2. PROTAC Anti-infection
  3. PROTACs SARS-CoV Virus Protease
  4. 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.

PROTAC SARS-CoV-2 Mpro degrader-5

PROTAC SARS-CoV-2 Mpro degrader-5 Chemical Structure

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PROTAC SARS-CoV-2 Mpro degrader-5 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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[1].

IC50 & Target

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.

PROTAC SARS-CoV-2 Mpro degrader-5 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293 cells stably expressing SARS-CoV-2 Mpro
Concentration: 0.125 μM, 0.25 μM, 0.5 μM, 1 μM, 2.5 μM, 5 μM, 10 μM, 20 μM
Incubation Time: 72 h
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.

Western Blot Analysis[1]

Cell Line: HEK293 cells stably expressing SARS-CoV-2 Mpro
Concentration: 10 μM
Incubation Time: 72 h
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.
Molecular Weight

647.72

Formula

C34H41N5O8
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC SARS-CoV-2 Mpro degrader-5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC SARS-CoV-2 Mpro degrader-5PROTACsSARS-CoVVirus ProteaseSARS coronavirusK48-linked polyubiquitinationubiquitin-proteasome systemproteasome-dependent turnoverhuman embryonic kidney cellsHEK293 stable cellsSARS-CoV-2 main proteaseCRBN E3 ubiquitin ligasecovid-19Inhibitorinhibitorinhibit

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