PROTAC SARS-CoV-2 Mpro degrader-5
PROTAC SARS-CoV-2 Mpro degrader-5 is a SARS-CoV-2 main protease (Mpro) PROTAC. PROTAC SARS-CoV-2 Mpro degrader-5 engages CRBN E3 ubiquitin ligase to form a ternary complex with SARS-CoV-2 Mpro, induces K48-linked polyubiquitination of SARS-CoV-2 Mpro, and drives proteasome-dependent turnover of SARS-CoV-2 Mpro with a high selectivity index (CC50/DC50 > 10) in human embryonic kidney cells.PROTAC SARS-CoV-2 Mpro degrader-5 can be used for the research of COVID-19.
For research use only. We do not sell to patients.
- Formula: C34H41N5O8
- Molecular Weight:647.72
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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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Biological Activity
Description
IC50 & Target
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Cereblon |
In Vitro
PROTAC SARS-CoV-2 Mpro degrader-5 (PROTAC A) (0.125-20 μM; 72 h) effectively induces dose-dependent degradation of SARS-CoV-2 Mpro in HEK293 stable cells with a DC50 of 0.883 μM and a maximum degradation rate of 68.5%, and has a selectivity index greater than 10[1].
PROTAC SARS-CoV-2 Mpro degrader-5 (10 μM; 72 h) induces K48-linked polyubiquitination of SARS-CoV-2 Mpro in HEK293 stable cells, mediating degradation via the ubiquitin-proteasome system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HEK293 cells stably expressing SARS-CoV-2 Mpro
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Concentration:0.125 μM, 0.25 μM, 0.5 μM, 1 μM, 2.5 μM, 5 μM, 10 μM, 20 μM
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Incubation Time:72 h
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Result:Induced dose-dependent degradation of Mpro with a DC50 value of 0.883 μM and a maximum degradation rate of 68.5%.
Exhibited a CC50 value (cytotoxic concentration) of 42.07 μM, resulting in a selectivity index (CC50/DC50) greater than 10.
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Cell Line:HEK293 cells stably expressing SARS-CoV-2 Mpro
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Concentration:10 μM
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Incubation Time:72 h
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Result:Increased K48-linked polyubiquitination of Mpro significantly compared to the control. Confirmed proteasomal involvement, as co-treatment with the proteasome inhibitor MG132 (2 μM for 18 hours) suppressed Mpro degradation.
Chemical Information
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Molecular Weight 647.72
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Formula C34H41N5O8
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SMILES
CC(C)[C@H](NC([C@H](CC1=CC=CC=C1)NC(CCCCCNC2=C3C(N(C4CCC(NC4=O)=O)C(C3=CC=C2)=O)=O)=O)=O)C(OC)=O
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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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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)
PROTAC SARS-CoV-2 Mpro degrader-5 Related Classifications
HY-181154 Related Classifications
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