Y-U0-S
Y-U0-S is a potent inhibitor of the coronavirus main protease (Mpro) and host cathepsins. The IC50 values of Y-U0-S against SARS-CoV-2 Mpro, SARS-CoV Mpro, Cathepsin B, and Cathepsin L are 0.81, 1.14, 0.86, and 21.13 μM, respectively. Y-U0-S exhibits broad-spectrum anti-coronavirus activity, with an EC50 of 0.22 μM against wild-type SARS-CoV-2. Y-U0-S forms an irreversible covalent bond with the catalytic site C145 of Mpro through its aldehyde warhead, and by optimizing multi-site occupancy of the scaffold to engage conserved residues, it effectively blocks enzyme activity and inhibits viral replication. Y-U0-S can be used for research on COVID-19.
For research use only. We do not sell to patients.
- Formula: C25H24ClFN4O3S
- Molecular Weight:515.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Cathepsin Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
Cathepsin B 0.86 μM (IC50) |
cathepsin L 21.13 μM (IC50) |
SARS-CoV-2 Mpro 0.81 μM (IC50) |
SARS-CoV Mpro 1.14 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Calu-3 | EC50 |
0.22 μM
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Antiviral activity against wild-type SARS-CoV-2 in human lung epithelial Calu-3 cells assessed by immunofluorescence for spike expression on day 2 after infection.
Antiviral activity against wild-type SARS-CoV-2 in human lung epithelial Calu-3 cells assessed by immunofluorescence for spike expression on day 2 after infection.
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42679698 |
| Calu-3 | CC50 |
34.4 μM
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Cytotoxicity against mock-infected human lung epithelial Calu-3 cells by MTT assay after 2 days.
Cytotoxicity against mock-infected human lung epithelial Calu-3 cells by MTT assay after 2 days.
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42679698 |
| Calu-3 | EC50 |
1.38 μM
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Antiviral activity against SARS-CoV-2 Gamma variant in human lung epithelial Calu-3 cells assessed by immunofluorescence for spike expression on day 2 after infection.
Antiviral activity against SARS-CoV-2 Gamma variant in human lung epithelial Calu-3 cells assessed by immunofluorescence for spike expression on day 2 after infection.
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42679698 |
| Calu-3 | EC50 |
1.49 μM
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Antiviral activity against SARS-CoV-2 Delta variant in human lung epithelial Calu-3 cells assessed by immunofluorescence for spike expression on day 2 after infection.
Antiviral activity against SARS-CoV-2 Delta variant in human lung epithelial Calu-3 cells assessed by immunofluorescence for spike expression on day 2 after infection.
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42679698 |
| Calu-3 | EC50 |
0.26 μM
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Antiviral activity against SARS-CoV-2 Omicron variant in human lung epithelial Calu-3 cells assessed by immunofluorescence for spike expression on day 2 after infection.
Antiviral activity against SARS-CoV-2 Omicron variant in human lung epithelial Calu-3 cells assessed by immunofluorescence for spike expression on day 2 after infection.
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42679698 |
| Calu-3 | EC50 |
1.19 μM
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Antiviral activity against reverse genetically generated wild-type rgSARS-CoV-2 in human lung epithelial Calu-3 cells assessed by GFP expression on day 2 after infection.
Antiviral activity against reverse genetically generated wild-type rgSARS-CoV-2 in human lung epithelial Calu-3 cells assessed by GFP expression on day 2 after infection.
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42679698 |
| Calu-3 | EC50 |
6.89 μM
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Antiviral activity against reverse genetically generated SARS-CoV-2 Mpro T21I/E166V mutant in human lung epithelial Calu-3 cells assessed by GFP expression on day 2 after infection.
Antiviral activity against reverse genetically generated SARS-CoV-2 Mpro T21I/E166V mutant in human lung epithelial Calu-3 cells assessed by GFP expression on day 2 after infection.
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42679698 |
| Calu-3 | EC50 |
3.52 μM
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Antiviral activity against reverse genetically generated SARS-CoV-2 Mpro L50F/E166V mutant in human lung epithelial Calu-3 cells assessed by GFP expression on day 2 after infection.
Antiviral activity against reverse genetically generated SARS-CoV-2 Mpro L50F/E166V mutant in human lung epithelial Calu-3 cells assessed by GFP expression on day 2 after infection.
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42679698 |
In Vitro
Y-U0-S (2 days) maintains broad-spectrum antiviral activity against Gamma, Delta, Omicron, and Nirmatrelvir (HY-138687)-resistant Mpro mutants in Calu-3 cells, with EC50 values ranging from 0.26 to 6.89 μM[1].
Y-U0-S inhibits the enzymatic activity of the Nirmatrelvir-resistant mutants Mpro (T211/E166V) and Mpro (L50F/E166V) in a recombinant protein system, with IC50 values of 7.03 μM and 6.27 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 515.00
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Formula C25H24ClFN4O3S
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SMILES
O=C(NCC1=CC=CS1)C(C2=CC(F)=CC(Cl)=C2)N3C[C@@H](C=O)N(C(C4=CN=CC(C)=C4)=O)CC3
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Y-U0-S Related Classifications
HY-189662 Related Classifications
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