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Glutaminase-IN-1 

Cat. No.: HY-114334
Handling Instructions

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.

For research use only. We do not sell to patients.

Glutaminase-IN-1 Chemical Structure

Glutaminase-IN-1 Chemical Structure

CAS No. : 2247127-79-1

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & 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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6169 mL 8.0845 mL 16.1689 mL
5 mM 0.3234 mL 1.6169 mL 3.2338 mL
10 mM 0.1617 mL 0.8084 mL 1.6169 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

618.47

Formula

C₂₆H₂₄F₃N₇O₃Se

CAS No.

2247127-79-1

SMILES

O=C(NC1=NN=C(CCCCC2=NN=C(NC(CC3=CC=CC(OC(F)(F)F)=C3)=O)C=C2)[Se]1)CC4=NC=CC=C4

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Glutaminase-IN-1
Cat. No.:
HY-114334
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Glutaminase-IN-1

Cat. No.: HY-114334