An inhibitor of the protein-protein interaction between Trx and caspase-3
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Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

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Product Type

KEA1-97

Item No. 42049

Technical Information
Formal Name
4,6-dichloro-N-(4′-fluoro[1,1′-biphenyl]-4-yl)-1,3,5-triazin-2-amine
CAS Number
2138882-71-8
Molecular Formula
C15H9Cl2FN4
Formula Weight
Purity
≥98%
A solid
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
ClC1=NC(Cl)=NC(NC2=CC=C(C3=CC=C(F)C=C3)C=C2)=N1
InChi Code
InChI=1S/C15H9Cl2FN4/c16-13-20-14(17)22-15(21-13)19-12-7-3-10(4-8-12)9-1-5-11(18)6-2-9/h1-8H,(H,19,20,21,22)
InChi Key
DUROVTLUQOYUPH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    KEA1-97 is a dichlorotriazine (DCT) inhibitor of the protein-protein interaction between thioredoxin (Trx) and caspase-3.1 It binds to lysine 72 (K72) of Trx and inhibits DCT-alkyne labeling of recombinant Trx at K72 (IC50 = 10 µM). KEA1-97 (100 µM) inhibits the interaction between Trx and caspase-3 in a cell-free assay. It reduces survival and proliferation of and induces apoptosis in Trx-overexpressing 231MFP breast cancer cells. In vivo, KEA1-97 (5 mg/kg) reduces tumor volume in a 231MFP mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Anderson, K.E., To, M., Olzmann, J.A., et alChemoproteomics-enabled covalent ligand screening reveals a thioredoxin-caspase 3 interaction disruptor that impairs breast cancer pathogenicity. ACS Chem. Biol. 12(10), 2522-2528 (2017).