Glutaminase
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S7655 | Telaglenastat (CB-839) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7753 | BPTES | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S8998 | IACS-6274 | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| E0134 | L-Albizziin | 29 mg/mL | <1 mg/mL | <1 mg/mL |
| S8778 | UPGL00004 | <1 mg/mL | 25 mg/mL | <1 mg/mL |
| S6417 | GK921 | -1 mg/mL | 33 mg/mL | -1 mg/mL |
| S8891 | JHU-083 | 62 mg/mL | 62 mg/mL | 62 mg/mL |
| S8620 | 6-Diazo-5-oxo-L-norleucine | 34 mg/mL | 7 mg/mL | <1 mg/mL |
Glutaminase製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| 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. |
Apoptotic sensitivity of K562 resistant (E) cells exposed to A1331852 (10 nM) for 4 h was restored following pharmacological inhibition of glutamine uptake or metabolism with GPNA (5 mM) for 48 h, CB-839 (10 μM) for 72 h, azaserine (25 μM) for 16 h and AOA (500 μM) for 24 h but not with EGCG (50 μM) for 24 h. Western blots confirmed the knockdown efficiency of the different siRNAs. ***P<0.001, **P<0.01; Error bars = Mean ± SEM (n=3).
|
|
| S7753 |
BPTESBPTES 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. |
Glu-dependent associates with sensitivity to glycolytic inhibitors 3-BrPA (left) and GLN-addicted associates with sensitivity to glutaminolytic inhibitors BPTEs.
|
|
| S8998新 |
IACS-6274IACS-6274 (IPN60090), is a potent, selective and orally active glutaminase inhibitor with potential antineoplastic and immunostimulating activities. |
||
| E0134新 |
L-AlbizziinL-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. |
||
| S8778 |
UPGL00004UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2. |
||
| S6417 |
GK921GK921 is a transglutaminase 2 (TGase 2) inhibitor with an IC50 of 8.93 μM under a modified assay condition. |
||
| S8891 |
JHU-083JHU-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 best fresh-prepared. |
||
| S8892 |
JHU395JHU395 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. |
||
| S8620 |
6-Diazo-5-oxo-L-norleucine6-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. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| 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. |
Apoptotic sensitivity of K562 resistant (E) cells exposed to A1331852 (10 nM) for 4 h was restored following pharmacological inhibition of glutamine uptake or metabolism with GPNA (5 mM) for 48 h, CB-839 (10 μM) for 72 h, azaserine (25 μM) for 16 h and AOA (500 μM) for 24 h but not with EGCG (50 μM) for 24 h. Western blots confirmed the knockdown efficiency of the different siRNAs. ***P<0.001, **P<0.01; Error bars = Mean ± SEM (n=3).
|
|
| S7753 |
BPTESBPTES 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. |
Glu-dependent associates with sensitivity to glycolytic inhibitors 3-BrPA (left) and GLN-addicted associates with sensitivity to glutaminolytic inhibitors BPTEs.
|
|
| S8998新 |
IACS-6274IACS-6274 (IPN60090), is a potent, selective and orally active glutaminase inhibitor with potential antineoplastic and immunostimulating activities. |
||
| E0134新 |
L-AlbizziinL-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. |
||
| S8778 |
UPGL00004UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2. |
||
| S6417 |
GK921GK921 is a transglutaminase 2 (TGase 2) inhibitor with an IC50 of 8.93 μM under a modified assay condition. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S8891 |
JHU-083JHU-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 best fresh-prepared. |
||
| S8892 |
JHU395JHU395 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. |
||
| S8620 |
6-Diazo-5-oxo-L-norleucine6-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. |
2022, 12(5)728 2021, 22(11)5602 2021, 71:101569 |
