polymerases

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。

Pimodivir (VX-787) 是一种通过口服的甲型流感病毒聚合酶抑制剂，与病毒 PB2 亚基相互作用。

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。

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).

Acyclovir sodium是一种鸟嘌呤核苷类似物和病毒DNA聚合酶抑制剂，具有抗病毒作用，用于治疗皮肤粘膜HSV感染，对HSV-1、HSV-2和VZV具有显著的活性。

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

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。

Tenofovir diphosphate TEA （TFV-DP TEA）是TFV-DP的三乙胺盐，是一种ATP竞争性的DNA聚合酶 (DNA polymerases) 抑制剂，能够抑制HIV-1逆转录酶（HIV-1 reverse transcriptase）。它通过掺入病毒DNA链中，终止病毒DNA的合成，从而抑制病毒基因组的复制，具有抗HIV/HBV的潜力。

1,5-Isoquinolinediol 是一种多聚（ADP-核糖）合成酶抑制剂，对PARP1的IC50值为 0.39 µM。它用于研究 PARP1 在 DNA 修复和氧化应激诱导的细胞死亡中的作用。

PSI-7409 tetrasodium is an active 5'-triphosphate metabolite of sofosbuvir (PSI-7977)(IC50s of 1.6, 2.8, 0.7 and 2.6 μM for GT 1b_Con1, GT 2a_JFH1, GT 3a, and GT 4a NS5B polymerases, respectively).

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).

Lucidenic lactone 是一种萜烯化合物，作为 DNA polymerases 抑制剂。它可抑制小牛 DNA polymerase-α、大鼠 DNA polymerase-β 以及 HIV-1 reverse transcriptase，IC50 分别为 42 μM、99 μM 和 69 μM。

Lucidenic acid O 是一种萜烯化合物，也是一种 DNA 聚合酶 (DNA polymerases) 抑制剂。Lucidenic lactone 可抑制小牛 DNA 聚合酶-α、大鼠 DNA 聚合酶-β 和 HIV-1 逆转录酶 (HIV-1 reverse transcriptase)，其 IC50 值分别为 42 μM、99 μM 和 69 μM。

PARP1-IN-37 (Compound 8) 是一种口服活性且具有选择性的聚 (ADP-核糖) 聚合酶 1 和 2 (PARP1/2) 抑制剂，其对PARP1的IC50为24 nM。在细胞中，PARP1-IN-37 的抑制PARP活性的EC50为3.7 μM。这种化合物有望用于BRCA突变肿瘤的研究，如乳腺癌和卵巢癌。

3′-Deoxy CTP 是一种核苷酸类似物，属于强制链终止剂。它通过缺乏 3′-羟基导致链终止，抑制 HCV 非结构蛋白 (NS5B) 聚合酶的 RNA 合成活性，从而阻断病毒复制。3′-Deoxy CTP 可用于研究 HCV 聚合酶的链终止机制和抗病毒药物的开发。

PMEG-DP disodium 是一种高效的DNA 聚合酶抑制剂 (IC50=2.5 μM)，对DNA 聚合酶 α和δ拥有显著的抑制效能。作为 G-9191 的活性代谢物，PMEG-DP disodium 能有效地抑制乳头状瘤病毒 (HPV) 感染的细胞系生长。该化合物可用于HPV相关疾病研究。

PNU-183792 是一种4-氧代二氢喹啉类化合物，具有口服活性，是疱疹病毒聚合酶（HSV polymerases）的抑制剂。它展示出广谱的抗病毒性能，对人巨细胞病毒（HCM）、水痘带状疱疹病毒和单纯疱疹病毒（HSV）聚合酶的IC50值分别为0.69 μM、0.37 μM和0.58 μM。值得注意的是，PNU-183792 对人类 α、γ 和 δ 聚合酶没有活性，并且还能抑制猴水痘病毒（SVV）、鼠巨细胞病毒（MCMV）和大鼠巨细胞病毒（RCMV）。

4'-Azidothymidine 5'-triphosphate exerts selectively action on both reverse transcriptase of human immunodeficiency virus type 1 and human DNA polymerases alpha and beta.

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].

Carotenoid mixture is a mixture of carotenoids that contains the antioxidative and anti-inflammatory carotenoid capsanthin and the antioxidative vitamin A precursor β-carotene , as well as additional carotenoids and carotenoid esters.1,2,3,4 1.Kim, J.S., Lee, W.M., Rhee, H.C., et al.Red paprika (Capsicum annuum L.) and its main carotenoids, capsanthin and β-carotene, prevent hydrogen peroxide-induced inhibition of gap-junction intercellular communicationChem. Biol. Interact.254146-155(2016) 2.Narisawa, T., Fukaura, Y., Hasebe, M., et al.Prevention of N-methylnitrosourea-induced colon carcinogenesis in rats by oxygenated carotenoid capsanthin and capsanthin-rich paprika juiceProc. Soc. Exp. Biol. Med.224(2)116-122(2000) 3.Horie, S., Okuda, C., T., Y., et al.Purified canola lutein selectively inhibits specific isoforms of mammalian DNA polymerases and reduces inflammatory responseLipids45(8)713-721(2010) 4.Negishi, H., Ueda, Y., and Azuma, M.Antioxidant fat-soluble vitamins and lipid peroxides in serumJ. Clin. Biochem. Nutr.26227-234(1999)

9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supplemented with α-ESA, apoptosis was induced via lipid peroxidation with an EC50 of 20 μM. It also inhibits DNA polymerases and topoisomerases with IC50s ranging from ~5-20 μM for different isoforms of the enzymes. α-ESA ethyl ester is a neutral, more lipid soluble form of the free acid.

Methyl alpha-eleostearate (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supplemented with α-ESA, apoptosis was induced via lipid peroxidation with an EC50 of 20 μM. It also inhibits DNA polymerases and topoisomerases with IC50s ranging from ~5-20 μM for different isoforms of the enzymes. α-ESA methyl ester is a neutral, more lipid soluble form of the free acid.

2'-Deoxyadenosine-5'-triphosphate (dATP) is a purine nucleotide and derivative of the nucleic acid adenosine 5'-triphosphate .1dATP is a substrate for DNA polymerase in the synthesis of DNA.2It is a noncompetitive inhibitor of ribonucleotide reductases, which provides feedback inhibition during DNA synthesis.1dATP has commonly been used in DNA synthesis, sequencing, and labeling in research applications.3,4dATP accumulates in adenosine deaminase deficiency, a disorder characterized by mutations in the gene for adenosine deaminase, the enzyme that catalyzes the deamination of adenosine and deoxyadenosine.5 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Key steps in nucleotide biosynthesis are regulated by feedback inhibitionBiochemistry(2002) 2.Berg, J.M., Tymoczko, J.L., and Stryer, L.DNA is replicated by polymerases that take instructions from templatesBiochemistry(2002) 3.Cadwell, R.C., and Joyce, G.F.Randomization of genes by PCR mutagenesisPCR Methods Appl.2(1)28-33(1992) 4.Steffens, D.L., Jang, G.Y., Sutter, S.L., et al.An infrared fluorescent dATP for labeling DNAGenome Res.5(4)393-399(1995) 5.Flinn, A.M., and Gennery, A.R.Adenosine deaminase deficiency: A reviewOrphanet J. Rare Dis.13(1)65(2018)