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Olgotrelvir sodium is an orally active dual inhibitor of coronavirus mainprotease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells .
Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin hemisulfate potently inhibits serine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits M pro (the mainprotease of SARS-CoV-2) and also has anti-inflammatory activity .
SPR38 is a potent SARS-CoV-2 mainprotease inhibitor, with a Ki of 0.260 μM. SPR38 also inhibits hCatL and hCatB, with Ki values of 1.92 μM and 11.1 μM, respectively .
SARS-CoV-2 Mpro-IN-21 (compound A8) is a potent SARS-CoV-2 and OVID-19 MainProtease M Pro inhibitor. SARS-CoV-2 Mpro-IN-21 shows excellent antioxidant activity in DPPH assay with an IC50 of 0.36 mg/mL. SARS-CoV-2 Mpro-IN-21 also exhibits better antibacterial potency against Klebsiella with an IC50 of 1.19 mg/mL .
(±)-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 mainprotease of SARS-CoV-2 (Mpro) .
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits M pro (the mainprotease of SARS-CoV-2) and also has anti-inflammatory activity .
Ulinastatin (Uristatin) is a trypsin and serine protease inhibitor. Ulinastatin is the main protein binding inhibitor of various trypsin, chymotrypsin, and various pancreatic proteases. Ulinastatin shows neuroprotective, anti-inflammatory, anti-apoptotic, anti-oxidant effects .
Solasurine is a steroidal alkaloid that can be isolated from Solanum surrattence. Solasurine can interact with the C3-like protease (SARS-CoV-2 mainprotease) amino acids Phe8, Pro9, Ile152, Tyr154, Pro293, Phe294, Val297, and Arg298 .
Kazinol F is a polyphenol from Broussonetia papyrifera. Kazinol F also is an effective Mpro inhibitor. Kazinol F has interaction with both the catalytic residues (His41 and Cys145) of Mpro and exhibits good binding affinity. Kazinol F can be used for the research of COVID-19 .
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 mainprotease (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) .
SARS-CoV-2 Mpro-IN-20 (compound MPI100) is a SARS-CoV-2mainprotease inhibitor. SARS-CoV-2 Mpro-IN-20 shows antiviral activity with the EC50 of 3.4 μM .
X77 is a potent non-covalent inhibitor of the mainprotease of SARS-CoV-2 (SARS-CoV-2 M pro) . X77 binds to SARS-CoV-2 M pro with a Kd value of 0.057 μM .
SPR41 is a potent SARS-CoV-2 mainprotease inhibitor with Ki values of 0.184, 0.252, 14.4 µM for SARS-CoV-2 M pro, hCatL, hCatB, respectively. SPR41 shows antiviral and cytotoxicity .
SPR39 is a potent SARS-CoV-2 mainprotease inhibitor with Ki values of 0.252, 3.38, 7.88 µM for SARS-CoV-2 M pro, hCatL, hCatB, respectively. SPR39 shows antiviral and cytotoxicity .
Euptox A (9-Oxo-10, 11-dehydroageraphorone), a cadenine sesquiterpene, is the main toxin that can be isolated from Eupatorium adenophorum. Euptox A induces apoptosis by improving the gene expression level of apoptotic proteases such as caspase-10 in HeLa cells .
Tectoquinone (2-Methylanthraquinone) is a SARSCoV-2mainprotease inhibitor against COVID-19. Tectoquinone exhibits strong mosquito larvicidal activity with the LC50 values of 3.3 and 5.4 μg/ml against A. aegypti and A. albopictus in 24 h, respectively .
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 mainprotease (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) .
SARS-CoV-2-IN-21 (compound 10), a penicillin sulfone benzyl C6 derivative, is a potent SARS-CoV-2 mainprotease inhibitor, with an IC50 of 5.3 μM. SARS-CoV-2-IN-21 can be used for COVID-19 research .
Simeprevir (TMC435; TMC435350) 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 mainprotease (M pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses .
Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir sodium inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir sodium also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir sodium inhibits the mainprotease (M pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses .
(Rac)-X77?is a racemate of X77. X77 is a potent non-covalent inhibitor of the mainprotease of SARS-CoV-2 (SARS-CoV-2 M pro) . X77 binds to SARS-CoV-2 M pro with a Kd value of 0.057 μM .
CDK9-IN-25 (compound 4a) is an imidazopyrazine CDK9 inhibitor (IC50: 0.24 μM). CDK9-IN-25 has good affinity to the mainprotease of COVID-19 and has antiviral activity against human coronavirus 229E (IC50: 63.28 μM) .
Silymarin is an extract of the milk thistle (Silybum marianum). Silymarin is an effective SARS-CoV-2 mainprotease (M pro) inhibitor. Silymarin can significantly reduce tumor cell proliferation, angiogenesis as well as insulin resistance. Silymarin has the chemopreventive effect on hepatocellular carcinoma (HCC). Silymarin has the potential for COVID-19 research .
Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78) .
SARS-CoV-2-IN-69 (Compound 7E) is a non-covalent SARS-CoV-2 inhibitor with an EC50 value of 7.4 μM. SARS-CoV-2-IN-69 is a potent inhibitor of SARS-CoV-2 mainprotease (M pro) and a non-covalent inhibitor of papain (PL pro) .
SARS-CoV-2 Mpro-IN-22 (compound 4), a hydrolysable tannin, is a potent SARS-CoV-2 mainprotease (Mpro) inhibitor with an IC50 value of 1.2 µg/mL. SARS-CoV-2 Mpro-IN-22 does not show any significant cytotoxic activity against A549 and HUVEC cell lines .
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 mainprotease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][2][5].
SARS-CoV-2-IN-59 (compound E07), an imidazoline derivative, is a non-peptide small molecule inhibitor of SARS-CoV-2 that targets the mainprotease (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) .
