2. PROTAC Anti-infection
  3. PROTACs SARS-CoV Virus Protease
  4. PROTAC SARS-CoV-2 Mpro degrader-7

PROTAC SARS-CoV-2 Mpro degrader-7 is a SARS-CoV-2 main protease (Mpro) PROTAC degrader with a DC50 of 0.985 μM. PROTAC SARS-CoV-2 Mpro degrader-7 promotes K48-linked polyubiquitination of SARS-CoV-2 Mpro, leading to proteasome-dependent degradation via the ubiquitin-proteasome system.PROTAC SARS-CoV-2 Mpro degrader-7 forms a ternary complex with SARS-CoV-2 Mpro and CRBN E3 ubiquitin ligase to enable viral protease ubiquitination.PROTAC SARS-CoV-2 Mpro degrader-7 exhibits a high selectivity index, and induces dose-dependent degradation of SARS-CoV-2 Mpro in stable cells expressing the viral protease.PROTAC SARS-CoV-2 Mpro degrader-7 can be used for the research of COVID-19.

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PROTAC SARS-CoV-2 Mpro degrader-7

PROTAC SARS-CoV-2 Mpro degrader-7 Chemical Structure

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PROTAC SARS-CoV-2 Mpro degrader-7 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

PROTAC SARS-CoV-2 Mpro degrader-7 is a SARS-CoV-2 main protease (Mpro) PROTAC degrader with a DC50 of 0.985 μM. PROTAC SARS-CoV-2 Mpro degrader-7 promotes K48-linked polyubiquitination of SARS-CoV-2 Mpro, leading to proteasome-dependent degradation via the ubiquitin-proteasome system.PROTAC SARS-CoV-2 Mpro degrader-7 forms a ternary complex with SARS-CoV-2 Mpro and CRBN E3 ubiquitin ligase to enable viral protease ubiquitination.PROTAC SARS-CoV-2 Mpro degrader-7 exhibits a high selectivity index, and induces dose-dependent degradation of SARS-CoV-2 Mpro in stable cells expressing the viral protease.PROTAC SARS-CoV-2 Mpro degrader-7 can be used for the research of COVID-19[1].

IC50 & Target

Cereblon

 

In Vitro

PROTAC SARS-CoV-2 Mpro degrader-7 (PROTAC C) (0.0781-10 μM; 72 h) effectively induces dose-dependent degradation of SARS-CoV-2 Mpro in HEK293 stable cells with a DC50 of 0.985 μM[1].
PROTAC SARS-CoV-2 Mpro degrader-7 (72 h) has low cytotoxicity in HEK293 cells, with a CC50 of 23.5 μM and a high selectivity index[1].
PROTAC SARS-CoV-2 Mpro degrader-7 (2.5 μM; 72 h, co-treated with 2 μM MG-132 (HY-13259) for 18 h) induces Mpro degradation via the ubiquitin-proteasome system in HEK293 stable cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC SARS-CoV-2 Mpro degrader-7 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293 stable cells expressing Flag-Mpro
Concentration: 0.0781 μM, 0.1563 μM, 0.3125 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 72 h
Result: Induced dose-dependent degradation of Mpro with a DC50 value of 0.985 μM and a maximum degradation rate of 79.4%.

Western Blot Analysis[1]

Cell Line: HEK293 stable cells expressing Flag-Mpro
Concentration: 2.5 μM (PROTAC); 2 μM MG-132 (proteasome inhibitor, co-treatment)
Incubation Time: 72 h (PROTAC); 18 h (MG132 co-treatment)
Result: Enhanced K48-linked polyubiquitination of Mpro, and suppressed Mpro degradation when co-treated with MG-132.
Molecular Weight

661.74

Formula

C35H43N5O8
SMILES

COC([C@H](CC(C)C)NC([C@H](CC1=CC=CC=C1)NC(CCCCCNC2=C3C(N(C4CCC(NC4=O)=O)C(C3=CC=C2)=O)=O)=O)=O)=O
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Room temperature in continental US; may vary elsewhere.
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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-7 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-7PROTACsSARS-CoVVirus ProteaseSARS coronavirusHEK293 cellsviral proteaseK48-linked polyubiquitinationubiquitin-proteasome systemHEK293 stable cellsternary complexproteasome-dependent degradationSARS-CoV-2 main proteaseCRBN E3 ubiquitin ligasecovid-19Inhibitorinhibitorinhibit

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