HCV Protease

Ribavirin (Tribavirin) is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses.

Filibuvir (PF-00868554) is a selective and noncovalent inhibitor of HCV NS5B RNA-dependent RNA polymerase. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM.

Artemisinin (Qinghaosu) is an ancient Chinese herbal therapy for malarial fevers which has been recently found to have potent activity against many forms of malarial organisms, including chloroquine-resistant Plasmodium falciparum.

EIDD-1931 (Beta-d-N4-hydroxycytidine) is a ribonucleoside analog with antiviral activity.It inhibits replication of severe acute respiratory syndrome coronavirus (SARS-CoV) in Vero 76 cells, Middle East respiratory syndrome coronavirus (MERS-CoV) in Calu-3 2B4 cells, and SARS-CoV-2 in Vero cells (IC50s =0.1, 0.15 and 0.3 μM, respectively)

Levovirin (L-Ribavirin), the L-enantiomer of ribavirin, is a guanosine nucleoside analog with immunomodulatory activity and is used in the study of hepatitis C virus infection.

VCH-916 is a novel nonnucleoside HCV NS5B polymerase inhibitor.

BAY-43-9695 is a non-nucleoside compound with anti-human cytomegalovirus (HCMV) activity. It is the major metabolite of BAY-38-4766.

JTK-109 is an inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitor and inhibits G1b and G3a subgenomic replicons and recombinant enzymes.

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.

MK-8325 is a potent and orally available HCV NS5A inhibitor with replicative activity against a wide range of genotypes.MK-8325 has demonstrated bioavailability in in vitro and in vivo assays and has a favorable overall ADME profile.

BILB-1941 (BILB-1941ZW) is an inhibitor of HCV NS5B polymerase and can be used in studies about HCV infection.

7-benzyl-5,6-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine is a inhibitor of Hepatitis C Virus(HCV).

Antiviral agent 17 is a nucleoside analog with antiviral and antiparasitic activity, inhibits hepatitis C virus 1B and inhibits Trypanosoma brucei and Trypanosoma brucei, and can be used in the study of viral infections and malignant diseases.

Setrobuvir (ANA-598) is an orally active non-nucleoside HCV NS5B polymerase inhibitor with inhibitory effects on de novo RNA synthesis and primer extension with IC50s between 4 and 5 nM. setrobuvir shows good binding affinity for SARS-CoV-2 RdRp and induces inhibition of RdRp.

BMS-929075 is an orally active HCV NS5B replicase (HCV NS5B replicase) palm site variant inhibitor with potency, high oral bioavailability and pharmacokinetic parameters.BMS-929075 shows cytotoxicity.

Sovaprevir is a non-structural 3 (NS3) protease inhibitor with antiviral activity for the treatment of HCV infection.

Adafosbuvir PM (AL-335 PM) is a small molecule NS5B inhibitor that can be used to study chronic hepatitis C.

CHLORCYCLIZINE is a histamine H1 antagonist and a potent hepatitis C virus (HCV) entry inhibitor.

Isatoribine(ANA245) free base is a potent TLR7 receptor agonist with anti-hepatitis C virus infection activity for the study of HCV infection.

SB-734117 inhibits productive replication of several HCMV strains. SB-734117 exhibited polypharmacology and was an inhibitor of several proteins from the AGC and CMCG kinase groups.

TMC647055 Choline Hydroxide Salt is a novel and potent non-nucleoside inhibitor of the HCV NS5B polymerase which potentially for the treatment of HCV infection. It has nanomolar cellular potency (EC(50) of 82 nM) with minimal associated cell toxicity (CC(

Uprifosbuvir (MK-3682) is a uridine nucleoside monophosphate prodrug inhibitor of hepatitis C virus NS5B RNA polymerase with antiviral activity for the study of chronic hepatitis C virus.

IDX184 is a potent, orally active, targeted HCV polymerase inhibitor and nucleoside polymerase.IDX184 effectively inhibits HCV polymerase (IC50=0.31 μM, Ki=52.3 nM). IDX184 is a liver-targeted nucleotide prodrug with anti-HCV activity that inhibits HCV NS5B polymerase and can be used in combination with pegylated interferon-α2a and ribavirin for the primary treatment of chronic hepatitis C. It has been shown to inhibit HCV polymerase and nucleoside polymerase.

Lycorine hydrochloride (Narcissine hydrochloride) is VE-cadherin inhibitor,and has IC50 of 1.2μM in Hey1B cell.It is an HCV inhibitor with strong activity.

Resiquimod (R848) is an imidazoquinoline amine and Toll-like receptor (TLR) agonist with potential immune response modifying activity. Resiquimod exerts its effect through the TLR signaling pathway by binding to and activating TLR7 and 8 mainly on dendritic cells, macrophages, and B-lymphocytes. This induces the nuclear translocation of the transcription activator NF-kB as well as activation of other transcription factors. This may lead to an increase in mRNA levels and subsequent production of cytokines, especially interferon-alpha (INF-a) and other cytokines, thereby enhancing T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate Langerhans' cells, leading to an enhanced activation of T-lymphocytes.

Daclatasvir (EBP 883) (BMS-790052) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.

Deferiprone (Deferidone) is an Iron Chelator. The mechanism of action of deferiprone is as an Iron Chelating Activity.

Honokiol (NSC-293100) is the active principle of magnolia extract. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2.

