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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 .
Bardoxolone (CDDO; RTA 401) is a Nrf2 activator. Bardoxolone shows anti-SARS-CoV-23CLpro with IC50 of 27.99 μM. Bardoxolone activates the Nrf2 pathway and inhibits the NF-κB pathway. Bardoxolone can induce cells differentiation, apoptosis and shows antiproliferative activity against cancer cells. Bardoxolone can increase ROS and decrease intracellular GSH levels.Bardoxolone inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis. Bardoxolone can be used for the research of cancer, inflammation and infection, such as SARS-CoV infection and glioblastoma .
Secutrelvir is an oral SARS-CoV-2 3C-like protease (3CLpro) inhibitor and antiviral agent, with IC50 values of 0.655 nM and 0.697 nM against SARS-CoV-2 3CLpro, respectively. Secutrelvir forms a reversible covalent bond with the catalytic cysteine C145 of SARS-CoV-2 3CLpro, thereby inhibiting viral replication. Secutrelvir exhibits activity against multiple SARS-CoV-2 variants and can be used in research related to coronavirus disease 2019 (COVID-19) .
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 .
PROTAC KRAS G12D degrader 2 is a peptidomimetic PROTAC specifically targeting the dimeric SARS-CoV-2 3CL Pro protein. PROTAC KRAS G12D degrader 2 inhibits SARS-CoV-2 3CLPro with an IC50 of 21.2 μM. PROTAC KRAS G12D degrader 2 specifically binds to the active site of SARS-CoV-2 3CL Pro. PROTAC KRAS G12D degrader 2 reduces protein levels of SARS-CoV-2 3CL Pro without affecting cell viability. PROTAC KRAS G12D degrader 2 can be used for the study of viral infections in Coronavirus genera .
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.
Methyl rosmarinate is an orally active hydroxycinnamic acid. Methyl rosmarinate exhibits an IC50 of 24.70 μM and a Ki of 15.29 μM against PTP1B, an IC50 of 41.46 μg/mL against BChE, a Ki of 0.61 mM against mushroom tyrosinase, and an IC50 of 2.50 μM against SARS-CoV-23CLpro. Methyl rosmarinate downregulates the phosphorylation levels of ERK, JNK, p38, Smad2 and Smad3. Methyl rosmarinate activates erythrocyte BPGM and promotes the production of 2,3-BPG. Methyl rosmarinate induces apoptosis of fibroblasts. Methyl rosmarinate prolongs the survival time of hypoxic mice. Methyl rosmarinate improves insulin sensitivity. Methyl rosmarinate binds to SARS-CoV-2 3CLpro and inhibits viral replication. Methyl rosmarinate induces glioblastoma cell death. Methyl rosmarinate activates the TGR5/AMPK axis and reduces the levels of ROS and MDA. Methyl rosmarinate shows inhibitory activity against MMP-1. Methyl rosmarinate can be used in research related to pulmonary fibrosis, hypoxia-induced injury, type 2 diabetes, Alzheimer's disease, hyperpigmentation disorders, COVID-19, glioblastoma and myocardial ischemia-reperfusion injury .
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 .
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) .
Ritonavir-d6 is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.61 μM .
SARS-CoV-2 3CLpro-IN-6 is a reversible covalent inhibitor of SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro-IN-6 has potent inhibitory activity for SARS-CoV-2 3CL pro with an IC50 value of 4.9 μM. SARS-CoV-2 3CLpro-IN-6 can be used for the research of coronavirus disease 2019 (COVID-19) .
SARS-CoV-2 3CLpro-IN-13 is a potent SARS-CoV-2 3CL protease inhibitor with an IC50 value of 21 nM. SARS-CoV-2 3CLpro-IN-13 shows anti-coronavirus activity .
SARS-CoV-2 3CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro probe-1 can detect endogenously expressed 3CLpro in SARS-CoV-2-infected cells .
Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-2 3CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis .
