rna polymerase i

Metarrestin (ML246) 是一种口服有效的选择性核仁周区室 (PNC) 抑制剂，可有效抑制转移。Metarrestin 破坏核仁结构并抑制 RNA 聚合酶 (Pol) I 转录，部分是通过与翻译延伸因子 eEF1A2 的相互作用。

Quarfloxin (CX-3543) 是一种氟喹诺酮衍生物，具有抗肿瘤活性，可靶向抑制RNA pol I 的活性，在神经母细胞瘤细胞中的 IC50 值在纳摩尔范围内。它破坏核糖体 DNA 模板中核仁蛋白和 G-四链体 DNA 结构之间的相互作用。

BMH-21 是一种小分子 DNA 嵌入剂，可结合核糖体 DNA 并抑制 RNA 聚合酶 I (Pol I) 转录，具有抗癌活性。

POL1-IN-1 (Compound 3A) 是一种RNA 聚合酶 1 POL1抑制剂，IC50值低于 0.5 uM。 它能有效抑制A375恶性黑色素瘤细胞系中RNA 聚合酶I 的转录。

Antiviral agent 34 是一种可口服且作用效果较强的抗病毒化合物，抑制甲型和乙型流感病毒。Antiviral agent 34 通过调节 RNA 聚合酶来抑制流感病毒的增殖。Antiviral agent 34 可用于研究病毒感染。

ZYN57939 (MTR-106) 是用于治疗 RNA 聚合酶 I 介导的疾病的 RNA 聚合酶 I 抑制剂。 ZYN57939 对人 HT-29 癌细胞系显示出抑制活性，IC50 为 0.855 μM。

RNA polymerase II-IN-2 (compound 20iii)是高效的RNA polymerase II (Pol II)抑制剂，其Ki值为74.1 nM。该化合物对癌细胞展现出细胞毒性，其对CHO和HEK293细胞的毒性分别为α-amanitin的2倍和5倍。

RNA polymerase II-IN-1（compound 19iv）是一款鹅膏毒素类化合物，能够抑制RNA聚合酶II（Pol II），其半抑制浓度IC50为36.66 nM。该化合物相较于α-Amanitin，对癌细胞展现出更高的细胞毒性，而对正常细胞的毒性较低。

Cynaroside (Luteolin 7-O-Glucoside) 是一个抗氧化类黄酮。它还是一种流感依赖 RNA 的RNA 聚合酶抑制剂，IC50为 32 nM。

ML-60218 是广谱 RNA pol III 抑制剂，对酿酒酵母和人类的 IC50 分别为 32 和 27 μM。 ML-60218 会破坏已组装的病毒质并阻碍新病毒质的形成。

RNA polymerase-IN-2 是一种DNA依赖性RNA聚合酶抑制剂，同时抑制CYP同工酶。

RNA polymerase-IN-2 (compound 5) acts as an inhibitor of DNA-dependent RNA polymerase. Additionally, it inhibits CYP isozymes [1].

Azelaic acid (Anchoic acid) 是头发和皮肤调理剂的组分，可由油酸臭氧分解产生。Azelaic acid 通过抑制微生物细胞原蛋白合成对痤疮丙酸杆菌和表皮葡萄球菌具有抑菌活性。Azelaic acid 还具有抑制色素沉着的功能，这是由于其清除自由基作用。

Bakuchiol 是一种从补骨脂种子中提取的植物雌激素，具有抗肿瘤和抗蠕虫特性，以及细胞毒活性和抗菌活性。

BMH-22 is an RNA polymerase I inhibitor that acts by causing nucleolar stress and showing potent anticancer activity across many tumor types.

BMH-23 is an RNA polymerase I inhibitor that acts by causing nucleolar stress and showing potent anticancer activity across many tumor types.

BMH-9 is an RNA polymerase I inhibitor that acts by causing nucleolar stress and showing potent anticancer activity across many tumor types.

Thiocoraline is a depsipeptide and DNAbis-intercalator originally isolated fromMicromonosporawith antibacterial and anticancer activities.1,2It is active against the Gram-positive bacteriaS. aureus,B. subtilis, andM. luteus(MICs = 0.05, 0.05, and 0.03 μg ml, respectively) but not Gram-negativeE. coli,K. pneumoniae, orP. aeruginosa(MICs = >100 μg ml for all).1Thiocoraline inhibits RNA and DNA polymerase and thymidylate synthase (IC50s = 6, 6, and 15 μg ml, respectively), as well as RNA and DNA synthesisin vitro(IC50s = 0.008 and 0.4 μg ml, respectively). It is cytotoxic to P388, A549, HT-29, and MEL-28 cancer cells (IC50s = 0.002, 0.002, 0.01, and 0.002 μg ml, respectively). 1.Romero, F., Espilego, F., Pérez Baz, J., et al.Thiocoraline, a new depsipeptide with antitumor activity produced by a marine Micromonospora. I. Taxonomy, fermentation, isolation, and biological activitiesJ. Antibiot. (Tokyo)50(9)734-737(1997) 2.Negri, A., Marco, E., García-Hernández, V., et al.Antitumor activity, X-ray crystal structure, and DNA binding properties of thiocoraline A, a natural bisintercalating thiodepsipeptideJ. Med. Chem.50(14)3322-3333(2007)

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.

Pol I-IN-1，一种高效的RNA聚合酶I（Pol I）抑制剂，其针对Pol I的大催化亚单RPA194的IC50值为0.21μM。

Pidnarulex HCl is the salt form of CX-5461, a first-in-class non-genotoxic small molecule targeted inhibitor of RNA polymerase I (Pol I) that activates the p53 pathway without causing DNA damage. CX-5461 selectively inhibits rRNA synthesis by Pol I in the nucleolus, but does not inhibit mRNA synthesis by RNA Polymerase II (Pol II) and does not inhibit DNA replication or protein synthesis. Inhibition of Pol I results in nucleolar stress and release of ribosomal proteins (RP) from the nucleolus. The RP bind to Mdm2 and liberate p53 to orchestrate apoptosis in cancer cells. CX-5461 demonstrates a favorable preclinical profile, potently and selectively kills cancer cells, demonstrates robust in vivo efficacy in multiple models, and has demonstrated oral bioavailability in multiple species.