. enzyme probably in a competitive and reversible manner since L-albizziin is also a substrate of the enzyme.
S7655	Telaglenastat (CB-839)	CB-839 (Telaglenastat) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1.	Nat Commun, 2024, 15(1):9820 Nat Commun, 2024, 15(1):5620 EBioMedicine, 2024, 102:105090
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.	Gastroenterology, 2024, S0016-5085(24)00062-3 Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0 Exp Mol Med, 2024, 10.1038/s12276-024-01214-1
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
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.
E2365	Glutaminase C-IN-1	Glutaminase C-IN-1 is an allosteric inhibitor of Glutaminase C (GAC) that inhibits cancer cell growth without affecting their normal cellular counterparts.
E0134	L-Albizziin	L-albizziin (L-alpha-amino-beta-ureidopropionic acid) is a potent inhibitor of glutamase. L-albizziin interferes with the utilisation of L-glutamine by the Debaryomyces spp. enzyme probably in a competitive and reversible manner since L-albizziin is also a substrate of the enzyme.
S8620	6-Diazo-5-oxo-L-norleucine	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.	Int J Mol Sci, 2024, 25(18)10183 iScience, 2023, 26(10):107790 Cancer Cell, 2022, 40(10):1207-1222.e10
S8891	JHU-083	JHU-083 (Ethyl 2-(2-Amino-4-methylpentanamido)-DON) is a novel prodrug of DON.JHU-083 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.	iScience, 2023, 26(10):107790
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. JHU395 delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and significantly inhibits tumor growth without observed toxicity.
E1203	Sirpiglenastat	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.

Glutaminase阻害剤の選択性比較