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SARS-CoV-23CLpro-IN-2 (Compound 1) is a potent inhibitor of 3CL protease. SARS-CoV-23CLpro-IN-2 has the potential for the research of SARS-CoV-2 diseases .
SARS-CoV-23CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-23CL protease. SARS-CoV-23CLpro probe-1 can detect endogenously expressed 3CLpro in SARS-CoV-2-infected cells .
SARS-CoV-23CLpro-IN-15 (compound a) is a beta-nitrostyrene coronavirus SARS-CoV-2 inhibitor that targets the SARS-CoV-23CL protease (3CLpro). SARS-CoV-23CLpro-IN-15 inhibits viral replication and transcription and plays a key role in the discovery of anti-COVID-19 lead compounds .
SARS-CoV-23CLpro-IN-1 (Compound 14c) is a potent inhibitor of SARS-CoV-23CL pro. 3CL pro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral agents. SARS-CoV-23CLpro-IN-1 has the potential for the research of infection diseases .
SARS-CoV-23CLpro-IN-16 (Compound 3a) is a covalent SARS-CoV-23CLpro inhibitor (IC50s: 2.124 μM). SARS-CoV-23CLpro-IN-16 binds to the active site and forms a covalent bond with Cys145 of 3CLpro .
SARS-CoV-23CLpro-IN-6 is a reversible covalent inhibitor of SARS-CoV-23CL protease. SARS-CoV-23CLpro-IN-6 has potent inhibitory activity for SARS-CoV-23CL pro with an IC50 value of 4.9 μM. SARS-CoV-23CLpro-IN-6 can be used for the research of coronavirus disease 2019 (COVID-19) .
SARS-CoV-23CLpro-IN-14 (compound 11j) is an orally active SARS-CoV-23CLpro inhibitor. SARS-CoV-23CLpro-IN-14 shows significant anti-SARS-CoV-2 activity (EC50 = 0.18 μM) and low cytotoxicity (CC50 > 50 μM) in Vero E6 cells .
SARS-CoV-23CLpro-IN-13 is a potent SARS-CoV-23CL protease inhibitor with an IC50 value of 21 nM. SARS-CoV-23CLpro-IN-13 shows anti-coronavirus activity .
SARS-CoV-23CLpro-IN-22 (Compound 17) is a cathepsin L (CTSL ) inhibitor with an IC50 value of 32.5 nM. SARS-CoV-23CLpro-IN-22 can be used for the study of SARS-CoV-2 virus .
SARS-CoV-23CLpro-IN-25 (compound 56) inhibits the SARS-CoV-23CLpro with the IC50 of 70 nM and displays antiviral activity in cells with the EC50 of 3.1 μM .
SARS-CoV-23CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CL pro). SARS-CoV-23CLpro-IN-5 has inhibitory activity for 3CL pro with an IC50 value of 3.8 nM. SARS-CoV-23CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-23CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19) .
SARS-CoV-23CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-23CLpro with an IC50 of 0.43 μM. SARS-CoV-23CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .
SARS-CoV-23CLpro-IN-23 (Compound Cd3) is a compound that can be isolated from Citrus depressa. SARS-CoV-23CLpro-IN-23 has good inhibitory activity to the SARS-CoV-2 spike protein, with KD of 0.79 μM. SARS-CoV-23CLpro-IN-23 can bind to key amino acid residue, disrupting the formation of the spike protein and h-ACE2 complex .
SARS-CoV-23CLpro-IN-27 (Compound 9H) is an inhibitor of SARS-CoV-23CL pro with an IC50 value of 21 nM. SARS-CoV-23CLpro-IN-27 exhibits excellent anti-SARS-CoV-2 replicon activity, demonstrating an EC50 value of 5 nM .
SARS-CoV-23CLpro-IN-19 (Compound C5a) is a non-covalent, non-peptide SARS-CoV-23CLpro inhibitor (IC50s: 0.7 μM). SARS-CoV-23CLpro-IN-19 has broad-spectrum activity against Omicron subvariants (BA.5, BQ.1.1, and XBB.1.5) infection in human cells, with EC50 values between 30-69 nM .
