rna-polymerases

Remdesivir triphosphate 是一种有效的病毒 RNA 依赖的 RNA 聚合酶抑制剂，对RSVRdRp 和 HCVRdRp 的IC50分别为 1.1 µM 和 5 µM。它是 Remdesivir 的活性三磷酸代谢物。

Tubercidin (Sparsomycin A) 是从Streptomyces tubercidicus 得到的抗生素，抑制粪链球菌生长的IC50值为 0.02 μM。它是腺苷磷酸化酶的弱抑制剂，并干扰腺苷和 AMP 的磷酸化。它有抗病毒作用。

GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC 50 s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734).

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'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM[1]. 3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is synthesized starting from cordycepin in good yield. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA by the RNA polymerases. 3'-Deoxyuridine-5'-triphosphate will be useful in studies at the molecular level on the relationship of template and substrate in RNA synthesis with chromatin, isolated nuclei or permeable cells, because it does not have any effect on poly (rA) synthesis[1]. [1]. M Saneyoshi, et al. Inhibitory Effects of 3'deoxycytidine 5'-triphosphate and 3'-deoxyuridine 5'-triphosphate on DNA-dependent RNA Polymerases I and II Purified From Dictyostelium Discoideum Cells. Nucleic Acids Res. 1981 Jul 10;9(13):3129-38.

3'-Deoxyuridine-5'-triphosphate trisodium (3'-dUTP trisodium) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II. 3'-Deoxyuridine-5'-triphosphate trisodium strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM[1]. 3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is synthesized starting from cordycepin in good yield. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA by the RNA polymerases. 3'-Deoxyuridine-5'-triphosphate will be useful in studies at the molecular level on the relationship of template and substrate in RNA synthesis with chromatin, isolated nuclei or permeable cells, because it does not have any effect on poly (rA) synthesis[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)

Juglone (Regianin) 是一种从黑胡桃Juglans regia 中发现的黄色染料，有抗菌作用。

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 是一种氧化性 DNA 损伤的产物，能够增强或抑制细菌 RNA 聚合酶转录的潜在表观遗传标记。

XSJ2-46，一种5'-氨基NI类似物，表现为有效的抗病毒药物，尤其针对Zika病毒。它通过抑制RNA依赖性RNA聚合酶（RdRp），展示出其活性，具有8.78 μM的IC50值。

BCH001 是喹啉衍生物，是一种选择性PAPD5抑制剂。它可以恢复先天性角化病诱导的多能干细胞中的端粒酶活性和端粒长度。它对聚 (A)-特异性核糖核酸酶或几种其他多核苷酸聚合酶均无抑制作用。它可用于调控衰老。

HeE1-2Tyr 是 一种pyridobenzothiazole，抑制黄病毒 RNA 依赖性 RNA 聚合酶。HeE1-2Tyr 在体外对Dengue, West Nile 和 SARS-CoV-2 RdRps 有显著的抑制活性(IC50为 27.6 µM) 。

Tsugaric acid A 能够显著抑制超氧阴离子的形成，还可以保护人类角质形成细胞，使其免受紫外线 B 诱导的损害。

Aphidicolin 17-acetate 是一种专一性抑制真核 DNA 聚合酶 α (DNA polymerase α) 的化合物。它对 DNA 聚合酶 β 和 γ 无影响。Aphidicolin 17-acetate 显著抑制海胆胚胎和 HeLa 细胞体内的 DNA 合成，但不影响 RNA 和蛋白质合成。