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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-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-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-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-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-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-23CLpro-IN-31 (Compound 13c) is a potent SARS-CoV-23CL protease (3CLpro) inhibitor of with an IC50 value of 37.33 nM. SARS-CoV-23CLpro-IN-31 blocks viral polyprotein cleavage and inhibits SARS-CoV-2 replication. SARS-CoV-23CLpro-IN-31 is promising for research of SARS-CoV-2 infection .
SARS-CoV-23CLpro-IN-16 (Compound 3a) is a covalent SARS-CoV-23CLpro inhibitor (IC50: 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-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-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-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-32 (compound B16) is a potent SARS-CoV-23CLpro inhibitor with an IC50 of 0.109 μM. SARS-CoV-23CLpro-IN-32 also exhibits anti-coronavirus HCoV-OC43 activity with an EC50 of 1.99 μM .
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-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-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-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 .
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 .
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].
D1N8 is a potent SARS-CoV-23CL pro inhibitor with an IC50 and CC50 values of 0.44 μM and >20 μM, respectively. D1N8 has the potential for the research of anti-SARS-CoV-2 agents targeting 3CL pro .
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 .
Antcin B is a SARS-CoV-23-chymotrypsin-like protease (3CL Pro) inhibitor. Antcin B binds to multiple key amino acid residues of 3CL Pro(such as Leu141, Asn142, Glu166, His163, etc.) through hydrogen bonds, salt bridges, and hydrophobic interactions, thereby inhibiting the activity of 3CL Pro, blocking the cleavage process of viral polyproteins, and suppressing the replication of the SARS-CoV-2 virus in host cells. Antcin B is promising for research of COVID-19 .
SARS-CoV-2-IN-71 (compound 8h) is a potent inhibitor of SARS-CoV-2. SARS-CoV-2-IN-71 inhibits coronavirus replication at multiple stages. SARS-CoV-2-IN-71 displays anti-coronaviral effect by simultaneously acting on 3CL pro and TMPRSS2 .
Iscartrelvir (WU-04) is a non-covalent inhibitor of SARS-CoV-2, targeting the 3CLpro protein. Iscartrelvir has high inhibitory effect on the 3CLpro protein of 6 SARS-CoV-2 variants (Alpha, Beta, Gamma, Delta, Lambda and Omicron) and 2 coronaviruses (SARS-CoV and MERS-CoV) .
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 .
(±)-Tuaimenal A ((+)-1) is a secondary metabolite and a derivative of Sesamol (HY-N1417). (±)-Tuaimenal A has potent inhibitory activity against SARS-CoV-23CLpro with an IC50 of 33.3 μM. (±)-Tuaimenal A can be used for SARS-CoV-2 infection research .
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.
Hydroxyethylamine (Compd VII) is a SARS-CoV-23CLpro inhibitor with an IC50 of ~10 μM in the spread assay. Hydroxyethylamine has potent antiviral activities .
INSCoV-614(1B) is a potent inhibitor of M pro(3CL pro). 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) .
INSCoV-600K(1) is a potent inhibitor of M pro(3CL pro). 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(3CL pro). 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 .
Walrycin B, an analogue of toxoflavin, is a potent SARS-CoV-23CL pro inhibitor with an IC50 of 0.26 μM. Walrycin B is a WalR response regulator inhibitor. Walrycin B has potent activity of inhibiting bacteria growth [2].
Asunaprevir (BMS-650032) is a potent and orally bioavailable hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM . Asunaprevir inhibits SARS-CoV-23CL pro activity .
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 .
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 .
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 .
Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-23CL pro protease [3].
VK13 (Compound 6) is a potent inhibitor of human cathepsin L (hCatL) with a Ki value of 0.55 nM and SARS-CoV-23CL pro(3CL-PR) with a Ki value of 2.6 nM. VK13 exhibits anti-CoV-2 activity with an EC50 of 1.25 μM .
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 .
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].
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 [2][3] . Boceprevir inhibits SARS-CoV-23CL pro activity .
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 .
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 .
Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM [2]. Tipranavir inhibits SARS-CoV-23CL pro activity [3].
SARS-CoV-IN-5 (compound 49) is a highly selective, nonpeptidic and noncovalent 3CL pro inhibitor with IC50s of 38 nM, 21.1 nM and 86 nM for 3CL pro of SARS-CoV-1, SARS-CoV-2, Bat coronavirus WIV1, respectively. SARS-CoV-IN-5 inhibits the replication of the SARS-CoV-2 delta variant with an EC50 of 0.272 μM. SARS-CoV-IN-5 significantly reduces the lung viral copies in a K18-hACE2 transgenic mouse model. SARS-CoV-IN-5 has good target-specific and potential broad-spectrum anticoronavirus activities against SARS-CoV-1, WIV1, MERS, HCoV-OC43, HCoV-229E, and HKU9 .
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 .
Nirmatrelvir-d6 (PF-07321332-d6) is deuterium labeled Nirmatrelvir. 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 .
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 3CL pro 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].
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].
