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SARS-CoV-2 Mpro Degrader

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標的別:	SARS-CoV (12) E3 Ligase Ligand-Linker Conjugates (1) Ligands for Target Protein for PROTAC (3) PROTAC Linkers (1) PROTACs (10) Virus Protease (9)
研究分野別:	Infection (16)
クリックケミストリー:	Azide (2)

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クリックケミストリー

Targets Recommended: SARS-CoV

製品番号	製品名	Target	研究分野	構造式

HY-157805

*PROTAC SARS-CoV-2* Mpro degrader-2**	PROTACs SARS-CoV	Infection
PROTAC SARS-CoV-2 Mpro degrader-2 (Compound 6) is a potent PROTAC degrader of SARS-CoV-2 M ^pro. PROTAC SARS-CoV-2 Mpro degrader-2 has broad-spectrum antiviral activity against CoVs, including SARS-CoV-2 (EC₅₀ = 10.8 μM), HCoV-OC43 (EC₅₀ = 1.6 μM) and HCoV-229E (EC₅₀ = 6.5 μM). PROTAC SARS-CoV-2 Mpro degrader-2 exhibits potent activity against SARS-CoV-2 in Calu-3 cells, with an EC₅₀ of 0.89 μM .

HY-174233

*PROTAC SARS-CoV-2* Mpro degrader-4**	PROTACs SARS-CoV Virus Protease	Infection
PROTAC SARS-CoV-2 Mpro degrader-4 (Compound LLP019) is a SARS-CoV-2 M ^Pro PROTAC degrader with a DC₅₀ value of 4.7 μM. PROTAC SARS-CoV-2 Mpro degrader-4 induces M ^Pro ubiquitination and proteasomal degradation to inhibit SARS-CoV-2 replication. PROTAC SARS-CoV-2 Mpro degrader-4 is promising for research of COVID-19 and related coronavirus infections. (Pink: DH03 (HY-32717); Black: linker (HY-42149); Blue: Thalidomide-4-O-CH2-COO(t-Bu) (HY-42771) .

HY-157804

*PROTAC SARS-CoV-2* Mpro degrader-1**	PROTACs SARS-CoV	Infection
PROTAC SARS-CoV-2 Mpro degrader-1 (compound 5) is a PROTAC degrader targeting the major SARS-CoV-2 protease with broad-spectrum antiviral activity .

HY-181192

*PROTAC SARS-CoV-2* Mpro degrader-6**	PROTACs SARS-CoV Virus Protease	Infection
PROTAC SARS-CoV-2 Mpro degrader-6 is a PROTACs degrader targeting the *SARS-CoV-2* main protease (M ^pro). PROTAC SARS-CoV-2 Mpro degrader-6 effectively induces the degradation of M ^pro and increases K48-linked polyubiquitination of M ^pro in HEK293 cells. PROTAC SARS-CoV-2 Mpro degrader-6 can be used in studies related to coronavirus disease 2019 (COVID-19) .

HY-161789

*PROTAC SARS-CoV-2* Mpro degrader-3**	PROTACs SARS-CoV Virus Protease	Infection
PROTAC SARS-CoV-2 Mpro degrader-3 (Compound P2) exhibits antiviral activity through the degradation of the main protease (Mpro) of human coronaviruses (HCoVs) (DC₅₀=27 μM). PROTAC SARS-CoV-2 Mpro degrader-3 inhibits the viral replication, with EC₅₀ of 4.6 μM, 4.6 μM, and 0.71 μM, for human coronaviruses HCoV-229E, HCoV-OC43 and SARS-CoV-2, respectively. (Pink: ligand for target protein Mpro ligand 2 (HY-161791); Black: linker (HY-161792); Blue: ligand for E3 ligase (S,R,S)-AHPC (HY-125845)) .

HY-181193

*PROTAC SARS-CoV-2* Mpro degrader-7**	PROTACs SARS-CoV Virus Protease	Infection
PROTAC SARS-CoV-2 Mpro degrader-7 is a SARS-CoV-2 main protease (Mpro) PROTAC degrader with a DC₅₀ of 0.985 μM. PROTAC SARS-CoV-2 Mpro degrader-7 promotes K48-linked polyubiquitination of SARS-CoV-2 Mpro, leading to proteasome-dependent degradation via the ubiquitin-proteasome system.PROTAC SARS-CoV-2 Mpro degrader-7 forms a ternary complex with SARS-CoV-2 Mpro and CRBN E3 ubiquitin ligase to enable viral protease ubiquitination.PROTAC SARS-CoV-2 Mpro degrader-7 exhibits a high selectivity index, and induces dose-dependent degradation of SARS-CoV-2 Mpro in stable cells expressing the viral protease.PROTAC SARS-CoV-2 Mpro degrader-7 can be used for the research of COVID-19 .

