Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA) , with an IC 50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity. 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 IC 50 of 1 nM. Glutaminase-IN-1 shows improved cellular uptake and antitumor activity. The IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Glutaminase-IN-1(10 mg/kg, s.c.) 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 1 nM (KGA)
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Glutaminase-IN-1
CAS number：2247127-79-1 molecular formula：C26H24F3N7O3Se
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| Chinese alias | 谷氨酰胺酶-IN-1 | ||
| English alias | - | ||
| CAS number | 2247127-79-1 | molecular formula | C26H24F3N7O3Se |
| molecular weight | 618.47 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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