PROTAC SARS-CoV-2 Mpro degrader-8
PROTAC SARS-CoV-2 Mpro degrader-8 is an antiviral PROTAC degrader targeting the SARS-CoV-2 main protease (Mpro), with weak direct binding affinity to Mpro (Kd=80.5 μM). PROTAC SARS-CoV-2 Mpro degrader-8 exhibits broad-spectrum antiviral activity against SARS-CoV-2 and the human endemic coronavirus HCoV-OC43. It can be used for research on coronavirus infections.
(Pink: SARS-CoV-2 Mpro ligand (HY-181904); Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Formula: C53H59F3N10O6S2
- Molecular Weight:1053.22
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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
- Purity & Documentation
- References
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Biological Activity
(Pink: SARS-CoV-2 Mpro ligand (HY-181904); Blue: VHL ligand (HY-112078); Black: linker).
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VHL |
PROTAC SARS-CoV-2 Mpro degrader-8 (PROTAC 6) does not inhibit the catalytic activity of purified SARS-CoV-2 Mpro[1].
PROTAC SARS-CoV-2 Mpro degrader-8 inhibits the replication of SARS-CoV-2 in Vero E6 cells with an EC50 of 8.3 μM, and shows no cytotoxicity at the highest concentration of 125 μM[1].
PROTAC SARS-CoV-2 Mpro degrader-8 (0.1-25 μM; 24 h) induces VHL- and proteasome-dependent degradation of SARS-CoV-2 Mpro in 293T-hACE2 cells, with a DC50 of 0.9 μM and a maximum degradation rate of 89% at 25 μM[1].
PROTAC SARS-CoV-2 Mpro degrader-8 inhibits the replication of SARS-CoV-2 in human lung Calu-3 cells with an EC50 of 2.5 μM, and shows no cytotoxicity at the highest concentration of 125 μM[1].
PROTAC SARS-CoV-2 Mpro degrader-8 inhibits the replication of human endemic coronavirus HCoV-OC43 in MRC-5 cells with an EC50 of 20.6 μM, and shows no cytotoxicity at the highest concentration of 125 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SARS-CoV-2-infected 293T-hACE2 cells
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Concentration:0.1-25 μM; 100 μM (VHL inhibitor VH298 co-treatment); 1 μM (proteasome inhibitor MG132 treatment)
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Incubation Time:24 h (post-treatment)
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Result:Induced concentration-dependent degradation of SARS-CoV-2 Mpro, with a DC50 of 0.9 μM and a Dmax of 89% ± 9% at 25 μM.
Increased the DC50 to 4.1 μM when co-treated with 100 μM VHL inhibitor VH298.
Rescued Mpro levels when treated with 1 μM proteasome inhibitor MG132.
Chemical Information
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Molecular Weight 1053.22
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Formula C53H59F3N10O6S2
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SMILES
O=C(C1=C2N=C(C3=CC=CC=C3)C=C(C(F)(F)F)N2N=C1)NC4=C(C(N5CCN(CCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(N[C@H](C7=CC=C(C8=C(C)N=CS8)C=C7)C)=O)C[C@@H](O)C6)=O)=O)CC5)=O)C(CCCC9)=C9S4
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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-8 Related Classifications
HY-181870 Related Classifications
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