Penciclovir (BRL 39123) is a Herpesvirus Nucleoside Analog DNA Polymerase Inhibitor. In HSV infected cells, penciclovir is phosphorylated by viral thymidine kinase and subsequently converted by cellular kinases into the active metabolite, penciclovir triphosphate, which competitively inhibits viral HSV polymerase by blocking deoxyguanosine triphosphate substrate binding. As a result, herpes viral DNA synthesis and replication are selectively inhibited.

Dasabuvir (ABT-333) is a non-nucleoside inhibitor of the hepatitis C virus (HCV) non-structural protein 5B (NS5B), an RNA-dependent RNA polymerase, with potential activity against HCV. Upon administration and after intracellular uptake, dasabuvir binds HCV NS5B polymerase and blocks viral RNA synthesis and replication. The HCV NS5B protein is essential for the replication of the HCV RNA genome.

Gentiopicroside (Gentiopicrin), a naturally occurring iridoid glycoside, extracted from Gentiana manshurica Kitag, inhibits P450 activity, with an IC50 and a Ki of 61 μM and 22.8 μM for CYP2A6; has antianti-inflammatoryand antioxidative effects.

Oenothein B is a specific inhibitor of poly(ADP-ribose) glycohydrolase. Oenothein B shows antioxidant, anti-inflammatory, antifungal, anti-HCV, and antitumor properties.

Boceprevir (SCH 503034) is a novel, potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with Ki of 14 nM in both enzyme assay and EC90 of 350 nM in cell-based replicon assay.

Simeprevir (TMC435) is a potent HCV NS3 4A protease inhibitor, and inhibits HCV replication with EC50 of 8 nM.

U18666A is a cell-permeable drug and is a cholesterol synthesis and transport inhibitor. It inhibits replication of Ebola virus, dengue virus, and human hepatitis C virus.

AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.

RO8191 (CDM-3008) (CDM-3008) is an agonist of interferon (IFN) receptor.

Platycodin D3 is a NF-κB inhibitor, it could as expectorants in diverse inflammatory pulmonary diseases, it can regulate the production and secretion of airway mucin; it can significantly enhance mitogen- and OVA-induced splenocyte proliferation in the OVA-immunized mice. Platycodin D3 also exerts anti-Hepatitis C virus (HCV) activity.

Furaprofen is an orally available, selective and potent HCV inhibitor with anti-inflammatory activity, inhibits carrageenan-induced paw edema in rats and inhibits cotton pellet-induced granulomas in rats at higher doses.

Pseudane IX (2-nonyl-1H-quinolin-4-one) reduces infection of Huh 7.5 cells by hepatitis C virus (HCV) with an IC50 of 1.4 μg/ml.

Micrococcin P1 is a macrocyclic peptide antibiotic and is a potent hepatitis C virus (HCV) inhibitor(EC50 range of 0.1-0.5 μM)

Ladanein is a phytochemicals inhibitor that is known to disrupt the interactions of core and other hepatitis C virus (HCV) proteins.Ladanein possesses free radicals DPPH and ABTS +.scavenging activity, it also displays moderate (20-40 microM) activities against K562, K562R (imatinib-resistant), and 697 human leukemia cell lines.

gamma-Fagarine possesses moderate levels of anti-HCV activities with IC50 values being 20.4 ± 0.4 ug/ml, respectively. It has sister chromatid exchanges (SCEs)-inducing activity

Sofosbuvir impurity G is a diastereoisomer of Sofosbuvir.Sofosbuvir is an HCV RNA replication inhibitor, with potent anti-hepatitis C virus activity.

2'-O-Methylcytidine is a nucleoside derivative and an inhibitor of hepatitis C virus (HCV) non-structural protein 5B (NS5B; IC50= 3.8 μM).1It inhibits HCV replication in a replicon assay (IC50= 21.2 μM). 1.Migliaccio, G., Tomassini, J.E., Carroll, S.S., et al.Characterization of resistance to non-obligate chain-terminating ribonucleoside analogs that inhibit hepatitis C virus replication in vitroJ. Bio. Chem.278(49)49164-49170(2003)

Glycyrin, one of the main PPAR-gamma ligands of licorice, can significantly decrease the blood glucose levels of genetically diabetic KK-A(y) mice.

Methyl 2-amino-5-bromobenzoate (Methyl 5-Bromoanthranilate) is a hepatitis C virus NS5b RNA polymerase inhibitor with antimicrobial activity that inhibits Pseudomonas aeruginosa infections and is involved in the production of many virulence factors and biofilm formation.

Sennidin A, has two hydroxyanthraquinone-like moieties, exerts inhibition on NS3 helicase with IC50 values of 0.8 μM.

Trachelogenin ((-)-Trachelogenin), isolated from Combretum fruticosum, is an HCV entry inhibitor with anti-proliferative effects. Its mechanism is related to affecting the phosphorylation of key proteins such as β-Catenin, c-Myc and GSK3 in the β-Catenin signaling pathway. chemical and concentration-dependent. Trachelogenin has antiviral, anti-inflammatory and analgesic activities with IC50 of 0.325 and 0.259 μg/mL in HCVcc and HCVpp models, respectively.

Coblopasvir dihydrochloride can be used to study chronic HCV infection and is a pan-genotypic nonstructural protein 5A (NS5A) inhibitor.