PROTAC SARS-CoV-2 Mpro degrader-4
PROTAC SARS-CoV-2 Mpro degrader-4 is a SARS-CoV-2 MPro PROTAC degrader with antiviral activity, with a DC50 value of 4.7 μM. PROTAC SARS-CoV-2 Mpro degrader-4 induces MPro ubiquitination and proteasomal degradation, and inhibits SARS-CoV-2 replication. PROTAC SARS-CoV-2 Mpro degrader-4 can be used in the research of coronavirus infections.
(Pink: SARS-CoV ligand (HY-32717); Blue: Cereblon ligand (HY-42771); Black: linker (HY-42149)).
For research use only. We do not sell to patients.
- Formula: C40H37ClFN7O10
- Molecular Weight:830.21
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
PROTAC SARS-CoV-2 Mpro degrader-4 (LLP019) (0.1-100 μM; 24 h) dose-dependently degrades MPro protein in HEK293F cells without obvious cytotoxicity[1].
PROTAC SARS-CoV-2 Mpro degrader-4 (25 μM; 5 h) degrades approximately 40% of MPro protein in HEK293F cells co-treated with Cycloheximide (HY-12320)[1].
PROTAC SARS-CoV-2 Mpro degrader-4 (12.5-50 μM; 48 h) potently inhibits the replication of SARS-CoV-2 (BavPat1/2020) and SARS-CoV-2 Delta variant (FFM-IND8424/2021) in Calu3 cells, but only partially inhibits SARS-CoV replication and shows no inhibitory effect on MERS-CoV replication[1].
PROTAC SARS-CoV-2 Mpro degrader-4 (25 μM; 5 h) exerts a ubiquitin-proteasome system (UPS)-dependent MPro protein degradation effect in HEK293F cells co-treated with Pevonedistat (HY-70062) or TAK243 (TAK-243), with degradation being inhibited[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293F
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Concentration:195 nM, 390 nM, 780 nM, 1.56 μM, 3.13 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM
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Incubation Time:24 h
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Result:Degraded ectopically expressed MPro in a dose-dependent manner, exhibiting maximal degradation up to 50 μM, and showing a hook effect with reversed degradation activity at 100 μM.
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Cell Line:HEK293F
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Concentration:25 μM
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Incubation Time:5 h (in the presence of cycloheximide and pevonedistat or TAK243)
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Result:The MPro degradation induced by PROTAC SARS-CoV-2 Mpro degrader-4 was blocked by the NEDD8-activating enzyme inhibitor pevonedistat and the ubiquitin-activating enzyme inhibitor TAK243, indicating that the degradation is dependent on the host's ubiquitin-proteasome system (UPS).
Chemical Information
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Molecular Weight 830.21
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Formula C40H37ClFN7O10
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SMILES
CCOC1=C(NC(CCOCCOCCNC(COC2=C(C(N(C3CCC(NC3=O)=O)C4=O)=O)C4=CC=C2)=O)=O)C=C(C(NC5=CC(Cl)=C(F)C=C5)=C(C#N)C=N6)C6=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)