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Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2 Mpro 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 .
Mpro inhibitor N3 is a potent SARS-CoV-2 MPro inhibitor with an EC50 value of 16.77 µM. Mpro inhibitor N3 shows antiviral activities against HCoV-229E, FIPV, IBV and MHV-A59 .
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) .
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) .
Mpro/PLPro-IN-2 (Compound 22l) is a non-covalent competitive dual inhibitor of the papain-like protease and main protease of SARS-CoV-2, with a Ki of 0.2 μM for the papain-like protease and a Ki of 1.1 μM for the main protease . Mpro/PLPro-IN-2 can be used in the research field of anti-SARS-CoV-2 .
SARS-CoV-2 Mpro-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-2 Mpro-IN-22 does not show any significant cytotoxic activity against A549 and HUVEC cell lines .
SARS-CoV-2 Mpro-IN-13 (compound 20j) is a covalent SARS-CoV-2 Protease Mpro inhibitor with an IC50 value of 19.0 nM. SARS-CoV-2 Mpro-IN-13 processes antiviral activity with an EC50 value of 138.1 nM .
SARS-CoV-2 Mpro-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-2 Mpro-IN-10 can be used for the research of SARS-CoV-2 virus .
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 M pro inhibitor with an IC50 of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3 .
SARS-CoV-2 Mpro-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-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 .
SARS-CoV-2 Mpro-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-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 MPro-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-CoV MPro-IN-2 has the potential for the research of COVID-19 .
SARS-CoV-2 Mpro-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-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 .
SARS-CoV-2 Mpro-IN-40 (compound 119) is an inhibitor of SARS-CoV-2 Mpro, with an IC50 value of 15.7 nM against Mpro Fret. SARS-CoV-2 Mpro-IN-40 exhibits low metabolic stability in human microsomes .
SARS-CoV-2 Mpro-IN-34 (Compound 26) is an inhibitor for SARS-CoV-2 Mpro with an IC50 of 6 nM. SARS-CoV-2 Mpro-IN-34 exhibits inhibitory efficacy against OC43 Mpro with an IC50 of 33 nM. SARS-CoV-2 Mpro-IN-34 exhibits antiviral activity in SARS-CoV-2 infected Vero E6 cell with an EC50 of 0.103 μM .
SARS-CoV-2 Mpro-IN-44 (Compound 25) is a broad-spectrum coronavirus main protease (Mpro) inhibitor. SARS-CoV-2 Mpro-IN-44 has inhibitory activity against a variety of high-risk coronaviruses (including SARS-CoV-2 and PEDV, etc.) (IC50: < 0.6 μM). SARS-CoV-2 Mpro-IN-44 achieves broad-spectrum inhibition of coronaviruses by enhancing the interaction with the conserved sites of Mpro. SARS-CoV-2 Mpro-IN-44 can be used for anti-coronavirus drug development .
SARS-CoV-2 Mpro-IN-29 (Compound 7) is an inhibitor of the SARS-CoV-2 main protease (Mpro) with an IC50 of 310 nM and an EC50 of 0.5 μM in Vero cells. SARS-CoV-2 Mpro-IN-29 binds to the active site of Mpro, blocking the cleavage of viral polyproteins, showing significant antiviral activity and enhanced metabolic function. SARS-CoV-2 Mpro-IN-29 holds potential for research on SARS-CoV-2 antiviral agents .
SARS-CoV-2 Mpro-IN-19 (compound MPI94) is a SARS-CoV-2 MPro inhibitor with the IC50 of 0.096 μM. SARS-CoV-2 Mpro-IN-19 can be used for study of COVID-19 .
SARS-CoV-2 Mpro-IN-42 (compound C5) is a potent SARS-CoV-2 Mpro inhibitor with an IC50 of 33.6 nM. SARS-CoV-2 Mpro-IN-42 can be used in the study of SARS-CoV-2 .
SARS-CoV-2 Mpro-IN-43 (Compound 1) is a coronavirus main protease (Mpro) inhibitor (IC50: 72 μM). SARS-CoV-2 Mpro-IN-43 interacts with key residues in the active site of Mpro via non-covalent binding, exerting its anti-coronavirus effect. SARS-CoV-2 Mpro-IN-43 exhibits moderate to low cytotoxicity, with CC50 values of 13.24, 41.02, and 42.26 µM in HaCaT, HEK293T, and HepG2 cells, respectively. SARS-CoV-2 Mpro-IN-43 can be used in anti-SARS-CoV-2 research .
