PROTAC SARS-CoV-2 Mpro degrader-3
PROTAC SARS-CoV-2 Mpro degrader-3 is a SARS-CoV-2 Mpro PROTAC degrader with a DC50 of 27 μM in HEK 293T cells. It also acts as an inhibitor of HCoV-229E, HCoV-OC43 and SARS-CoV-2 Mpro, with an IC50 of 0.748 μM and a Kd of 37 μM against SARS-CoV-2 Mpro. PROTAC SARS-CoV-2 Mpro degrader-3 forms a ternary complex with purified SARS-CoV-2 Mpro and VCB E3 ligase to induce intracellular protease degradation. It reduces coronavirus replication and can be used in research on coronavirus infections.
(Pink: SARS-CoV ligand (HY-161790); Blue: VHL ligand (HY-125845); Black: linker (HY-161792)).
For research use only. We do not sell to patients.
- Formula: C53H73N10NaO14S2
- Molecular Weight:1161.33
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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-3 (Compound P2) (3-5 days) inhibits the replication of HCoV-229E in Huh-7 cells with an EC50 of 4.6 μM, and shows no cytotoxicity at a concentration of 100 μM[1].
PROTAC SARS-CoV-2 Mpro degrader-3 (3-5 days) inhibits the replication of HCoV-OC43 in RD cells, with an EC50 of 4.6 μM[1].
PROTAC SARS-CoV-2 Mpro degrader-3 (3-5 days) inhibits the replication of SARS-CoV-2 in Vero cells, with an EC50 of 0.71 μM[1].
PROTAC SARS-CoV-2 Mpro degrader-3 (pre-incubated for 15 min; substrate incubated for 1 h) inhibits purified SARS-CoV-2 Mpro, with an IC50 of 0.748 μM and a Kd of 37 μM[1].
PROTAC SARS-CoV-2 Mpro degrader-3 binds to the purified VCB E3 ligase complex with a Kd value of 37 nM[1].
PROTAC SARS-CoV-2 Mpro degrader-3 (injected at 50 μM for 120 seconds, followed by injection of 0.25/1 μM VCB for 120 seconds) forms a ternary complex with purified SARS-CoV-2 Mpro and the VCB E3 ligase complex[1].
PROTAC SARS-CoV-2 Mpro degrader-3 (compound P2) (1.5-50 μM; 24 h, with 4 h GC376 pre-incubation) induces SARS-CoV-2 Mpro degradation in stably transfected HEK 293T cells, with a DC50 of 27 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK 293T cells stably overexpressing SARS-CoV-2 Mpro
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Concentration:1.5, 3.0, 6.0, 12.5, 25.0, 50.0 μM
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Incubation Time:24 h
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Result:Induced significant degradation of SARS-CoV-2 Mpro at 6.0 μM, with a 50% degradation concentration (DC50) of 27 μM.
Chemical Information
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Molecular Weight 1161.33
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Formula C53H73N10NaO14S2
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SMILES
O=C(N[C@@H](C(C)(C)C)C(N1C[C@H](O)C[C@H]1C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)COCCCCCN4N=NC(COC5=CC=C(COC(N[C@H](C(N[C@@H](C[C@@H]6CCNC6=O)C(O)S(=O)(O[Na])=O)=O)CC(C)C)=O)C=C5)=C4
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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)