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Cat. No.: HY-157804

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PROTAC SARS-CoV-2 Mpro degrader-1

PROTAC SARS-CoV-2 Mpro degrader-1 is a SARS-CoV-2 M^pro PROTAC degrader with a DC₅₀ of 18.1 μM. PROTAC SARS-CoV-2 Mpro degrader-1 recruits the Von-Hippel Lindau (VHL) E3 ligase to mediate ubiquitination and proteasomal degradation of SARS-CoV-2 M^pro, without inhibiting the catalytic activity of M^pro. PROTAC SARS-CoV-2 Mpro degrader-1 exhibits broad-spectrum antiviral activity against coronaviruses (SARS-CoV-2, HCoV-OC43, HCoV-229E). PROTAC SARS-CoV-2 Mpro degrader-1 can be used in studies related to SARS-CoV-2 infection, HCoV-OC43 infection, and HCoV-229E infection.
(Pink: SARS-CoV-2 Mpro ligand (HY-14397); Blue: VHL ligand (HY-112078); Black: linker).

For research use only. We do not sell to patients.

CAS No.: 3029579-46-9
Formula: C₅₂H₆₃ClN₈O₈S
Molecular Weight:995.62

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

PROTAC SARS-CoV-2 Mpro degrader-1 Chemical Structure

CAS No.: 3029579-46-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC SARS-CoV-2 Mpro degrader-1 is a SARS-CoV-2 M^pro PROTAC degrader with a DC₅₀ of 18.1 μM. PROTAC SARS-CoV-2 Mpro degrader-1 recruits the Von-Hippel Lindau (VHL) E3 ligase to mediate ubiquitination and proteasomal degradation of SARS-CoV-2 M^pro, without inhibiting the catalytic activity of M^pro. PROTAC SARS-CoV-2 Mpro degrader-1 exhibits broad-spectrum antiviral activity against coronaviruses (SARS-CoV-2, HCoV-OC43, HCoV-229E). PROTAC SARS-CoV-2 Mpro degrader-1 can be used in studies related to SARS-CoV-2 infection, HCoV-OC43 infection, and HCoV-229E infection^[1]. (Pink: SARS-CoV-2 Mpro ligand (HY-14397); Blue: VHL ligand (HY-112078); Black: linker).

IC₅₀ & Target^[1]

VHL

All PROTACs Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MRC5	CC₅₀	238 μM Compound: 5	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34534839]
MRC5	CC₅₀	238 μM Compound: 5	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 38394929]
Vero	CC₅₀	>250 μM Compound: 5	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 38394929]
Vero C1008	CC₅₀	>250 μM Compound: 5	Cytotoxicity against African green monkey Vero E6 cells assessed as reduction of cell viability measured after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero E6 cells assessed as reduction of cell viability measured after 72 hrs by MTT assay	[PMID: 34534839]

In Vitro

PROTAC SARS-CoV-2 Mpro degrader-1 (Compound 5) potently inhibits SARS-CoV-2 replication in Vero E6 cells at non-toxic concentrations (EC₅₀ = 21.5 μM), and suppresses the replication of a broad spectrum of coronaviruses in MRC-5 cells (EC₅₀ = 2.5 μM against HCoV-OC43, EC₅₀ = 3.2 μM against HCoV-229E)^[1].
PROTAC SARS-CoV-2 Mpro degrader-1 (1-25 μM; 24 h) induces concentration-dependent degradation of overexpressed SARS-CoV-2 M^pro in transfected 293T cells, with a DC₅₀ of 18.1 μM and a degradation rate of 67% at 25 μM, without inhibiting the catalytic activity of M^pro[1].
PROTAC SARS-CoV-2 Mpro degrader-1 (10 μM; 0-60 min) exhibits favorable metabolic stability in liver microsomes, with a half-life >60 min, and undergoes linker-specific N-dealkylation and aliphatic hydroxylation as the major metabolic pathways^[1].

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

Western Blot Analysis^[1]

Cell Line:

293T
Concentration:

1 μM, 10 μM, 25 μM
Incubation Time:

24 h post-transfection
Result:

Induced concentration-dependent degradation of overexpressed SARS-CoV-2 Mpro in transfected 293T cells, with a DC₅₀ of 18.1 μM.
Achieved 67% degradation of Mpro at 25 μM.
Did not affect Mpro catalytic activity, as no cleavage inhibition was observed.

Chemical Information

CAS No. 3029579-46-9
Molecular Weight 995.62
Formula C₅₂H₆₃ClN₈O₈S
SMILES

ClC1=CC=C(C(N2C3=CC=C(OC)C=C3C(CC(NCCN4CCN(CC4)C(CCC(N[C@H](C(N5[C@@H](C[C@H](C5)O)C(N[C@@H](C)C6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)C(C)(C)C)=O)=O)=O)=C2C)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Desantis J, et al. Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity. Eur J Med Chem. 2024 Mar 15;268:116202. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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PROTAC SARS-CoV-2 Mpro degrader-1

All PROTACs Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC SARS-CoV-2 Mpro degrader-1 Related Classifications

HY-157804 Related Classifications