Glutaminase-IN-1 is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA; IC50: 1 nM). Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.

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.?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 could statistically significantly prolong the survival of H22-bearing mice.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.

2247127-79-1

C26H24F3N7O3Se

618.47

CB839 derivative;Glutaminase-IN-1

DMSO:125 mg/mL (202.11 mM),Need ultrasonic
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In solvent: -80°C for 2 years