HCV Inhibitor

Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC₅₀ of 9 μM.

RS47 is a selective RelB inhibitor with a Kd value of 1.1 μM. RS47 also acts as an inhibitor of HCV replication. RS47 can block the non-canonical NF-κB signaling pathway without affecting the canonical pathway. RS47 exerts anti-tumor effects of inhibiting proliferation and promoting apoptosis on colorectal cancer, B-cell lymphoma and other related tumors both in vitro and in vivo by disrupting the binding of RelB to target DNA. RS47 can be used for the research of tumors and infectious diseases.

Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC₅₀s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC₅₀s of 1.5 μM and 3.27 μM, respectively.

IMAB027 (ASP1650) is a specific anti-CLDN6 mAb, while CLDN6 (Claudin 6) is a tight junction membrane protein, aberrantly expressed in various human cancer types, ovarian cancers particularly. IMAB 027 shows anti-tumor activity, and induces apoptosis in CLDN6⁺ ovarian and testicular cancer cell lines.

Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC₅₀s ranging from 0.03 to 6.92 nM) and HIV-2 (EC₅₀s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains. Azvudine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC₅₀ values of 34 pM against GT1a and 4 pM against GT1b replicon.

Bemnifosbuvir (AT-511) is a potent and orally active HCV viral replication inhibitor. Bemnifosbuvir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₉₀=0.47 μM). Bemnifosbuvir has pangenotypic antiviral activity.

Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a K_i of 14 nM in both enzyme assay and an EC₉₀ of 350 nM in cell-based replicon assay. Boceprevir inhibits SARS-CoV-2 3CL^pro activity.

Saikosaponin B2 is an antiviral and anticancer agent that regulates multiple transporters (such as various solute carriers and ATP-binding cassette transporters including MRP1, MRP2, and OCT2). Saikosaponin B2 is isolated from the plant glycoside component of the roots of Bupleurum scorzonerifolium. Saikosaponin B2 enhances the liver targeting of anticancer drugs via vinegar-baked Radix Bupleuri. Saikosaponin B2 inhibits HCV entry, replication, and translation, is effective against Daclatasvir (HY-10466)-resistant strains, and exerts a synergistic effect when used in combination with Daclatasvir. Saikosaponin B2 is commonly used in studies related to hepatocellular carcinoma and HCV infection.

NM107 (2'-C-Methylcytidine) is an nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase, the EC₅₀ of NM107 in the wild-type replicon cells is 1.85 μM.

Oenothein B is a dimeric macrocyclic ellagitannin and has widely pharmacological activities, including antioxidant, anti-inflammatory, antifungal, anti-HCV, and antitumor properties. Oenothein B is a potent and specific inhibitor of poly(ADP-ribose) glycohydrolase.

Platycodin D3 is a triterpenoid saponin that can be found in Platycodon grandiflorum. Platycodin D3 exhibits multiple activities including anti-inflammation, regulation of airway mucus secretion, improvement of asthmatic airway inflammation and remodeling, and inhibition of hepatitis C virus (HCV) replication. The IC₅₀ value of Platycodin D3 against HCV NS5B RNA-dependent RNA polymerase is 8 μg/mL. Platycodin D3 can be used in studies related to asthma, hepatitis C virus infection and inflammatory diseases.

Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus. Oglufanide inhibits vascular endothelial growth factor (VEGF). Oglufanide can stimulate the immune response to hepatitic C virus (HCV) and intracellular bacterial infections. Oglufanide shows antitumor and anti-angiogenesis activities.

Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC₅₀ of < 28 nM.

Bemnifosbuvir hemisulfate (AT-527), a hemisulfate salt of AT-511, a guanosine nucleotide proagent, is a potent and orally active HCV viral replication inhibitor. Bemnifosbuvir hemisulfate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₉₀=0.47 μM). Bemnifosbuvir hemisulfate has pangenotypic antiviral activity.

NHC-triphosphate tetraammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a triphosphate form. NHC-triphosphate tetraammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.

Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC₅₀s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.

DDX3-IN-1 (Compound 16f) is the inhibitor for DEAD box polypeptide 3 (DDX3) with an IC₅₀ >100 μM. DDX3-IN-1 exhibits antiviral activity against HIV and HCV.

Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC₅₀s ranging from 0.03 to 6.92 nM) and HIV-2 (EC₅₀s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains. Azvudine (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

2'-C-Methyladenosine is an inhibitor of hepatitis C virus (HCV) replication. 2'-C-Methyladenosine inhibits HCV replicon and NS5B-catalyzed RNA synthesis with IC₅₀ values of 0.3μM and 1.9 μM, respectively. 2'-C-Methyladenosine also potently inhibits LRV1 in Leishmania guyanensis (Lgy) and Leishmania braziliensis.