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 (2 days post-infection) inhibits wild-type SARS-CoV-2 in Calu-3 cells with EC50 = 0.47 μM and CC50 = 41.3 μM, and retains antiviral activity against Gamma, Delta, Omicron, and Nirmatrelvir (HY-138687)-resistant Mpro mutants[1].
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 SARS-CoV-2 Mpro and SARS-CoV Mpro, with submicromolar IC50 values of 0.22 μM and 0.25 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. Further protocols information, click here.
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.
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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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-R Related Classifications
HY-189663 Related Classifications
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