Asunaprevir (Standard) is the analytical standard of Asunaprevir. This product is intended for research and analytical applications. Asunaprevir (BMS-650032) is a potent and orally bioavailable hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM . Asunaprevir inhibits SARS-CoV-23CLpro activity .
Z-L(D-Val)G-CHN2 is the isoform of Z-LVG-CHN2 (HY-108137). Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-23CL pro protease [3].
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-23CL pro activity .
Boceprevir (Standard) is the analytical standard of Boceprevir. This product is intended for research and analytical applications. 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 [2][3] . Boceprevir inhibits SARS-CoV-23CL pro activity .
Walrycin B (Standard) is the analytical standard of Walrycin B. This product is intended for research and analytical applications. Walrycin B, an analogue of toxoflavin, is a potent SARS-CoV-23CLpro inhibitor with an IC50 of 0.26 μM. Walrycin B is a WalR response regulator inhibitor. Walrycin B has potent activity of inhibiting bacteria growth[1][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].
PF-00835231 is a CoV-2cysteine 3C-like protease (3CL pro) inhibitor, with IC50s of 0.27 nM and 4 nM for SARS CoV-2 and SARS CoV-1 3CL pro, respectively. PF-00835231 is developed for the research of anti-SARS-CoV-2/COVID-19. PF-00835231 can inhibit cell infections and also suppress infections in animal models [2][3].
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 [2][3] . Boceprevir inhibits SARS-CoV-23CLpro activity .
Tipranavir-d7 is deuterated labeled Tipranavir (HY-15148). Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM [2]. Tipranavir inhibits SARS-CoV-23CL pro activity [3].
Tipranavir (Standard) is the analytical standard of Tipranavir. This product is intended for research and analytical applications. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM [2]. Tipranavir inhibits SARS-CoV-23CL pro activity [3].
Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively [2]. Grazoprevir inhibits SARS-CoV-23CL pro activity [3].
Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively [2]. Grazoprevir sodium salt inhibits SARS-CoV-23CL pro activity [3].
Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively [2]. Grazoprevir hydrate inhibits SARS-CoV-23CL pro activity [3].
Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively [2]. Grazoprevir potassium salt inhibits SARS-CoV-23CL pro activity [3].
Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 main protease (M pro and 3CL pro) inhibitor with improved metabolic stability. Ibuzatrelvir has demonstrated pan-human coronavirus antiviral activity and off-target selectivity profile in vitro and in preclinical animal studies. Ibuzatrelvir is well tolerated with a safety profile similar to placebo and prevents viral infection and transmission. Ibuzatrelvir can be used to inhibit COVID-19 [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-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 [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 .
Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors [2]. Naldemedine can be used in opioid-induced constipation (OIC) research [2]. Naldemedine tosylate is predicted to bind to 3CL pro encoded by SARS-CoV2 genome [3].
Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors [2]. Naldemedine can be used in opioid-induced constipation (OIC) research [2]. Naldemedine is predicted to bind to 3CL pro encoded by SARS-CoV2 genome [3].
Grazoprevir (Standard) is the analytical standard of Grazoprevir. This product is intended for research and analytical applications. Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively [2]. Grazoprevir inhibits SARS-CoV-23CLpro activity [3].
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-23CL Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [2][3].
Imidazole- 15N2 (Glyoxaline- 15N2) is 15N labeled Imidazole. 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-23CL Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [2][3] .
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].
NIP-22c is a novel coronavirus 3CLpro inhibitor. The EC50 for Verona, Calu3, Caco2 and HBTEC-ALI were 4.6, 1.1, 0.1 and 0.6 μM, respectively. NIP-22c has antiviral activity .
CMX990 is a SARS-CoV-23CL protease inhibitor. The EC90s for inhibiting SARS-CoV-2 were 9.6 nM and 101 nM in human bronchial epithelial cells (HBECs) and HeLa-ACE2 cells, respectively. CMX990 has good ADME and pharmacokinetic properties .
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 (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-23CL Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [2][3].
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 is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CL pro 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].
Antcin B is a SARS-CoV-23-chymotrypsin-like protease (3CL Pro) inhibitor. Antcin B binds to multiple key amino acid residues of 3CL Pro(such as Leu141, Asn142, Glu166, His163, etc.) through hydrogen bonds, salt bridges, and hydrophobic interactions, thereby inhibiting the activity of 3CL Pro, blocking the cleavage process of viral polyproteins, and suppressing the replication of the SARS-CoV-2 virus in host cells. Antcin B is promising for research of COVID-19 .
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].
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.
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. ,
Nirmatrelvir-d6 (PF-07321332-d6) is deuterium labeled Nirmatrelvir. 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 .
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 [2][3] . Boceprevir inhibits SARS-CoV-23CLpro activity .
Tipranavir-d7 is deuterated labeled Tipranavir (HY-15148). Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM [2]. Tipranavir inhibits SARS-CoV-23CL pro activity [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 [2][3]. Telaprevir inhibits SARS-CoV-23CLpro activity .
Imidazole- 15N2 (Glyoxaline- 15N2) is 15N labeled Imidazole. 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-23CL Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [2][3] .
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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