SARS-CoV-2 Mpro-IN-18 (compound 84) is a potent SARS-CoV-2 Mpro inhibitor with the IC50 of 3.23 nM. SARS-CoV-2 Mpro-IN-18 can be used for study of anti-SARS-CoV-2 agent .
SARS-CoV-2 Mpro-IN-24 (Compound X77) is a inhibitor of SARS-CoV-2 Mpro (IC50=2.8 μM) and also a non-covalent inhibitor of SARS-CoV Mpro (IC50=3.4 μM) .
SARS-CoV-2 Mpro-IN-14 (Compound 19) is an inhibitor of SARS-CoV-2 Mpro with an IC50 of 0.044 μM. SARS-CoV-2 Mpro-IN-14 exhibits water solubility, has no cytotoxicity, and can be used in the study of COVID-19 .
SARS-CoV-2 Mpro-IN-17 (compound S5-28) is an orally active and noncovalent SARS-CoV-2 Mpro inhibitor with the EC50 of 1.35 μM. SARS-CoV-2 Mpro-IN-17 can be used for study of COVID-19 .
SARS-CoV MPro-IN-1 is a SARS-CoV-2 3CLpro 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 .
SARS-CoV-2 Mpro-IN-20 (compound MPI100) is a SARS-CoV-2 main protease inhibitor. SARS-CoV-2 Mpro-IN-20 shows antiviral activity with the EC50 of 3.4 μM .
SARS-CoV-2 Mpro-IN-21 (compound A8) is a potent SARS-CoV-2 and OVID-19 Main Protease 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 .
SARS-CoV-2 Mpro-IN-39 (Compound 9d) is an inhibitor of the main protease (Mpro) of SARS-CoV-2, with an IC50 value of 5.94 µM, an EC50 value of 9.33 µM for inhibiting the replication of SARS-CoV-2 in Vero cells, and a cytotoxicity CC50 value of 289.63 µM. SARS-CoV-2 Mpro-IN-39 can be used in the research of the anti-COVID-19 field .
SARS-CoV-2 Mpro-IN-36 (Compound 6d) is an inhibitor of SARS-CoV-2 M pro with an IC50 of 110 nM. SARS-CoV-2 Mpro-IN-36 exhibits antiviral activity with an EC50 of 1.6 μM .
SARS-CoV-2 Mpro-IN-25 (Compound 3a) is a SARS-CoV-2 protease inhibitor with an IC50 value of 0.26 μM. SARS-CoV-2 Mpro-IN-25 exhibits antiviral activity and can be used in pneumonia-related research .
SARS-CoV-2 Mpro-IN-41 (Compound 7e) is an orally active inhibitor of COX-2 and SARS-CoV-2 M pro (IC50 values are 9.66 μM and 13.24 μM, respectively). SARS-CoV-2 Mpro-IN-41 also has a certain inhibitory activity against COX-1 (IC50: 46.11 μM). SARS-CoV-2 Mpro-IN-41 can significantly inhibit the expression of inflammatory-related cytokines (such as TNF-α, IL-6, IL-1β) and exert anti-inflammatory effects. SARS-CoV-2 Mpro-IN-41 exerts anti-inflammatory and antiviral effects by selectively inhibiting COX-2 and SARS-CoV-2 M pro. SARS-CoV-2 Mpro-IN-41 can be used for anti-inflammatory and anti-coronavirus research .
SARS-CoV-2 Mpro-IN-32 (Compound 1) is a selective inhibitor of SARS-CoV-2 M Pro with an IC50 value of 230 nM. SARS-CoV-2 Mpro-IN-32 can also inhibit the replication of multiple SARS-CoV-2 variants in vitro .
