Glutaminase
Inhibitory Selectivity
Glutaminase Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7655 |
CB-839CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. 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).
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| 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.
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| S8778New |
UPGL00004UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2. |
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| S6417New |
GK921GK921 is a transglutaminase 2 (TGase 2) inhibitor with an IC50 of 8.93 μM under a modified assay condition. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7655 |
CB-839CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. 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.
|
|
| S8778New |
UPGL00004UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2. |
||
| S6417New |
GK921GK921 is a transglutaminase 2 (TGase 2) inhibitor with an IC50 of 8.93 μM under a modified assay condition. |
