An inhibitor of cruzain
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Cruzain-IN-1

Item No. 37350

Technical Information
Formal Name
6-[(3,5-difluorophenyl)amino]-9-ethyl-9H-purine-2-carbonitrile
CAS Number
1199523-24-4
Synonyms
  • Cruzain Inhibitor 1
Molecular Formula
C14H10F2N6
Formula Weight
Purity
≥95%
A solid
DMSO: Soluble: ≥10 mg/ml
SMILES
N#CC1=NC2=C(N=CN2CC)C(NC3=CC(F)=CC(F)=C3)=N1
InChi Code
InChI=1S/C14H10F2N6/c1-2-22-7-18-12-13(20-11(6-17)21-14(12)22)19-10-4-8(15)3-9(16)5-10/h3-5,7H,2H2,1H3,(H,19,20,21)
InChi Key
SZYYBVWPURUFRR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    Cruzain-IN-1 is an inhibitor of the Trypanosoma protease cruzain (IC50 = 0.2 nM).1 It is selective for cruzain over the Trypanosoma proteases cathepsin L-like protein and cathepsin B-like protease (IC50s = <6 and 6,000 nM, respectively) and a panel of 71 mammalian cysteine proteases, aspartyl proteases, peptidases, matrix metalloproteinases (MMPs), and serine proteases at 1 µM. Cruzain-IN-1 is active against T. brucei (MIC50 = 25 µM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mott, B.T., Ferreira, R.S., Simeonov, A., et alIdentification and optimization of inhibitors of Trypanosomal cysteine proteases: Cruzain, rhodesain, and TbCatB. J. Med. Chem. 53(1), 52-60 (2010).