K777 tosylate
Based on 3 publication(s) in Google Scholar
K777 tosylate is a potent, orally active and irreversible cysteine protease inhibitor. K777 tosylate is also a potent CYP3A4 inhibitor with an IC50 of 60 nM. K777 tosylate irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 tosylate is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 tosylate inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.
For research use only. We do not sell to patients.
- CAS No.: 502960-91-0
- Formula: C39H46N4O7S2
- Molecular Weight:746.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) K777 tosylate
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Biological Activity
K777 (K11777) tosylate can inhibit entry driven by other viral envelope proteins, including HIV-based pseudotypes bearing spikes from coronaviruses (SARS-CoV, HCoV-229E, NL63, MERS-CoV) or glycoproteins from filoviruses (EBOV, SUDV, TAFV, RESTV, BEBOV and MARV).
K777 tosylate inhibits SARS-CoV, HCoV-229E, NL63, MERS-CoV, EBOV, SUDV, TAFV, RESTV, BEBOV, MARV and Nipah pseudovirus entry with IC50 values of 0.68 nM, 1.48 nM, 6.78 nM, 46.12 nM, 0.87 nM, 1.14 nM, 2.26 nM, 3.37 nM, 5.91 nM, 1.9 nM and 0.42 nM, respectively.
In contrast, 100 nM K777 tosylate does not inhibit infection mediated by envelope glycoproteins from an alphavirus (CHIKV), a rhabdovirus (VSV), a flavivirus (HCV), the retroviruses MLV-A and XMRV or two arenaviruses, Lassa and Junin virus[1].
K777 tosylate alone demonstrates up to ~70% inhibition of 229E-S-mediated transduction. Simultaneous treatment with Camostat and K777 tosylate increases inhibition to ~ 90%. Similar inhibition patterns are obtained using the human intestinal epithelial cell line Caco-2, which express endogenous TMPRSS2 and cathepsins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 IFN-γR-KO mice (6-8 weeks of age) injected with Cryptosporidium parvum[3]
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Dosage:35 mg/kg, 70 mg/kg, and 105 mg/kg
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Administration:Oral administration; twice a day; for 10 days
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Result:Rescued mice from otherwise lethal infections.
Chemical Information
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CAS No. 502960-91-0
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Molecular Weight 746.94
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Formula C39H46N4O7S2
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SMILES
O=S(O)(C1=CC=C(C=C1)C)=O.O=S(/C=C/[C@H](CCC2=CC=CC=C2)NC([C@@H](NC(N3CCN(CC3)C)=O)CC4=CC=CC=C4)=O)(C5=CC=CC=C5)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Immunity
Spatiotemporal dynamics of CXCL10 encode contextual immune information revealed by the genetically encoded fluorescent sensor. [Abstract]2025 Sep 9;58(9):2320-2335.e9. PMID: 40818452 -
eGastroenterology
2026 Mar 31;4(1):e100348. PMID: 41948149 -
Purity & Documentation
References
[1]. Zhou Y, et al. Protease inhibitors targeting coronavirus and filovirus entry. Antiviral Res. 2015 Apr;116:76-84. [Content Brief]
[2]. Jacobsen W, et al. In vitro evaluation of the disposition of A novel cysteine protease inhibitor. Drug Metab Dispos. 2000 Nov;28(11):1343-51. [Content Brief]
[3]. Ndao M, et al. A cysteine protease inhibitor rescues mice from a lethal Cryptosporidium parvum infection. Antimicrob Agents Chemother. 2013 Dec;57(12):6063-73. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)