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SARS-CoV-2Mpro-IN-18 (compound 84) is a potent SARS-CoV-2Mpro inhibitor with the IC50 of 3.23 nM. SARS-CoV-2Mpro-IN-18 can be used for study of anti-SARS-CoV-2 agent .
SARS-CoV-2Mpro-IN-19 (compound MPI94) is a SARS-CoV-2MPro inhibitor with the IC50 of 0.096 μM. SARS-CoV-2Mpro-IN-19 can be used for study of COVID-19 .
SARS-CoV-2Mpro-IN-23 (Compound 2) is an inhibitor for SARS-CoV-2 main protease (Mpro), which inhibits wildtype Mpro and mutant Mpro variants, with IC50 of 0.057-0.92 μM. SARS-CoV-2Mpro-IN-23 inhibits the post-entry viral processes of wild-type SARS-CoV-2 single-round infectious particles (SRIPs), suppresses the viral replication of Mpro wildtype and Mpro mutants with EC50 of 0.02-0.52 μM .
SARS-CoV-2Mpro-IN-13 (compound 20j) is a covalent SARS-CoV-2 Protease Mpro inhibitor with an IC50 value of 19.0 nM. SARS-CoV-2Mpro-IN-13 processes antiviral activity with an EC50 value of 138.1 nM .
SARS-CoV-2Mpro-IN-14 (Compound 19) is an inhibitor of SARS-CoV-2Mpro with an IC50 of 0.044 μM. SARS-CoV-2Mpro-IN-14 exhibits water solubility, has no cytotoxicity, and can be used in the study of COVID-19 .
SARS-CoV-2Mpro-IN-20 (compound MPI100) is a SARS-CoV-2 main protease inhibitor. SARS-CoV-2Mpro-IN-20 shows antiviral activity with the EC50 of 3.4 μM .
SARS-CoV-2Mpro-IN-17 (compound S5-28) is an orally active and noncovalent SARS-CoV-2Mpro inhibitor with the EC50 of 1.35 μM. SARS-CoV-2Mpro-IN-17 can be used for study of COVID-19 .
SARS-CoV-2Mpro-IN-4 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 900 nM and 60 nM respectively. SARS-CoV-2Mpro-IN-4 has antiviral activity against SARS-CoV2. SARS-CoV-2Mpro-IN-4 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 8.2 nM .
SARS-CoV-2Mpro-IN-5 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 1800 nM and 145 nM respectively. SARS-CoV-2Mpro-IN-5 has antiviral activity against SARS-CoV2. SARS-CoV-2Mpro-IN-5 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 14.7 nM .
SARS-CoV-2Mpro-IN-25 (Compound 3a) is a SARS-CoV-2protease inhibitor with an IC50 value of 0.26 μM. SARS-CoV-2Mpro-IN-25 exhibits antiviral activity and can be used in pneumonia-related research .
SARS-CoV-2Mpro-IN-22 (compound 4), a hydrolysable tannin, is a potent SARS-CoV-2 main protease (Mpro) inhibitor with an IC50 value of 1.2 µg/mL. SARS-CoV-2Mpro-IN-22 does not show any significant cytotoxic activity against A549 and HUVEC cell lines .
SARS-CoV-2Mpro-IN-21 (compound A8) is a potent SARS-CoV-2 and OVID-19 Main Protease M Pro inhibitor. SARS-CoV-2Mpro-IN-21 shows excellent antioxidant activity in DPPH assay with an IC50 of 0.36 mg/mL. SARS-CoV-2Mpro-IN-21 also exhibits better antibacterial potency against Klebsiella with an IC50 of 1.19 mg/mL .
SARS-CoV-2Mpro-IN-10 (27h) is a potent M pro inhibitor with IC50 value and EC50 values of 10.9 nM and 43.6 nM, respectively. SARS-CoV-2Mpro-IN-10 can be used for the research of SARS-CoV-2 virus .
SARS-CoV-2Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 M pro inhibitor with an IC50 of 0.18 μM. SARS-CoV-2Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3 .
SARS-CoV-2Mpro-IN-2 (compound GC-14) is a selective, low cytotoxic and non-covalent M pro inhibitor (IC50=0.40 μM) with good anti-SARS-CoV-2 activity (EC50=1.1 μM). SARS-CoV-2Mpro-IN-2 can be used in COVID-19 studies .
