An inhibitor of GLS1
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Glutaminase-IN-1

Item No. 42339

Technical Information
Formal Name
N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-selenadiazol-2-yl]-2-pyridineacetamide
CAS Number
2247127-79-1
Synonyms
  • GLS-IN-1
  • GLS Inhibitor 1
  • Glutaminase Inhibitor 1
Molecular Formula
C26H24F3N7O3Se
Formula Weight
Purity
≥95%
Formulation
A solid
DMSO: Sparingly Soluble: 1-10 mg/ml
SMILES
O=C(CC1=CC(OC(F)(F)F)=CC=C1)NC(C=C2)=NN=C2CCCCC3=NN=C(NC(CC4=CC=CC=N4)=O)[Se]3
InChi Code
InChI=1S/C26H24F3N7O3Se/c27-26(28,29)39-20-9-5-6-17(14-20)15-22(37)31-21-12-11-18(33-34-21)7-1-2-10-24-35-36-25(40-24)32-23(38)16-19-8-3-4-13-30-19/h3-6,8-9,11-14H,1-2,7,10,15-16H2,(H,31,34,37)(H,32,36,38)
InChi Key
KWZUDGWKTNIKJY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    Glutaminase-IN-1 is an inhibitor of glutaminase 1 (GLS1), also known as kidney-type (K-type) glutaminase (IC50 = 1 nM) and a selenium-containing derivative of CB-839 (Item No. 22038).1 It is selective for GLS1 over glutamate dehydrogenase (GDH; IC50 = >13 µM). It inhibits the proliferation of A549 lung, H22 liver, Caki-1 kidney, and HCT116 colon cancer cells (IC50s = 0.017, 6.78, 0.019, and 0.009 µM, respectively). Glutaminase-IN-1 (10 µM) induces the production of reactive oxygen species (ROS) in A549 cells. It decreases tumor weight in an HCT116 mouse xenograft model when administered at a dose of 10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chen, Z., Li, D., Xu, N., et alNovel 1,3,4-selenadiazole-containing kidney-type glutaminase inhibitors showed improved cellular uptake and antitumor activity. J. Med. Chem. 62(2), 589-603 (2019).