3CLPro-IN-3 (Compound A36) is an inhibitor for SARS-CoV-23CLpro with IC50 of 51.3 nM. 3CLPro-IN-3 exhibits antiviral activity against human coronavirus 229E, OC43 and mouse hepatitis virus MHV .
SARS-CoV-23CLpro-IN-21 (Compound D6) irreversibly and covalently inhibits SARS-CoV-23CL pro with an IC50 of 0.03 μM. SARS-CoV-23CLpro-IN-21 also inhibits SARS-CoV-13CL pro with an IC50 of 0.12μM .
SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-23CL protease(3CLpro) with an IC50 and EC50 of 0.17 and 1.45 nM, respectively. SARS-CoV-23C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals .
SARS-CoV-2-IN-10 is a potent and nontoxic inhibitor of SARS-CoV-23CL protease(3CLpro) with an IC50 and EC50 of 0.13 and 1.03 nM, respectively. SARS-CoV-23C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals .
Hydroxyethylamine (Compd VII) is a SARS-CoV-23CLpro inhibitor with an IC50 of ~10 μM in the spread assay. Hydroxyethylamine has potent antiviral activities .
3CPLro-IN-1 (compound A17) is a potent and orally active inhibitor of SARS-CoV-23CLpro with an IC50 of 5.65 μM. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive agent target for fighting COVID-19 .
MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2 is a fluorescent substrate used for fluorescence resonance energy transfer (FRET) protease assays. This substrate is employed to measure the activity of SARS-CoV-23CLpro .
3CPLro-IN-2 (compound C1) is a potent and orally active inhibitor of SARS-CoV-23CLpro with an IC50 and Ki of 1.55 and 6.09 μM, respectively. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive agent target for fighting COVID-19 .
MERS-CoV-IN-2 (compound 3c) is a MERS-CoV 3CLpro inhibitor (IC50=17nM). MERS-CoV-IN-2 inhibits the activity of the 3CLpro enzyme by binding to the active site of the enzyme, specifically the S4 subsite, thereby exhibiting antiviral activity against SARS-CoV-2 and MERS-CoV .
PROTAC KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPro). Protac KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPRO). The PROTAC molecule is designed by partially coupling a GC-376-based dipeptidyl 3CLPro ligand with pomadomide via a piperazine-piperidine linker .
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-23CLpro 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.
SARS-CoV-2-IN-107 (Compound A7) is the inhibitor for SARS-CoV-23CLpro with an IC50 of 261.3 nM. SARS-CoV-2-IN-107 inhibits the SARS-CoV-2 replication with an EC50 of 11.7 μM. SARS-CoV-2-IN-107 exhibits anti-inflammatory activity with a NO inhibition rate of 68.6% in LPS (HY-D1056)-stimulated RAW264.7 macrophages .
Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-23CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis[2][3].
SARS-CoV MPro-IN-1 is a SARS-CoV-23CLpro covalent inhibitor, with an IC50 of 40 nM. SARS-CoV MPro-IN-1 shows good anti-SARS-CoV-2-infection activity in cell culture with an EC50 of 0.33 μM. SARS-CoV MPro-IN-1 has the potential for COVID-19 research .
MAC-5576 is a SARS-CoV-23CL protease inhibitor, with an IC50 of 81 nM. MAC-5576 also inhibits 3CLpro (IC50=0.5 μM), HAV 3Cpro (IC50=0.5 μM), and thrombin (IC50=13 μM) [2].
Merbromin is a mixed inhibitor of the 3-chymotrypsin-like protease (3CLpro) of SARS-CoV-2, with an IC50 of 2.7 μM. Merbromin effectively inhibits the replication of the Zika virus (ZIKV) and shows anti-ZIKV activity by inhibiting ZIKVpro. Merbromin can also be used as a topical disinfectant for cuts and scrapes, and it serves as a biological dye [2].
Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-23CLpro activity[6].
