PROTAC SARS-CoV-2 Mpro degrader-8

Cat. No.: HY-181870: Ficha de datos Instrucciones de manejo
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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 (K_d=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).

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PROTAC SARS-CoV-2 Mpro degrader-8 Estructura química

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Descripciòn

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 (K_d=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^[1].
(Pink: SARS-CoV-2 Mpro ligand (HY-181904); Blue: VHL ligand (HY-112078); Black: linker).

IC₅₀ & Target

VHL

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:	SARS-CoV-2-infected 293T-hACE2 cells
Concentration:	0.1-25 μM; 100 μM (VHL inhibitor VH298 co-treatment); 1 μM (proteasome inhibitor MG132 treatment)
Incubation Time:	24 h (post-treatment)
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.

Peso molecular

1053.22

Fòrmula

C₅₃H₅₉F₃N₁₀O₆S₂

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Eleuteri M, et al. Discovery of a tetrahydrobenzothiophen-2-yl-pyrazolo [1, 5-a] pyrimidine-3-carboxamide-based PROTAC as degrader of SARS-CoV-2 Main Protease[J]. European Journal of Medicinal Chemistry, 2026: 118721.