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ProductsBack/K777 [K11777] [233277-99-1]
Chemical Structure
Chemical Structure
Chemical Structure

K777 [K11777] [233277-99-1]

Research Use Only
AG-CR1-0158
AdipoGen Life Sciences
CAS Number233277-99-1
DownloadMSDS
Product group Chemicals
Estimated Purity>98%
Molecular Weight574.7
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    K777 [K11777]
  • Delivery Days Customer
    10
  • CAS Number
    233277-99-1
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Molecular Formula
    C32H38N4O4S
  • Molecular Weight
    574.7
  • Scientific Description
    Broad-range cathepsin inhibitor (for all known cathepsins) useful for inflammasome inhibition. Inhibits cathepsins B, L, S, C, V, K and papain in cell-free assays. Inhibits cathepsin X as well. Suppresses particle-induced NLRP3 activation and IL-1beta secretion more efficiently than Ca074Me (cathepsin B inhibitor), which in contrast suppresses nigericin-induced IL-1beta secretion. Selectively inhibits particle-induced cell death but not nigericin- or sAdT-induced cell death. Potent and selective CCR4 antagonist. Potent, irreversible cysteine protease inhibitor. Potent cysteine protease cruzain (cruzipain) inhibitor. Active against Trypanosoma cruzi the causative agent of Chagas disease, a parasitic infection which is a leading cause of heart disease. Antiparasitic agent with anti-trypanosomal , anti-leishmanial, anti-schistosomiasis, anti-amebiasis (EhCP1 (E. Histolytica cysteine proteinase 1)), anti-anthelmintic (hookworm first-stage larvae) and anti-cryptosporidial activity. Shown to have antiviral activity by targeting cathepsin-mediated cell entry. - Chemical. CAS: 233277-99-1. Formula: C32H38N4O4S. MW: 574.7. Synthetic. Broad-range cathepsin inhibitor (for all known cathepsins) useful for inflammasome inhibition. Inhibits cathepsins B, L, S, C, V, K and papain in cell-free assays. Inhibits cathepsin X as well. Suppresses particle-induced NLRP3 activation and IL-1beta secretion more efficiently than Ca074Me (cathepsin B inhibitor), which in contrast suppresses nigericin-induced IL-1beta secretion. Selectively inhibits particle-induced cell death but not nigericin- or sAdT-induced cell death. Potent and selective CCR4 antagonist. Potent, irreversible cysteine protease inhibitor. Potent cysteine protease cruzain (cruzipain) inhibitor. Active against Trypanosoma cruzi the causative agent of Chagas disease, a parasitic infection which is a leading cause of heart disease. Antiparasitic agent with anti-trypanosomal , anti-leishmanial, anti-schistosomiasis, anti-amebiasis (EhCP1 (E. Histolytica cysteine proteinase 1)), anti-anthelmintic (hookworm first-stage larvae) and anti-cryptosporidial activity. Shown to have antiviral activity by targeting cathepsin-mediated cell entry.
  • SMILES
    CN1CCN(C(N[C@@](C(N[C@@](/C=C/S(C2=CC=CC=C2)(=O)=O)([H])CCC3=CC=CC=C3)=O)([H])CC4=CC=CC=C4)=O)CC1
  • Storage Instruction
    -20°C,2°C to 8°C
  • UNSPSC
    12352200

References

  • Cysteine protease inhibitors cure an experimental Trypanosoma cruzi infection: J. Engel, et al.; J. Exp. Med. 188, 725 (1998)
  • In vitro evaluation of the disposition of A novel cysteine protease inhibitor: W. Jacobsen, et al.; Drug Metab. Dispos. 28, 1343 (2000)
  • Leishmania tropica: cysteine proteases are essential for growth and pathogenicity: H. Mahmoudzadeh-Niknam, et al.; Exp. Parasitol. 106, 158 (2004)
  • A cysteine protease inhibitor protects dogs from cardiac damage during infection by Trypanosoma cruzi: S.C. Barr, et al.; Antimicrob. Agents Chemother. 49, 5160 (2005)
  • Use of recombinant Entamoeba histolytica cysteine proteinase 1 to identify a potent inhibitor of amebic invasion in a human colonic model: S.G. Melendez-Lopez, et al.; Eukaryot. Cell 6, 1130 (2007)
  • Schistosomiasis mansoni: novel chemotherapy using a cysteine protease inhibitor: M.H. Abdulla, et al.; PLoS Med. 4, e14 (2007)
  • Vinyl sulfones as antiparasitic agents and a structural basis for drug design: I.D. Kerr, et al.; J. Biol. Chem. 284, 25697 (2009)
  • In vitro and in vivo studies of the trypanocidal properties of WRR-483 against Trypanosoma cruzi: Y.T. Chen, et al.; PLoS Negl. Trop. Dis. 4, e825 (2010)
  • Cure of hookworm infection with a cysteine protease inhibitor: J.J. Vermeire, et al.; PLoS Negl. Trop. Dis. 6, e1680 (2012)
  • Mapping inhibitor binding modes on an active cysteine protease via NMR spectroscopy: G.M. Lee, et al.; Biochem. 51, 10087 (2012)