SARS-CoV-2 3CLpro-IN-22 (Compound 17) is a cathepsin L (CTSL ) inhibitor with an IC50 value of 32.5 nM. SARS-CoV-2 3CLpro-IN-22 can be used for the study of SARS-CoV-2 virus .
SARS-CoV-2 3CLpro-IN-31 (Compound 13c) is a potent SARS-CoV-2 3CL protease (3CLpro) inhibitor of with an IC50 value of 37.33 nM. SARS-CoV-2 3CLpro-IN-31 blocks viral polyprotein cleavage and inhibits SARS-CoV-2 replication. SARS-CoV-2 3CLpro-IN-31 is promising for research of SARS-CoV-2 infection .
GRL-0496 is a potent chloropyridyl ester-derived SARS-CoV3CLpro inhibitor, with an IC50 of 30 nM in both enzyme inhibitory and antiviral assays. GRL-0496 shows SARS-CoV antiviral activity, with an EC50 of 6.9 μM .
SARS-CoV-2 3CLpro-IN-16 (Compound 3a) is a covalent SARS-CoV-2 3CLpro inhibitor (IC50: 2.124 μM). SARS-CoV-2 3CLpro-IN-16 binds to the active site and forms a covalent bond with Cys145 of 3CLpro .
SARS-CoV-2 3CLpro-IN-15 (compound a) is a beta-nitrostyrene coronavirus SARS-CoV-2 inhibitor that targets the SARS-CoV-2 3CL protease (3CLpro). SARS-CoV-2 3CLpro-IN-15 inhibits viral replication and transcription and plays a key role in the discovery of anti-COVID-19 lead compounds .
SARS-CoV-2 3CLpro-IN-2 (Compound 1) is a potent inhibitor of 3CL protease. SARS-CoV-2 3CLpro-IN-2 has the potential for the research of SARS-CoV-2 diseases .
SARS-CoV-2 3CLpro-IN-30 (compound 29) is a potent inhibitor of SARS-CoV-2 3CL protease (SARS-CoV-2 3CLpro), with the IC50 and EC50 of 0.04 and 0.3 μM .
SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CL pro). SARS-CoV-2 3CLpro-IN-5 has inhibitory activity for 3CL pro with an IC50 value of 3.8 nM. SARS-CoV-2 3CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-2 3CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19) .
SARS-CoV-2 3CLpro-IN-25 (compound 56) inhibits the SARS-CoV-2 3CLpro with the IC50 of 70 nM and displays antiviral activity in cells with the EC50 of 3.1 μM .
SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC50 of 0.43 μM. SARS-CoV-2 3CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .
SARS-CoV-2 3CLpro-IN-33 (Compound 16) is an orally active SARS-CoV-2 3CL protease inhibitor, with an IC50 value of 1.5 nM. SARS-CoV-2 3CLpro-IN-33 shows excellent anti-SARS-CoV-2 viral activity in the HEK293T-AT cell model with an EC50 of 0.017 μM. SARS-CoV-2 3CLpro-IN-33 can be used for the study of COVID-19 infetction .
SARS-CoV-2 3CLpro-IN-23 (Compound Cd3) is a compound that can be isolated from Citrus depressa. SARS-CoV-2 3CLpro-IN-23 has good inhibitory activity to the SARS-CoV-2 spike protein, with KD of 0.79 μM. SARS-CoV-2 3CLpro-IN-23 can bind to key amino acid residue, disrupting the formation of the spike protein and h-ACE2 complex .
SARS-CoV-2 3CLpro-IN-27 (Compound 9H) is an inhibitor of SARS-CoV-2 3CL pro with an IC50 value of 21 nM. SARS-CoV-2 3CLpro-IN-27 exhibits excellent anti-SARS-CoV-2 replicon activity, demonstrating an EC50 value of 5 nM .
SARS-CoV-2 3CLpro-IN-21 (Compound D6) irreversibly and covalently inhibits SARS-CoV-2 3CL pro with an IC50 of 0.03 μM. SARS-CoV-2 3CLpro-IN-21 also inhibits SARS-CoV-13CLpro with an IC50 of 0.12μM .