SARS-CoV-2Mpro-IN-9 (compound c7) is a nonpeptidic, noncovalent SARS-CoV-2 M pro inhibitor (IC50=0.085 μM), with improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. SARS-CoV-2Mpro-IN-9 inhibits viral replication (EC50=1.10 μM) in SARS-CoV-2-infected Vero E6 cells, while exhibits low cytotoxic effects (CC50>50 μM) .
PROTAC SARS-CoV-2Mpro degrader-2 (Compound 6) is a potent PROTAC degrader of SARS-CoV-2 M pro. PROTAC SARS-CoV-2Mpro 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-2Mpro degrader-2 exhibits potent activity against SARS-CoV-2 in Calu-3 cells, with an EC50 of 0.89 μM .
PROTAC SARS-CoV-2Mpro 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-2Mpro 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)) .
SARS-CoV-2-IN-59 (compound E07), an imidazoline derivative, is a non-peptide small molecule inhibitor of SARS-CoV-2 that targets the main protease (Mpro) of the coronavirus. SARS-CoV-2-IN-59 has a strong interaction with residues on Mpro (Met 165, Gln 166, Met 165, His 41, Gln 189) .
SARS-CoV-2-IN-1 is a potent Mpro inhibitor. SARS-CoV-2-IN-1 inhibits the purified recombinant SARS-CoV-2Mpro, SARS-CoVMpro and MERS-CoV Mpro with IC50s of 0.67, 0.90 and 0.58 μM, respectively .
SARS-CoV-2-IN-68 (compound 6C) is a covalent SARS-CoV-2PLpro/Mpro inhibitor with potent antiviral activities. SARS-CoV-2-IN-68 binds to Zn-finger domain of PLpro .
SARS-CoV-2-IN-36 is a potent SARS-CoV-2Mpro(SARS-CoV) inhibitor with an IC50 of 2.37 μM and a Kd of 1.19 μM in enzymatic assays. SARS-CoV-2-IN-36 shows antiviral activity against UC-1074, RG2674, and NVDBB-2220 SARS-CoV-2 variants in Vero cells .
Mpro ligand 1 is the ligand for target protein for PROTAC SARS-CoV-2Mpro degrader-3 (HY-161789). Mpro ligand 1 is the active form of Mpro ligand 2 (HY-161791) .
Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2Mpro with an EC50 of 16.77 μM for SARS-CoV-2. Mpro inhibitor N3 hemihydrate specifically inhibits Mpro from multiple coronaviruses, including SARS-CoV and MERS-CoV. Mpro inhibitor N3 hemihydrate displays inhibition against HCoV-229E, FIPV, and MHV-A59 with individual IC50 of 4.0 μM, 8.8 μM, and 2.7 μM, respectively .
D-4-77 is a potent inhibitor of SARS-CoV-2Mpro with an IC50 value of 0.95 μM. D-4-77 has antiviral active with an EC50 value of 0.49 μM. D-4-77 suppresses SARS-CoV-2Mpro -induced antagonism of the host NF-κB innate immune response .
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-2MPro Inhibitor MP18 (HY-158763)) .
SARS-CoVMPro-IN-1 is a SARS-CoV-2 3CLpro covalent inhibitor, with an IC50 of 40 nM. SARS-CoVMPro-IN-1 shows good anti-SARS-CoV-2-infection activity in cell culture with an EC50 of 0.33 μM. SARS-CoVMPro-IN-1 has the potential for COVID-19 research .
GRL-190-21 (compound 5e) is an inhibitor for SARS-Cov-2-Mpro with a Ki of 0.04 nM and exhibits antiviral activity in VeroE6 cells with EC50 of 0.26 μM. GRL-190-21 reduces the infectivity, replication, and cytopathic effect of SARS-CoV-2 without significant toxicity .
Jobosic acid, a saturated fatty acid, is a selective SARS-CoV-2 inhibitor. Jobosic acid inhibits Mpro and spike-RBD/ACE-2 interaction with IC50 values of 7.5 μg/mL and 3 μg/mL, respectively. Jobosic acid shows viral entry inhibition for the omicron SARS-CoV-2 variant .