SARS-CoV-2 Mpro-IN-37 (compound 8r) is a SARS-CoV-2 main protease (M pro) inhibitor, with an IC50 of 0.0199 μM. SARS-CoV-2 Mpro-IN-37 inhibits SARS-CoV-1 M pro and MERS-CoV M pro with IC50s of 0.00945 and 0.111 μM, respectively. SARS-CoV-2 Mpro-IN-37 displays high antiviral activity in the nanomolar range without showing cellular toxicity .
SARS-CoV-2 Mpro-IN-31 (Compound 18) is an inhibitor of SARS-CoV-2 M Pro with an IC50 value of 11 nM. Additionally, SARS-CoV-2 Mpro-IN-31 effectively inhibits the enzymatic activity of the cysteine proteases cathepsin B and cathepsin L, with IC50 values of 24 nM and 1.8 nM, respectively .
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)) .
SARS-CoV-2 Mpro-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-2 Mpro-IN-2 can be used in COVID-19 studies .
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 .
CDD-1819 is a non-covalent and non-peptide potent SARS-CoV-2 Mpro inhibitor with a Ki of 5 nM. CDD-1819 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants .
CDD-1733 is a non-covalent and non-peptide potent SARS-CoV-2 Mpro inhibitor with a Ki of 12 nM. CDD-1733 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants .
CDD-1845 is a non-covalent and non-peptide potent SARS-CoV-2 Mpro inhibitor with a Ki of 3 nM. CDD-1845 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants .
SARS-CoV-2 Mpro-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-2 Mpro-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) .
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) .
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 .
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)) .
Olgotrelvir (STI-1558) is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir can effectively inhibit both SARS-CoV-2 replication and entry into host cells .
Olgotrelvir (STI-1558) sodium is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir sodium is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir sodium can effectively inhibit both SARS-CoV-2 replication and entry into host cells .
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 .
SARS-CoV-2-IN-36 is a potent SARS-CoV-2 Mpro (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 .
Leupeptin (hemisulfate) (Standard) is the analytical standard of Leupeptin (hemisulfate). This product is intended for research and analytical applications. Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin hemisulfate potently inhibits serine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].
SARS-CoV-2-IN-1 is a potent Mpro inhibitor. SARS-CoV-2-IN-1 inhibits the purified recombinant SARS-CoV-2 Mpro, SARS-CoV Mpro and MERS-CoV Mpro with IC50s of 0.67, 0.90 and 0.58 μM, respectively .
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-2 Mpro and PEDV Mpro, respectively .
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 .
D-4-77 is a potent inhibitor of SARS-CoV-2 Mpro 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-2 Mpro -induced antagonism of the host NF-κB innate immune response .
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-2 MPro 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 .
Tectoquinone (2-Methylanthraquinone) is an inhibitor for SARS CoV-2 major protease (SARS CoV-2 Mpro). Tectoquinone exhibits anti-termite and antiviral activities .
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)) .
(±)-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) .
X77 is a potent non-covalent inhibitor of the main protease 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 .
(Rac)-X77?is a racemate of X77. X77 is a potent non-covalent inhibitor of the main protease 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 .
Garcinone B, a xanthone derivative, is a nature product that could be isolated from the pericarp of Mangosteen. Garcinone B is a potent ACE2 and Mpro inhibitor. Garcinone B can be used in research of COVID-19 .
Setomimycin is a potent antibiotic. Setomimycin inhibits the SARS-CoV-2 Mpro enzyme with an IC50 value of 12.02 µM. Setomimycin shows anti-inflammatory and antioxidant properties. Setomimycin shows antiproliferative and antitumor activity .
SARS-CoV-2-IN-68 (compound 6C) is a covalent SARS-CoV-2 PLpro/Mpro inhibitor with potent antiviral activities. SARS-CoV-2-IN-68 binds to Zn-finger domain of PLpro .
Tectoquinone (Standard) is the analytical standard of Tectoquinone. This product is intended for research and analytical applications. Tectoquinone (2-Methylanthraquinone) is an inhibitor for SARS CoV-2 major protease (SARS CoV-2 Mpro). Tectoquinone exhibits anti-termite and antiviral activities .
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 .
LY1 is a potent, selective and covalent inhibitor against both SARS-CoV-2 PL pro and M pro with Kd values of 1.5 μM and 2.3 μM for M pro C145A protein and PL pro C111A protein, respectively. LY1 potent against the viral proteases, with IC50s of 0.12 μM and 0.99 μM against M pro and PL pro. LY1 shows high selectivity over other kinases, human proteases and metalloenzyme .
