Y-U0-R
Y-U0-R is a potent covalent inhibitor of coronavirus main protease (Mpro), with IC50 values of 0.22 and 0.25 μM against SARS-CoV-2 Mpro and SARS-CoV Mpro, respectively. Y-U0-R exhibits broad-spectrum anti-coronavirus activity, with an EC50 of 0.47 µM against SARS-CoV-2. Y-U0-R forms a stable hemithioacetal covalent bond with the catalytic residue C145 through its aldehyde warhead, and occupies multiple active subsites and residue networks, resulting in time-dependent irreversible inhibition of enzymatic activity. Y-U0-R can be used for research on COVID-19 and SARS-CoV-2 infection.
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Cathepsin Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
SARS-CoV-2 Mpro 0.22 μM (IC50) |
SARS-CoV Mpro 0.25 μM (IC50) |
Cathepsin B 2.58 μM (IC50) |
cathepsin L 34.79 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 |
0.47 μM
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Antiviral activity against wild-type SARS-CoV-2 in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
Antiviral activity against wild-type SARS-CoV-2 in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
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42679698 |
| Calu-3 | CC50 |
41.3 μM
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Cytotoxicity against mock-infected human lung epithelial Calu-3 cells assessed by MTT assay on day 2.
Cytotoxicity against mock-infected human lung epithelial Calu-3 cells assessed by MTT assay on day 2.
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42679698 |
| Calu-3 | EC50 |
1.44 μM
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Antiviral activity against SARS-CoV-2 Gamma variant in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
Antiviral activity against SARS-CoV-2 Gamma variant in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
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42679698 |
| Calu-3 | EC50 |
2.79 μM
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Antiviral activity against SARS-CoV-2 Delta variant in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
Antiviral activity against SARS-CoV-2 Delta variant in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
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42679698 |
| Calu-3 | EC50 |
0.58 μM
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Antiviral activity against SARS-CoV-2 Omicron variant in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
Antiviral activity against SARS-CoV-2 Omicron variant in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
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42679698 |
| Calu-3 | EC50 |
2.77 μM
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Antiviral activity against reverse-genetic wild-type SARS-CoV-2 in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
Antiviral activity against reverse-genetic wild-type SARS-CoV-2 in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
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42679698 |
| Calu-3 | EC50 |
9.92 μM
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Antiviral activity against reverse-genetic SARS-CoV-2 Mpro T21I/E166V mutant in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
Antiviral activity against reverse-genetic SARS-CoV-2 Mpro T21I/E166V mutant in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
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42679698 |
| Calu-3 | EC50 |
3.57 μM
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Antiviral activity against reverse-genetic SARS-CoV-2 Mpro L50F/E166V mutant in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
Antiviral activity against reverse-genetic SARS-CoV-2 Mpro L50F/E166V mutant in human lung epithelial Calu-3 cells infected at MOI 0.01 assessed as spike protein or GFP immunostaining at 2 days post-infection.
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42679698 |
In Vitro
Y-U0-R retains inhibitory activity against SARS-CoV-2 Mpro mutants T21I/E166V and L50F/E166V, with IC50 values of 2.89 μM and 2.30 μM, respectively[1].
Y-U0-R inhibits cathepsin B and cathepsin L with IC50 values of 2.58 μM and 34.79 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-R Related Classifications
HY-189663 Related Classifications
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