MPI8 (TG0205221) is an inhibitor of the major protease of SARS-CoV-2(MPro) with high antiviral activity. MPI8 exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2MPro and host cell cysteine protease L (cathepsin L). This dual inhibition enhanced the overall antiviral potency and effect of MPI8. MPI8 can be used in clinical studies of COVID-19 .
SARS-CoVMPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 M pro with an IC50 value of 72.07 nM. The main protease (M pro) of the virus as the major enzyme processing viral polyproteins contributes to the replication and transcription of SARS-CoV-2 in host cells, and has been characterized as an attractive target in agent discovery. SARS-CoVMPro-IN-2 has the potential for the research of COVID-19 .
Mpro inhibitor N3 is a potent SARS-CoV-2MPro inhibitor with an EC50 value of 16.77 µM. Mpro inhibitor N3 shows antiviral activities against HCoV-229E, FIPV, IBV and MHV-A59 .
Polycarpine hydrochloride (1a) is a broad-spectrum Mpro inhibitor (IC50 = 30 nM) that can be isolated from the Polycarpa aurata and also serves as an anti-coronaviral agent. Polycarpine hydrochloride possesses antiviral and antifungal activities, with IC50 values of 30.0 nM and 0.12 μM against SARS-CoV-2Mpro and PEDV Mpro, respectively .
(±)-Alliin (Standard) is the analytical standard of (±)-Alliin. This product is intended for research and analytical applications. (±)-Alliin is the main active component of garlic. (±)-Alliin is a putative inhibitor of the main protease of SARS-CoV-2 (Mpro) .
Lufotrelvir (PF-07304814), a phosphate proagent of PF-00835231, acts as a potent 3CLpro protease (Mpro) inhibitor with SARS-CoV-2 antiviral activity. Lufotrelvir binds and inhibits SARS-CoV-2 3CLpro activity with a Ki of 174nM. Lufotrelvir is promising single antiviral agent and also can be used for the research of combination with other antivirals that target other critical stages of the coronavirus life cycle.
CDD-1733 is a non-covalent and non-peptide potent SARS-CoV-2Mpro inhibitor with a Ki of 12 nM. CDD-1733 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants .
CDD-1819 is a non-covalent and non-peptide potent SARS-CoV-2Mpro inhibitor with a Ki of 5 nM. CDD-1819 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants .
CDD-1845 is a non-covalent and non-peptide potent SARS-CoV-2Mpro inhibitor with a Ki of 3 nM. CDD-1845 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants .
Olgotrelvir sodium is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells .
Setomimycin is a potent antibiotic. Setomimycin inhibits the SARS-CoV-2Mpro enzyme with an IC50 value of 12.02 µM. Setomimycin shows anti-inflammatory and antioxidant properties. Setomimycin shows antiproliferative and antitumor activity .
Mpro/PLpro-IN-1 (Compound 29) is a potent inhibitor of M pro/PL pro. Mpro/PLpro-IN-1 is a dual acting SARS-CoV-2 proteases inhibitor featuring micromolar inhibitory potency versus M pro (IC50 = 1.72 μM) and submicromolar potency versus PL pro (IC50 = 0.67 μM) .
Jaceidin triacetate(compound 54) is a natural compound isolated formmarulabark.Jaceidin triacetatecan inhibitSARS-CoV-2 Mpro, with theIC50of 11.9μM.Jaceidin triacetateinhibits the replication of Sars-Cov-2 Viral in Vero-E6 cells .
Simeprevir- 13C,d3 is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][2][5].
Carmofur (HCFU) is a rat recombinant acid ceramidase inhibitor with an IC50 of 29 nM. Carmofur is also a protease inhibitor of SARS-CoV-2 main protease (Mpro), fatty acid amide hydrolase (FAAH) and N-acylethanolamine acid amidase (NAAA). Carmofur has anti-cancer, anti-inflammatory and anti-virus activities, and can be used for the study of COVID-19 and acute lung injury (ALI) .
Proglumetacin is an orally active and potent cyclo-oxygenase inhibitor. Proglumetacin can inhibits SARS-CoVMpro (main protease of the SARS-CoV-2), with an AC50 of 8.9 μM (activity concentration at half maximal activity). Proglumetacin has anti-inflammatory activity, can be used for inflammation (such as Rheumatoid arthritis, and Allergic air pouch inflammation) research[1][2][3].
