rna-polymerases

GS-441524 was shown to be a safe and effective treatment for feline infectious peritonitis (FIP). The optimum dosage was found to be 4.0 mg/kg SC q24h for at least 12 weeks

GS-443902 trisodium (GS-441524 triphosphate trisodium), the active triphosphate metabolite of Remdesivir (GS-5734), serves as a potent inhibitor of viral RNA-dependent RNA-polymerases (RdRp), displaying inhibitory concentrations (IC50) of 1.1 μM for RSV RdRp and 5 μM for HCV RdRp.

Juglone (Regianin) is a natural naphthoquinone found in the black walnut (J. nigra) and other plants in the Juglandaceae family. Juglone also irreversibly inhibits peptidyl-prolyl cis/trans isomerases of the parvulin family, including human Pin1, yeast Ess1/Ptf1, and E. coli parvulin (Ki = 55.9 nM). Juglone also blocks transcription by RNA polymerases I, II, and III (IC50s = 2-7 μM) and attenuates kidney fibrosis in rats treated with unilateral ureteral obstruction, both through Pin1-independent mechanisms.

Tubercidin (Sparsomycin A), an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.

Streptolydigin inhibits RNA synthesis by binding to RNA polymerase and does not inhibit eukaryotic RNA polymerases. Streptolydigin is a 3-acetyltetramic acid antibiotic and a potent bacterial RNA polymerase inhibitor (Ki: 18 μM and a Kd: 15 μM).

3′-Deoxy CTP is a nucleotide analog that functions as a potent chain terminator. By lacking a 3′-hydroxyl group, 3′-Deoxy CTP induces chain termination, thereby inhibiting the RNA synthesis activity of HCV non-structural protein (NS5B) polymerase and halting viral replication. This compound is useful for studying the chain termination mechanism of HCV polymerases and for developing antiviral drugs.

3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II and strongly competes with UTP incorporation into RNA, with a Ki value of 2.0 μM[1].

'3'-Deoxyuridine-5'-triphosphate trisodium (3'-dUTP trisodium) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II by competitively blocking UTP incorporation into RNA with a dissociation constant (Ki) of 2.0 μM[1].

Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers. 1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980)

Thio-ITP, also known as 6-Thioinosine 5'-triphosphate, is a competitive inhibitor of RNA polymerase activity. It exhibits a strong apparent affinity towards the polymerases, with Ki values of 40.9 μM for RNA polymerase I and 38.0 μM for RNA polymerase II.

5-(Hydroxymethyl)uracil is a product of oxidative DNA damage and is capable of enhancing or inhibiting potential epigenetic markers for transcription by bacterial RNA polymerases.

XSJ2-46, a 5'-amino NI analog, is an antiviral agent possessing anti-Zika virus properties and demonstrates reasonable inhibition of RNA-dependent RNA polymerases (RdRp), with an IC50 of 8.78 μM [1].

BCH001 is a specific small-molecule inhibitor of PAPD5.

HeE1-2Tyr, a pyridobenzothiazole compound, is a potent inhibitor of flavivirus RNA-dependent RNA polymerases (RdRp). It significantly inhibits the RdRp activity of West Nile, Dengue, and SARS-CoV-2 in vitro, with an IC50 of 27.6 µM.

Ribavirin-13C5 (Standard) is the standard form of Ribavirin-13C5, suitable for quantitative analysis, quality control, and related research in biochemical experiments. Ribavirin-13C5 is intended to be used as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog. 1,2 Once it enters cells, ribavirin is metabolized into an active triphosphate form that causes viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml). 3 Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50 = 109.5 μM). 4 Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers.

Tsugaric acid A significantly inhibits superoxide anion formation in fMLP/CB-stimulated rat neutrophils and protects human keratinocytes against damage induced by ultraviolet B (UV B) light, indicating that tsugaric acid A can safeguard keratinocytes from photodamage.

Aphidicolin 17-acetate is a selective inhibitor of eukaryotic DNA polymerase α (DNA polymeraseα) that does not inhibit DNA polymerases β and γ. It significantly suppresses DNA synthesis in sea urchin embryos and HeLa cells in vivo without affecting RNA and protein synthesis.