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
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Biological Activity
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Cereblon |
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.
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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.
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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