K777
Based on 3 publication(s) in Google Scholar
K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.14%
- CAS. Nr.: 233277-99-1
- Formel: C32H38N4O4S
- Molecular Weight:574.73
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Publications Citing Use of MedChemExpress (MCE) K777
MoreAlle Cathepsin Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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CYP3 |
EBOV |
MARV |
Trypanosoma |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C2C12 | CC50 |
>10 μM
Compound: K11777
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Cytotoxicity against mouse C2C12 cells assessed as reduction in cell viability measured after 48 hrs by 4',6-diamidino-2-phenylindole staining based microscopic analysis
Cytotoxicity against mouse C2C12 cells assessed as reduction in cell viability measured after 48 hrs by 4',6-diamidino-2-phenylindole staining based microscopic analysis
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[PMID: 32125159] |
| HEK-293T | CC50 |
>10 μM
Compound: 48; K11777
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Cytotoxicity against human HEK293T cells
Cytotoxicity against human HEK293T cells
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[PMID: 33486200] |
| HEK-293T | IC50 |
<7 nM
Compound: 48; K11777
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Antiviral activity against Human coronavirus NL63 infected in HEK293T cells expressing human ACE2 assessed as inhibition of viral replication incubated for 2 days by Dual-Glo luciferase assay
Antiviral activity against Human coronavirus NL63 infected in HEK293T cells expressing human ACE2 assessed as inhibition of viral replication incubated for 2 days by Dual-Glo luciferase assay
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[PMID: 33486200] |
| HEK-293T | IC50 |
0.36 nM
Compound: 3a; K11777
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Antiviral activity against Ebola virus pseudotyped infected in HEK293T cells assessed as reduction in viral cytopathic effect
Antiviral activity against Ebola virus pseudotyped infected in HEK293T cells assessed as reduction in viral cytopathic effect
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[PMID: 35305462] |
| HEK-293T | IC50 |
0.68 nM
Compound: 48; K11777
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Antiviral activity against SARS-CoV infected in HEK293T cells expressing human ACE2 assessed as inhibition of viral replication incubated for 2 days by Dual-Glo luciferase assay
Antiviral activity against SARS-CoV infected in HEK293T cells expressing human ACE2 assessed as inhibition of viral replication incubated for 2 days by Dual-Glo luciferase assay
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[PMID: 33486200] |
| HeLa | CC50 |
>10 μM
Compound: K11777
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Cytotoxicity against human HeLa cells by Alamar blue assay
Cytotoxicity against human HeLa cells by Alamar blue assay
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[PMID: 34378914] |
| J774.1 | CC50 |
41 μM
Compound: K11777
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Cytotoxicity against mouse J774.1 cells by Alamar blue assay
Cytotoxicity against mouse J774.1 cells by Alamar blue assay
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[PMID: 34378914] |
| J774.1 | CC50 |
41 μM
Compound: K11777
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Cytotoxicity against mouse J774.1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse J774.1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 35597010] |
| Jurkat | GI50 |
7 μM
Compound: 1, K-777
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Antiparasitic activity against Trypanosoma brucei brucei infected human Jurkat cells
Antiparasitic activity against Trypanosoma brucei brucei infected human Jurkat cells
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[PMID: 19773167] |
| NHDF | CC50 |
60 μM
Compound: K11777
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Cytotoxicity against HDF cells assessed as reduction in cell viability measured after 48 hrs by resazurin dye based fluorescence assay
Cytotoxicity against HDF cells assessed as reduction in cell viability measured after 48 hrs by resazurin dye based fluorescence assay
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[PMID: 32125159] |
| Vero | CC50 |
>10 μM
Compound: 21; K11777
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Cytotoxicity against african green monkey Vero cells incubated for 3 days
Cytotoxicity against african green monkey Vero cells incubated for 3 days
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[PMID: 32539378] |
| Vero | IC50 |
46 nM
Compound: 48; K11777
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Antiviral activity against recombinant MERS-CoV pseudovirus infected in Vero cells assessed as inhibition of viral replication incubated for 2 days by Dual-Glo luciferase assay
Antiviral activity against recombinant MERS-CoV pseudovirus infected in Vero cells assessed as inhibition of viral replication incubated for 2 days by Dual-Glo luciferase assay
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[PMID: 33486200] |
K777 (K11777) 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 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 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 alone demonstrates up to ~ 70% inhibition of 229E-S-mediated transduction. Simultaneous treatment with Camostat and K777 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. Nr. 233277-99-1
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Appearance Solid
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Molecular Weight 574.73
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Formel C32H38N4O4S
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Color White to off-white
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SMILES
O=C(N1CCN(C)CC1)N[C@@H](CC2=CC=CC=C2)C(N[C@@H](CCC3=CC=CC=C3)/C=C/S(=O)(C4=CC=CC=C4)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
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 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (173.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7399 mL | 8.6997 mL | 17.3995 mL | 43.4987 mL |
| 5 mM | 0.3480 mL | 1.7399 mL | 3.4799 mL | 8.6997 mL | |
| 10 mM | 0.1740 mL | 0.8700 mL | 1.7399 mL | 4.3499 mL | |
| 15 mM | 0.1160 mL | 0.5800 mL | 1.1600 mL | 2.8999 mL | |
| 20 mM | 0.0870 mL | 0.4350 mL | 0.8700 mL | 2.1749 mL | |
| 25 mM | 0.0696 mL | 0.3480 mL | 0.6960 mL | 1.7399 mL | |
| 30 mM | 0.0580 mL | 0.2900 mL | 0.5800 mL | 1.4500 mL | |
| 40 mM | 0.0435 mL | 0.2175 mL | 0.4350 mL | 1.0875 mL | |
| 50 mM | 0.0348 mL | 0.1740 mL | 0.3480 mL | 0.8700 mL | |
| 60 mM | 0.0290 mL | 0.1450 mL | 0.2900 mL | 0.7250 mL | |
| 80 mM | 0.0217 mL | 0.1087 mL | 0.2175 mL | 0.5437 mL | |
| 100 mM | 0.0174 mL | 0.0870 mL | 0.1740 mL | 0.4350 mL |
K777 Related Classifications
HY-119293 Related Classifications
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