SARS-CoV-2 3CLpro-IN-19 (Compound C5a) is a non-covalent, non-peptide SARS-CoV-2 3CLpro inhibitor (IC50s: 0.7 μM). SARS-CoV-2 3CLpro-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-2 3CLpro with IC50 of 51.3 nM. 3CLPro-IN-3 exhibits antiviral activity against human coronavirus 229E, OC43 and mouse hepatitis virus MHV .
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 .
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 3.49 μM .
Ledipasvir (GS-5885) hydrochloride is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir hydrochloride is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.62 μM .
ALG-097558 is an orally active 3CLpro inhibitor. ALG-097558 demonstrates pan-coronavirus activity against various SARS-CoV-2 variants as well as other human coronaviruses (HCoVs) such as SARS-CoV-1, α-HCoV 229E, and β-HCoV OC43. ALG-097558 demonstrates potent inhibition with IC50s of 2 nM (SARS-CoV-2 3CLpro) and 6 nM (229E 3CLpro). ALG-097558 demonstrates antiviral activity in the SARS-CoV-2 hamster infection model. ALG-097558 can be used for the study of viral infections[1].
(S)-ML188 is a SARS-CoV 3-chymotrypsin-like protease (3CLpro) inhibitor (IC50: 1.5 μM). (S)-ML188 has antiviral activity with an EC50 value of 12.9 μM against SARS-CoV. (S)-ML188 inhibits the activity of 3CLpro via non-covalent binding and can be used in the study of SARS-CoV .
(±)-Tuaimenal A ((+)-1) is a secondary metabolite and a derivative of Sesamol (HY-N1417). (±)-Tuaimenal A has potent inhibitory activity against SARS-CoV-2 3CLpro with an IC50 of 33.3 μM. (±)-Tuaimenal A can be used for SARS-CoV-2 infection research .
SARS-CoV-2 3CLpro-IN-37 is a non-covalent SARS-CoV-2 3CLpro inhibitor with an IC50 of 3.2 nM. SARS-CoV-2 3CLpro-IN-37 blocks the cleavage and replication of viral polyproteins. SARS-CoV-2 3CLpro-IN-37 is applicable to research related to COVID-19 .
SARS-CoV-2 3CLpro-IN-36 is a SARS-CoV-2 3CLpro inhibitor and antiviral agent with a human sub-micromolar IC50 against SARS-CoV-2 3CLpro.SARS-CoV-2 3CLpro-IN-36 forms a covalent bond with catalytic Cys145 of SARS-CoV-2 3CLpro; its tetrazole core occupies the S1 pocket and interacts with His163, while its chloroacetamide carbonyl forms hydrogen bonds with the backbone amides of Gly143 and Ser144 in the oxyanion hole.SARS-CoV-2 3CLpro-IN-36 reduces SARS-CoV-2 replication in infected cells.SARS-CoV-2 3CLpro-IN-36 can be used for the research of SARS-CoV-2 infection .
SARS-CoV-2 3CLpro-IN-35 is a SARS-CoV-2 3CLpro inhibitor with an IC50 of 0.15 μM. SARS-CoV-2 3CLpro-IN-35 inhibits the proliferation of bladder cancer cells, exerts anti-SARS-CoV-2 activity, and exhibits low cytotoxicity in fibroblasts. SARS-CoV-2 3CLpro-IN-35 is applicable to research related to SARS-CoV-2 infection and bladder cancer .
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-2 3CLpro .
Glecaprevir (Standard) is the analytical standard of Glecaprevir. This product is intended for research and analytical applications. Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM. Glecaprevir is also a SARS-CoV3CLpro inhibitor with an IC50 of 4.09 μM .