Proglumetacin is an orally active and potent cyclo-oxygenase inhibitor. Proglumetacin can inhibits SARS-CoV Mpro (mainprotease 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].
SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a potent inhibitor of SARS-CoV-2 3CL pro. 3CL pro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral agents. SARS-CoV-2 3CLpro-IN-1 has the potential for the research of infection diseases .
Bofutrelvir (FB2001) is a SARS-CoV-2 mainproteaseM pro inhibitor with an IC50 value of 53 nM and an EC50 value of 0.53 μM. Bofutrelvir exhibits potent antiviral efficacy against several current SARS-CoV-2 variants with EC50 values of 0.26-0.42 μM. Bofutrelvir has an additive antiviral effect when combined with Remdesivir (HY-104077) .
ML2006a4 is an orally active inhibitor for SARS-CoV-2 mainprotease (M pro) with IC50 in picomolare value. ML2006a4 is cell permeable and antiviral active, that inhibits replication in SARS-CoV-2 in cells Huh7.5.1-ACE2-TMPRSS2 (Huh7.5.1++) in picomolare level
SARS-CoV MPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 M pro with an IC50 value of 72.07 nM. The mainprotease (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-CoV MPro-IN-2 has the potential for the research of COVID-19 .
SARS-CoV-2 Mpro-IN-4 is a dual Inhibitor of MainProtease (M Pro) and Cathepsin L (CatL), with IC50s of 900 nM and 60 nM respectively. SARS-CoV-2 Mpro-IN-4 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-4 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 8.2 nM .
SARS-CoV-2 Mpro-IN-5 is a dual Inhibitor of MainProtease (M Pro) and Cathepsin L (CatL), with IC50s of 1800 nM and 145 nM respectively. SARS-CoV-2 Mpro-IN-5 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-5 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 14.7 nM .
Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 mainprotease (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 .
MAT-POS-e194df51-1 is an orally active, non-covalent and non-peptide SARS-CoV-2mainprotease (M pro) inhibitor with an IC50 value of 37nM. MAT-POS-e194df51-1 is cytotoxic with EC50 values of 64 nM and 126 nM in A549-ACE2-TMPRSS2 cells and HeLa -ACE2 cells, respectively .
SARS-CoV-2-IN-32 (compound 3g) is a COVID-19 inhibitor. SARS-CoV-2-IN-32 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-32 exhibits comparatively high binding affinity (-8.8 Kcal/mole) to COVID-19 mainprotease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-32 can be used in studies of cancer and COVID-19 .
SARS-CoV-2-IN-33 (compound 3m) is a COVID-19 inhibitor. SARS-CoV-2-IN-33 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-33 exhibits comparatively good binding affinity (-8.0 Kcal/mole) to COVID-19 mainprotease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-33 can be used in studies of cancer and COVID-19 .
SARS-CoV-2 Mpro-IN-23 (Compound 2) is an inhibitor for SARS-CoV-2 mainprotease (Mpro), which inhibits wildtype Mpro and mutant Mpro variants, with IC50 of 0.057-0.92 μM. SARS-CoV-2 Mpro-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 .
PROTAC SARS-CoV-2 Mpro degrader-3 (Compound P2) exhibits antiviral activity through the degradation of the mainprotease (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)) .
MPD2 is a Cereblon-binding ligand-based PROTAC that degrades MPro, the mainprotease 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)) .
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits M pro (the mainprotease of SARS-CoV-2) and also has anti-inflammatory activity .
Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin hemisulfate potently inhibits serine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits M pro (the mainprotease of SARS-CoV-2) and also has anti-inflammatory activity .
Tectoquinone (2-Methylanthraquinone) is a SARSCoV-2mainprotease inhibitor against COVID-19. Tectoquinone exhibits strong mosquito larvicidal activity with the LC50 values of 3.3 and 5.4 μg/ml against A. aegypti and A. albopictus in 24 h, respectively .
Silymarin is an extract of the milk thistle (Silybum marianum). Silymarin is an effective SARS-CoV-2 mainprotease (M pro) inhibitor. Silymarin can significantly reduce tumor cell proliferation, angiogenesis as well as insulin resistance. Silymarin has the chemopreventive effect on hepatocellular carcinoma (HCC). Silymarin has the potential for COVID-19 research .
(±)-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 mainprotease of SARS-CoV-2 (Mpro) .
Solasurine is a steroidal alkaloid that can be isolated from Solanum surrattence. Solasurine can interact with the C3-like protease (SARS-CoV-2 mainprotease) amino acids Phe8, Pro9, Ile152, Tyr154, Pro293, Phe294, Val297, and Arg298 .
Kazinol F is a polyphenol from Broussonetia papyrifera. Kazinol F also is an effective Mpro inhibitor. Kazinol F has interaction with both the catalytic residues (His41 and Cys145) of Mpro and exhibits good binding affinity. Kazinol F can be used for the research of COVID-19 .
Euptox A (9-Oxo-10, 11-dehydroageraphorone), a cadenine sesquiterpene, is the main toxin that can be isolated from Eupatorium adenophorum. Euptox A induces apoptosis by improving the gene expression level of apoptotic proteases such as caspase-10 in HeLa cells .
SARS-CoV-2 Mpro-IN-22 (compound 4), a hydrolysable tannin, is a potent SARS-CoV-2 mainprotease (Mpro) inhibitor with an IC50 value of 1.2 µg/mL. SARS-CoV-2 Mpro-IN-22 does not show any significant cytotoxic activity against A549 and HUVEC cell lines .
SARS-CoV MPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 M pro with an IC50 value of 72.07 nM. The mainprotease (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-CoV MPro-IN-2 has the potential for the research of COVID-19 .
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 mainprotease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][2][5].
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