PROTAC SARS-CoV-2 Mpro degrader-2
PROTAC SARS-CoV-2 Mpro degrader-2 is a SARS-CoV-2 Mpro PROTAC degrader with a DC50 of 1.34 μM. PROTAC SARS-CoV-2 Mpro degrader-2 recruits the VHL E3 ligase to mediate ubiquitination and proteasomal degradation of SARS-CoV-2 Mpro, without inhibiting the catalytic activity of Mpro. PROTAC SARS-CoV-2 Mpro degrader-2 exhibits anti-SARS-CoV-2 activity in infected cells, as well as broad-spectrum antiviral activity against coronaviruses including HCoV-OC43 and HCoV-229E. PROTAC SARS-CoV-2 Mpro degrader-2 can be used in studies related to SARS-CoV-2 infection, HCoV-OC43 infection, and HCoV-229E infection.
(Pink: SARS-CoV-2 Mpro ligand (HY-14397); Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3057294-32-0
- Formula: C48H56ClN7O7S
- Molecular Weight:910.52
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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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Biological Activity
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VHL |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Calu-3 | CC50 |
>125 μM
Compound: 6
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Cytotoxicity against human Calu-3 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human Calu-3 cells incubated for 72 hrs by MTT assay
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[PMID: 38394929] |
| MRC5 | CC50 |
>125 μM
Compound: 6
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Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 38394929] |
| Vero | CC50 |
>125 μM
Compound: 6
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 38394929] |
PROTAC SARS-CoV-2 Mpro degrader-2 (Compound 6) potently inhibits the replication of SARS-CoV-2 in Vero E6 cells (EC50 = 10.8 μM), as well as the replication of HCoV-OC43 (EC50 = 1.6 μM) and HCoV-229E (EC50 = 6.5 μM) in MRC-5 cells, at non-toxic concentrations[1].
PROTAC SARS-CoV-2 Mpro degrader-2 potently inhibits SARS-CoV-2 replication in Calu-3 lung cells at non-toxic concentrations (EC50 = 0.89 μM)[1].
PROTAC SARS-CoV-2 Mpro degrader-2 (1-25 μM; 24 h) degrades overexpressed SARS-CoV-2 Mpro in a concentration-dependent manner in 293T cells, with a DC50 of 7.3 μM and a degradation rate of 72% at 25 μM, and does not inhibit the catalytic activity of Mpro[1].
PROTAC SARS-CoV-2 Mpro degrader-2 (1-25 μM; 48 h) induces concentration-dependent degradation of virally expressed SARS-CoV-2 Mpro in infected Calu-3 cells, with a DC50 of 1.34 μM[1].
PROTAC SARS-CoV-2 Mpro degrader-2 (10 μM; 0-60 min at 37 °C) exhibits favorable metabolic stability in liver microsomes, with a half-life of >60 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:293T (pcDNA3.1-Mpro-transfected)
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Concentration:1-25 μM
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Incubation Time:24 h (post-transfection)
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Result:Induced concentration-dependent degradation of overexpressed SARS-CoV-2 Mpro, with a DC50 of 7.3 μM.
Resulted in 72% degradation of Mpro at 25 μM.
Did not inhibit Mpro catalytic activity, as evidenced by the lack of detectable full-length FLAG-nsp4-Mpro fusion protein.
Chemical Information
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CAS No. 3057294-32-0
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Molecular Weight 910.52
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Formula C48H56ClN7O7S
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SMILES
ClC1=CC=C(C(N2C3=CC=C(OC)C=C3C(CC(N4CCN(CC4)CC(N[C@H](C(N5[C@@H](C[C@H](C5)O)C(N[C@@H](C)C6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)C(C)(C)C)=O)=O)=C2C)=O)C=C1
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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)
PROTAC SARS-CoV-2 Mpro degrader-2 Related Classifications
HY-157805 Related Classifications
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