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
-
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]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
All Cathepsin Isoforms
More
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
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Calu-3 | EC50 |
0.22 μM
|
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.
|
42679698 |
| Calu-3 | CC50 |
34.4 μM
|
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.
|
42679698 |
| Calu-3 | EC50 |
1.38 μM
|
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.
|
42679698 |
| Calu-3 | EC50 |
1.49 μM
|
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.
|
42679698 |
| Calu-3 | EC50 |
0.26 μM
|
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.
|
42679698 |
| Calu-3 | EC50 |
1.19 μM
|
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.
|
42679698 |
| Calu-3 | EC50 |
6.89 μM
|
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.
|
42679698 |
| Calu-3 | EC50 |
3.52 μM
|
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.
|
42679698 |
In Vitro
Y-U0-S (2 days) inhibits wild-type SARS-CoV-2 in Calu-3 cells with an EC50 of 0.22 μM and a CC50 of 34.4 μM[1].
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 exhibits inhibitory activity against SARS-CoV-2 Mpro, SARS-CoV Mpro, Cathepsin B, and Cathepsin L in recombinant protease systems, with IC50 values of 0.81, 1.14, 0.86, and 21.13 μM[1], respectively.
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. Further protocols information, click here.
Chemical Information
-
Molecular Weight 515.00
-
Formula C25H24ClFN4O3S
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Y-U0-S Related Classifications
HY-189662 Related Classifications
Powered by Bioz