E3 ligase Ligand 66 is an E3 ligase ligand that can be used to recruit IAP proteins. E3 ligase Ligand 66 can be linked to SARS-CoV-2 Mpro ligand 1 (HY-176442) through a linker to form PROTAC BP-198 (HY-176440) .
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) .
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) .
Miltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC50 of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; Ki = 0.04 μM) and SARS-CoV main protease (Mpro) .
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-CoV Mpro (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].
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.
NZ-804 is an orally active inhibitor for SARS-CoV-2 main protease Mpro with an IC50 of 8.9 nM. NZ-804 inhibits the SARS-CoV-2 replication in HeLa-hACE2 cell with an EC50 of 14 nM. NZ-804 exhibits board-spectrum antiviral activity aganst multiple CoVs. NZ-804 diminishes virus replication in mouse and hamster model .
(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) .
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) .
TKB272 is an orally active and selective antiviral agent targeting the main protease (Mpro) of SARS-CoV-2. It effectively blocks the infection and replication of various SARS-CoV-2 strains, including Omicron variants such as XBB.1.5 and EG.5.1. The enzymatic inhibitory activity of TKB272 shows an IC50 of 0.7 µM (against SARS-CoV-2WK-521 Mpro), and its antiviral activity at the cellular level reaches an EC50 as low as 2.6 nM (against BQ.1.1 strain in HeLahACE2-TMPRSS2 cells), with a cytotoxicity CC50 of 98 µM, indicating no apparent toxicity. In addition, TKB272 significantly suppresses the replication of SARS-CoV-2XBB.1.5 in B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse models. TKB272 holds promise for research in the field of SARS-CoV-2 infection .
SP inhibitor 1 (compound 34) is a selective SARS-CoV-2 spike protein (SP) inhibitor with an IC50 of 3.26 μM, >25 μM, >25 μM for SP, M pro and PL pro protein, respectively. SP inhibitor 1 is a vitro SARS-CoV-2 replication inhibitor at non-toxic concentrations (0.3250<5.98 μM). SP inhibitor 1 shows cellular antiviral activity .
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 .
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 main protease of SARS-CoV-2) and also has anti-inflammatory activity .
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits M pro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity .
Ebselen (SPI-1005), a glutathione peroxidase mimetic, is a potent voltage-dependent calcium channel (VDCC) blocker . Ebselen potently inhibits M pro (IC50=0.67 μM) and COVID-19 virus (EC50=4.67 μM) .Ebselen is an inhibitor of HIV-1 capsid CTD dimerization. Ebselen, an organoselenium compound, can permeate the blood-brain barrier and has anti-inflammatory, antioxidant and anticancer activity .
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits M pro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity .
Tectoquinone (2-Methylanthraquinone) is an inhibitor for SARS CoV-2 major protease (SARS CoV-2 Mpro). Tectoquinone exhibits anti-termite and antiviral activities .
SARS-CoV-2 Mpro-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-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 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-CoV MPro-IN-2 has the potential for the research of COVID-19 .
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 .
Leupeptin (hemisulfate) (Standard) is the analytical standard of Leupeptin (hemisulfate). This product is intended for research and analytical applications. Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin hemisulfate potently inhibits serine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].
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-2 Mpro 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) .
Garcinone B, a xanthone derivative, is a nature product that could be isolated from the pericarp of Mangosteen. Garcinone B is a potent ACE2 and Mpro inhibitor. Garcinone B can be used in research of COVID-19 .
Tectoquinone (Standard) is the analytical standard of Tectoquinone. This product is intended for research and analytical applications. Tectoquinone (2-Methylanthraquinone) is an inhibitor for SARS CoV-2 major protease (SARS CoV-2 Mpro). Tectoquinone exhibits anti-termite and antiviral activities .
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 .
Miltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC50 of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; Ki = 0.04 μM) and SARS-CoV main protease (Mpro) .
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 main protease of SARS-CoV-2) and also has anti-inflammatory 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.
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.
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.
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.
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 .
(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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