Punicalagin (Standard) is the analytical standard of Punicalagin. This product is intended for research and analytical applications. Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 [2][3].
Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-23CLpro activity[4].
Telaprevir (Standard) is the analytical standard of Telaprevir. This product is intended for research and analytical applications. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide [2][3]. Telaprevir inhibits SARS-CoV-23CLpro activity .
Telaprevir (Standard) is the analytical standard of Telaprevir. This product is intended for research and analytical applications. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide [2][3]. Telaprevir inhibits SARS-CoV-23CLpro activity .
Imidazole (Standard) is the analytical standard of Imidazole. This product is intended for research and analytical applications. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-23CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [2][3].
Antiviral agent 25 (compound 6g) is a new non-peptide analog covalent inhibitor of SARS-CoV-23CL pro. Antiviral agent 25 has a strong inhibitory effect on SARS-CoV-23CL pro and SARS-CoV-2 PL pro with IC50 values of 0.118 µM, 0.448 µM, respectively. Antiviral agent 25 has antiviral effect on SARS-CoV-2 with an EC50 value of 7.249 µM .
DB12055 (MK-0767 analog) is a covalent SARS-CoV-23CL protease inhibitor. DB12055 has the potential for the study of dyslipidemia and diabetes mellitus .
Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CL PRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research .
Nirmatrelvir (Standard) is the analytical standard of Nirmatrelvir. This product is intended for research and analytical applications. Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CL PRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research .
INSCoV-600K(1) is a potent inhibitor of M pro(3CLpro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-600K(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1) .
INSCoV-601I(1) is a potent inhibitor of M pro(3CLpro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-601I(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1) .
CCF0058981 (CCF981), 3-chlorophenyl analogue, is a noncovalent SARS-CoV-23CL pro(SC2) inhibitor with an IC50 of 68 nM. CCF0058981 inhibits SC1 (SARS-CoV-1 3CL pro) with an IC50 of 19 nM. CCF0058981 has antiviral efficacy and has the potential for COVID-19 research .
INSCoV-614(1B) is a potent inhibitor of M pro(3CLpro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-614(1B) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1) .
YH-53 is a potent 3CL pro inhibitor with Ki values of 6.3 nM, 34.7 nM for SARS-CoV-1 3CL pro and SARS-CoV-23CL pro, respectively. YH-53 strongly blocks the SARS-CoV-2 replication. YH-53 is a peptidomimetic compound with a unique benzothiazolyl ketone. YH-53 has the potential for COVID-19 research [2].
Merbromin is a mixed inhibitor of the 3-chymotrypsin-like protease (3CLpro) of SARS-CoV-2, with an IC50 of 2.7 μM. Merbromin effectively inhibits the replication of the Zika virus (ZIKV) and shows anti-ZIKV activity by inhibiting ZIKVpro. Merbromin can also be used as a topical disinfectant for cuts and scrapes, and it serves as a biological dye [2].
SARS-CoV-23CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-23CL protease. SARS-CoV-23CLpro probe-1 can detect endogenously expressed 3CLpro in SARS-CoV-2-infected cells .
Imidazole (Standard) is the analytical standard of Imidazole. This product is intended for research and analytical applications. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-23CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [2][3].
MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2 is a fluorescent substrate used for fluorescence resonance energy transfer (FRET) protease assays. This substrate is employed to measure the activity of SARS-CoV-23CLpro .
Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-23CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis[2][3].
Punicalagin (Standard) is the analytical standard of Punicalagin. This product is intended for research and analytical applications. Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 [2][3].
Telaprevir (Standard) is the analytical standard of Telaprevir. This product is intended for research and analytical applications. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide [2][3]. Telaprevir inhibits SARS-CoV-23CLpro activity .
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.
Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-23CLpro activity[6].
Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-23CLpro activity[4].
SARS-CoV-23CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-23CL protease. SARS-CoV-23CLpro probe-1 can detect endogenously expressed 3CLpro in SARS-CoV-2-infected cells .
SARS-CoV-23CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-23CLpro with an IC50 of 0.43 μM. SARS-CoV-23CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .
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