Glutaminase-IN-1
Modify Date: 2024-01-09 22:13:36
Glutaminase-IN-1 structure
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Common Name | Glutaminase-IN-1 | ||
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| CAS Number | 2247127-79-1 | Molecular Weight | 618.47 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C26H24F3N7O3Se | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Glutaminase-IN-1Glutaminase-IN-1, a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 shows improved cellular uptake and antitumor activity. |
| Name | Glutaminase-IN-1 |
|---|
| Description | Glutaminase-IN-1, a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 shows improved cellular uptake and antitumor activity. |
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| Related Catalog | |
| Target |
IC50: 1 nM (KGA)[1]. |
| In Vitro | Glutaminase-IN-1 (CPD20), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 shows improved cellular uptake and antitumor activity. The IC50 values of Glutaminase-IN-1 are 17 nM, 6.78 μM, 19 nM and 9 nM in A549, H2, Caki-1 and HCT116 cell lines, respectively. Glutaminase-IN-1 has better KGA inhibitory activity than the corresponding BPTES and CB839[1]. |
| In Vivo | Glutaminase-IN-1(10 mg/kg, i.h.) reduced the size and weight of the HCT116 tumor, and statistical analysis showed that the 40% reduction in tumor weight by CPD20 is statistically significant. Glutaminase-IN-1 could statistically significantly prolong the survival of H22-bearing mice[1]. |
| References |
| Molecular Formula | C26H24F3N7O3Se |
|---|---|
| Molecular Weight | 618.47 |
| Storage condition | 2-8℃ |