SARS-CoV-2 3CLpro-IN-34 (Compound 55) is a highly efficient non-covalent inhibitor of the SARS-CoV-2 3CL pro protease (b. SARS-CoV-2 3CL pro protease) with an IC50 of 1.9 μM. SARS-CoV-2 3CLpro-IN-34 can inhibit the 3CL pro protein of SARS-CoV-1, with its IC50 being 3.2 μM, and it shows high selectivity towards host cysteine proteases (such as cathepsins L/K and calpain). SARS-CoV-2 3CLpro-IN-34 exhibits antiviral activity in cells infected with SARS-CoV-2, with its EC50 being 25 μM, and it is not affected by P-gp inhibitors and shows no significant cytotoxicity. SARS-CoV-2 3CLpro-IN-34 can be used for research on SARS-CoV-2 infection .
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.62 μM .
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-2 3CLpro activity .
Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 3.49 μM .
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 . Telaprevir inhibits SARS-CoV-2 3CLpro activity .
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 14.2 μM .
SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease(3CLpro) with an IC50 and EC50 of 0.17 and 1.45 nM, respectively. SARS-CoV-2 3C-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-2 3CL protease(3CLpro) with an IC50 and EC50 of 0.13 and 1.03 nM, respectively. SARS-CoV-2 3C-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 .
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 .
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 .
Hydroxyethylamine (Compd VII) is a SARS-CoV-2 3CLpro inhibitor with an IC50 of ~10 μM in the spread assay. Hydroxyethylamine has potent antiviral activities .
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-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease .
3CPLro-IN-1 (compound A17) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro 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 .
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 .
SARS-CoV-2-IN-107 (Compound A7) is the inhibitor for SARS-CoV-2 3CLpro 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 .
3CPLro-IN-2 (compound C1) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro 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 .
Ritonavir- 13C,d3 is the 13C- and deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.61 μM.
Amprenavir-d4-1 is deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.09 μM.
Amprenavir-d4 is the deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.09 μM .
Amprenavir (Standard) is the analytical standard of Amprenavir. This product is intended for research and analytical applications. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.09 μM.
MAC-5576 is a SARS-CoV-2 3CL 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) .
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-2 3CLpro 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].
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 . Boceprevir inhibits SARS-CoV-2 3CLpro activity .
rel-Ritonavir-d6 (rel-ABT 538-d6) is the deuterium labeled rel-Ritonavir. rel-Ritonavir is a relative configuration of Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to study of HIV infection and AIDS. Ritonavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.61 μM .
Narlaprevir (Standard) is the analytical standard of Narlaprevir. This product is intended for research and analytical applications. Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM . Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease . Narlaprevir is also a SARS-CoV3CLpro inhibitor with an IC50 of 2.3 μM .
Atazanavir-d5 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 3.49 μM .
Atazanavir (sulfate) (Standard) is the analytical standard of Atazanavir (sulfate). This product is intended for research and analytical applications. Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir sulfate is also a SARS-CoV3CLpro inhibitor with an IC50 of
3.49 μM .
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 . Telaprevir inhibits SARS-CoV-2 3CLpro activity .
Paritaprevir (Standard) is the analytical standard of Paritaprevir. This product is intended for research and analytical applications. Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor) .
MI-30 is an orally active SARS-CoV-23CLpro inhibitor (IC50 = 17.2 nM). MI-30 reduces viral load and lung lesions in a mouse model of SARS-CoV-2 infection. MI-30 may be used in coronavirus infection research .
Catechin-5-O-gallate is a bioactive substance. Catechin-5-O-gallate can be isolated from bioactive Himalayan plants. Catechin-5-O-gallate is predicted to be a P-glycoprotein inhibitor, and binds to SARS-CoV-23CLpro, PLpro and RdRp. Catechin-5-O-gallate can be used in studies related to COVID-19 .
Danoprevir (Standard) is the analytical standard of Danoprevir (HY-10238). This product is intended for research and analytical applications. Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC50 of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC50 higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC50s=0.2-0.4 nM) as well as 2b and 3a (IC50s=1.6, 3.5 nM) . Danoprevir is also a SARS-CoV3CLpro inhibitor with an IC50 of 0.05 μM .