Carmofur (Standard) is the analytical standard of Carmofur. This product is intended for research and analytical applications. Carmofur (HCFU) is a rat recombinant acid ceramidase inhibitor with an IC50 of 29 nM. Carmofur is also a protease inhibitor of SARS-CoV-2 main protease (Mpro), fatty acid amide hydrolase (FAAH) and N-acylethanolamine acid amidase (NAAA). Carmofur has anti-cancer, anti-inflammatory and anti-virus activities, and can be used for the study of COVID-19 and acute lung injury (ALI) .
(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-2Mpro degrader-3 (HY-161789) .
SARS-CoV-2Mpro-IN-22 (compound 4), a hydrolysable tannin, is a potent SARS-CoV-2 main protease (Mpro) inhibitor with an IC50 value of 1.2 µg/mL. SARS-CoV-2Mpro-IN-22 does not show any significant cytotoxic activity against A549 and HUVEC cell lines .
SARS-CoVMPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 M pro with an IC50 value of 72.07 nM. The main protease (M pro) of the virus as the major enzyme processing viral polyproteins contributes to the replication and transcription of SARS-CoV-2 in host cells, and has been characterized as an attractive target in agent discovery. SARS-CoVMPro-IN-2 has the potential for the research of COVID-19 .
Polycarpine hydrochloride (1a) is a broad-spectrum Mpro inhibitor (IC50 = 30 nM) that can be isolated from the Polycarpa aurata and also serves as an anti-coronaviral agent. Polycarpine hydrochloride possesses antiviral and antifungal activities, with IC50 values of 30.0 nM and 0.12 μM against SARS-CoV-2Mpro and PEDV Mpro, respectively .
(±)-Alliin (Standard) is the analytical standard of (±)-Alliin. This product is intended for research and analytical applications. (±)-Alliin is the main active component of garlic. (±)-Alliin is a putative inhibitor of the main protease of SARS-CoV-2 (Mpro) .
Jaceidin triacetate(compound 54) is a natural compound isolated formmarulabark.Jaceidin triacetatecan inhibitSARS-CoV-2 Mpro, with theIC50of 11.9μM.Jaceidin triacetateinhibits the replication of Sars-Cov-2 Viral in Vero-E6 cells .
SARS-CoV-2 3CLpro/3C-like protease Protein is the recombinant Virus-derived SARS-CoV-2 3CLpro/3C-like protease protein, expressed by E. coli , with tag free. The total length of SARS-CoV-2 3CLpro/3C-like protease Protein is 306 a.a., with molecular weight of ~33.8 kDa.
SARS-CoV-2 3CLpro/3C-like protease Protein (Tag Free) is the recombinant virus-derived SARS-CoV-2 3CLpro/3C-like protease, expressed by E. coli , with tag Free labeled tag. ,
SARS-CoV-2 3CLpro/3C-like protease Protein (His-Avi) is the recombinant Virus-derived SARS-CoV-2 3CLpro/3C-like protease protein, expressed by E. coli , with N-His, N-Avi labeled tag. The total length of SARS-CoV-2 3CLpro/3C-like protease Protein (His-Avi) is 306 a.a., with molecular weight of ~36.5 kDa.
SARS-CoV-2 3CLpro/3C-like protease Protein (sf9, His) is the recombinant Virus-derived SARS-CoV-2 3CLpro/3C-like protease protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of SARS-CoV-2 3CLpro/3C-like protease Protein (sf9, His) is 306 a.a., with molecular weight of ~37 kDa.
SARS-CoV-2 3CLpro/3C-like protease Protein (sf9, His-Avi) is the recombinant Virus-derived SARS-CoV-2 3CLpro/3C-like protease protein, expressed by Sf9 insect cells , with N-His, N-Avi labeled tag. The total length of SARS-CoV-2 3CLpro/3C-like protease Protein (sf9, His-Avi) is 306 a.a., with molecular weight of ~37.1 kDa.
Simeprevir- 13C,d3 is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][2][5].
(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-2Mpro degrader-3 (HY-161789) .
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