HY-181154

*PROTAC SARS-CoV-2* Mpro degrader-5**	PROTACs SARS-CoV Virus Protease	Infection
PROTAC SARS-CoV-2 Mpro degrader-5 is a SARS-CoV-2 main protease (Mpro) PROTAC. PROTAC SARS-CoV-2 Mpro degrader-5 engages CRBN E3 ubiquitin ligase to form a ternary complex with SARS-CoV-2 Mpro, induces K48-linked polyubiquitination of SARS-CoV-2 Mpro, and drives proteasome-dependent turnover of SARS-CoV-2 Mpro with a high selectivity index (CC₅₀/DC₅₀ > 10) in human embryonic kidney cells.PROTAC SARS-CoV-2 Mpro degrader-5 can be used for the research of COVID-19 .

HY-181870

*PROTAC SARS-CoV-2* Mpro degrader-8**	PROTACs SARS-CoV	Infection
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 .

HY-162464

MPD2	PROTACs SARS-CoV	Infection
MPD2 is a Cereblon-binding ligand-based PROTAC that degrades *MPro, the main protease of SARS-CoV-2. MPD2 effectively reduced MPro* protein levels in 293T cells in a time-dependent manner (DC₅₀=296 nM). MPD2 exhibited potent antiviral activity against multiple SARS-CoV-2 strains and had enhanced potency against Nirmatrelvir (HY-138687) resistant strains. MPD2 provides a new direction for antiviral drug development against SARS-CoV-2 and other emerging coronavirus pathogens (Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker (HY-W275882)；Red: SARS-CoV-2 MPro Inhibitor MP18 (HY-158763)) .

HY-176440

BP-198	Virus Protease SARS-CoV PROTACs	Infection
BP-198 is an *Mpro* PROTAC degrader. BP-198 promotes the ubiquitination and degradation of Mpro. BP-198 has antiviral effects against SARS-CoV-2 (IC50: 11.8 μM) and has stronger activity against drug-resistant viruses. (Pink: target protein ligand (HY-176442); blue: E3 ligase ligand (HY-176441); black: linker (HY-W457968); E3 ligase-linker conjugate (HY-176443)) .

HY-161790

Mpro ligand 1	Ligands for Target Protein for PROTAC SARS-CoV Virus Protease	Infection
Mpro ligand 1 is the ligand for target protein for PROTAC SARS-CoV-2 Mpro degrader-3 (HY-161789). Mpro ligand 1 is the active form of Mpro ligand 2 (HY-161791) .

HY-161791

Mpro ligand 2	Ligands for Target Protein for PROTAC SARS-CoV Virus Protease	Infection
Mpro ligand 2 (Compound 8) is the ligand for target protein, which can be used for synthesis of PROTAC SARS-CoV-2 Mpro degrader-3 (HY-161789) .

HY-161792

N3-C5-O-C-Boc	PROTAC Linkers	Infection
N3-C5-O-C-Boc is a linker, which can be utilized for the synthesis of PROTAC SARS-CoV-2 Mpro degrader-3 (HY-161789) .

HY-161793

(S,R,S)-AHPC-NHCO-C-O-C5-N3	E3 Ligase Ligand-Linker Conjugates	Infection
(S,R,S)-AHPC-NHCO-C-O-C5-N3 is a conjugate of ligand for E3 ligase (HY-125845) and linker (HY-161792). (S,R,S)-AHPC-NHCO-C-O-C5-N3 can be utilized for synthesis of PROTAC SARS-CoV-2 Mpro degrader-3 (HY-161789) .

HY-181904

SARS-CoV-2 Mpro ligand 2	Ligands for Target Protein for PROTAC Virus Protease	Infection
SARS-CoV-2 Mpro ligand 2 (Compound 24) is a ligand for the target protein for PROTAC (SARS-CoV-2 *Mpro). SARS-CoV-2* Mpro ligand 2 can be used to synthesize PROTAC SARS-CoV-2 Mpro degrader-8 (HY-181870) .

HY-181905

(S,R,S)-AHPC-Me-C2-piperazine		Infection
(S,R,S)-AHPC-Me-C2-piperazine is an E3 ligase ligand-linker conjugate containing an E3 ligase ligand (HY-112078) and a PROTAC linker. (S,R,S)-AHPC-Me-C2-piperazine can be used in the PROTAC SARS-CoV-2 Mpro degrader-8 (HY-181870) .

製品番号	製品名		Classification

HY-161792

N3-C5-O-C-Boc		Azide
N3-C5-O-C-Boc is a linker, which can be utilized for the synthesis of PROTAC SARS-CoV-2 Mpro degrader-3 (HY-161789) .

HY-161793

(S,R,S)-AHPC-NHCO-C-O-C5-N3		Azide
(S,R,S)-AHPC-NHCO-C-O-C5-N3 is a conjugate of ligand for E3 ligase (HY-125845) and linker (HY-161792). (S,R,S)-AHPC-NHCO-C-O-C5-N3 can be utilized for synthesis of PROTAC SARS-CoV-2 Mpro degrader-3 (HY-161789) .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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