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 .
SARS-CoV-2 3CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro 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-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease .
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-2 3CLpro .
Methyl rosmarinate is an orally active hydroxycinnamic acid. Methyl rosmarinate exhibits an IC50 of 24.70 μM and a Ki of 15.29 μM against PTP1B, an IC50 of 41.46 μg/mL against BChE, a Ki of 0.61 mM against mushroom tyrosinase, and an IC50 of 2.50 μM against SARS-CoV-23CLpro. Methyl rosmarinate downregulates the phosphorylation levels of ERK, JNK, p38, Smad2 and Smad3. Methyl rosmarinate activates erythrocyte BPGM and promotes the production of 2,3-BPG. Methyl rosmarinate induces apoptosis of fibroblasts. Methyl rosmarinate prolongs the survival time of hypoxic mice. Methyl rosmarinate improves insulin sensitivity. Methyl rosmarinate binds to SARS-CoV-2 3CLpro and inhibits viral replication. Methyl rosmarinate induces glioblastoma cell death. Methyl rosmarinate activates the TGR5/AMPK axis and reduces the levels of ROS and MDA. Methyl rosmarinate shows inhibitory activity against MMP-1. Methyl rosmarinate can be used in research related to pulmonary fibrosis, hypoxia-induced injury, type 2 diabetes, Alzheimer's disease, hyperpigmentation disorders, COVID-19, glioblastoma and myocardial ischemia-reperfusion injury .
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 .
Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-2 3CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis .
Atazanavir (sulfate) (Standard) is the analytical standard of Atazanavir (sulfate). This product is intended for research and analytical applications. Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir sulfate is also a SARS-CoV3CLpro inhibitor with an IC50 of
3.49 μM .
SARS-CoV-2 3CLpro/3C-like protease is a viral cysteine protease that plays a crucial role in the co-translational proteolytic processing of coronavirus polyproteins. Since no homologous proteins with similar cleavage sites exist in the human body, SARS-CoV-2 3CLpro/3C-like protease is a high-quality target for the development of drugs related to COVID-19. SARS-CoV-2 3CLpro/3C-like protease protein is a recombinant, untagged SARS-CoV-2 3CLpro/3C-like protease protein expressed by E.coli.
SARS-CoV-2 3CLpro/3C-like protease Protein (Tag Free) is a viral cysteine protease that plays a crucial role in the co-translational proteolytic processing of coronavirus polyproteins. Since no homologous proteins with similar cleavage sites exist in the human body, SARS-CoV-2 3CLpro/3C-like protease Protein (Tag Free) is a high-quality target for the development of drugs related to COVID-19. SARS-CoV-2 3CLpro/3C-like protease Protein (Tag Free) is a recombinant, SARS-CoV-2 3CLpro/3C-like protease Protein (Tag Free) expressed by E.coli.
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.
Ritonavir-d6 is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.61 μM .
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 3.49 μM .
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.62 μM .
Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 3.49 μM .
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 . Telaprevir inhibits SARS-CoV-2 3CLpro activity .
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 14.2 μM .
Ritonavir- 13C,d3 is the 13C- and deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.61 μM.
Amprenavir-d4-1 is deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.09 μM.
Amprenavir-d4 is the deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.09 μM .
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 . Boceprevir inhibits SARS-CoV-2 3CLpro activity .
rel-Ritonavir-d6 (rel-ABT 538-d6) is the deuterium labeled rel-Ritonavir. rel-Ritonavir is a relative configuration of Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to study of HIV infection and AIDS. Ritonavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 1.61 μM .
Atazanavir-d5 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration . Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp) . Atazanavir is also a SARS-CoV3CLpro inhibitor with an IC50 of 3.49 μM .
SARS-CoV-2 3CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro probe-1 can detect endogenously expressed 3CLpro in SARS-CoV-2-infected cells .
SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC50 of 0.43 μM. SARS-CoV-2 3CLpro-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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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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