hep2

SIBA (5'-Deoxy-5'-isobutylthioadenosine) 是 SAH 的合成类似物，可作为 S-腺苷甲硫氨酸介导的甲基转移的抑制剂。它干扰多种酶活性，可逆地阻断单纯疱疹病毒 1 型病毒的繁殖。

Cyclophosphamide是一种烷化剂类抗肿瘤药物，其主要作用靶点是DNA。环磷酰胺通过与DNA发生烷基化反应，干扰DNA的复制和转录过程，从而抑制肿瘤细胞的增殖。

Remdesivir (GS-5734) 是一种核苷类似物，一种广谱的抗病毒化合物，通过抑制病毒的 RNA 依赖性 RNA 聚合酶发挥活性。Remdesivir 对埃博拉病毒、SARS 病毒、MERS病毒等均有活性，对 COVID-19 有潜在治疗价值。

PC786是一种有效和选择性的的非核苷类RSV L蛋白聚合酶抑制剂，用于吸入治疗RSV感染，对RSV-A（IC50=0.09~0.71 nM）和RSV-B （IC 50=1.3~50.6 nM）具有抗病毒活性, 在HEp-2细胞能够抑制RSV RNA依赖性RNA聚合酶（RdRp）。

Pyrazofurin 是一种嘧啶核苷类似物，通过靶向 UMP synthase 有效抑制细胞增殖和 DNA 合成，同时也是一种高度敏感的 orotate-phosphoribosyltransferase 抑制剂，在 Hep-2、HNSCC-14B 和 HNSCC-14C 细胞系中的 IC50 范围为 0.06–0.37 μM，因此，Pyrazofurin 使研究核苷酸生物合成抑制及抗增殖机制的重要探针。

Biguanidinium-porphyrin free TFA是一种靶向线粒体的光敏剂，对人肝癌HEp2细胞具有较低的暗毒性(IC50=8.2 mM， 1 J/cm-2 )。

EP2 receptor antagonist-3 是一种选择性的 EP2 受体拮抗剂，在 hEP2 SPA 实验中的 IC50 为 8 nM，和在 hEP2 cAMP 实验中的 IC50 为 50 nM。其可增强巨噬细胞对 Amyloid-β 斑块的清除。在 CD-1 小鼠中，该化合物表现出适中的清除率和良好的暴露，并且在小鼠和大鼠中具有良好的中枢神经系统 (CNS) 暴露。EP2 receptor antagonist-3 可用于阿尔茨海默病的研究。

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, parasite level remains stable and then begins dropping[1]. Purfalcamine inhibits proliferation with EC50s of 171-259 nM for P. falciparum strains (3D7, Dd2, FCB, HB3 and W2), which indicates effectiveness against drug-resistant parasites[1]. Given that the EC50 value for P. falciparum (3D7) is 230 nM, Purfalcamine shows a therapeutic window ranging from 23-fold to 36-fold (EC50s for CHO=12.33 μM, HEp2=7.235 μM, HeLa=7.029 μM and Huh7=5.476 μM)[1]. Purfalcamine (10 mg/kg; oral gavage; BID; for 6 days) demonstrates a delay in the onset of parasitemia in treated mice[1]. Purfalcamine (20 mg/kg; orally gavage) exhibits a Cmax of 2.6 μM with a half-life of 3.1 hours[1]. Animal Model: Male BALB/c mice, 7 weeks of age with the malaria parasite[1] [1]. Nobutaka Kato, et al. Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nat Chem Biol. 2008 Jun;4(6):347-56. [2]. Rajshekhar Y Gaji, et al. Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother. 2014 May;58(5):2598-607.

TG8-260作为一种新一代EP2拮抗剂，主要用于减缓炎症驱动的中枢神经系统及外周疾病的病理效应。研究表明，TG8-260可以显著降低匹罗卡品诱发的大鼠持续癫痫状态后海马区的神经炎症及胶质增生。此外，其药代动力学特性表明，TG8-260的血浆半衰期达2.14小时，口服生物利用度为77.3%。TG8-260亦为CYP450的有效抑制剂，能在BV2-hEP2小胶质细胞中抑制EP2受体介导的炎症基因表达，显示出其在外周炎症疾病动物模型中研究抗炎通路的潜在应用价值。

Ivangustin 是从药用植物 Inula britannica 中提取得到的一种倍半萜内酯，对HEp2、SGC-7901和HCT116人癌细胞系表现出显著的细胞毒性。

13(E)-Labd-13-ene-8alpha,15-diol shows antiviral and anticancer activity, it shows strong anti-HRV2 and HRV3 activity with a 50% inhibitory concentration (IC50) of 2.68 and 0.87 microg/mL,respectively; it also exhibits antilung and antilaryngeal cancer ac

Piscidinol A is toxic against the 4T1 and HEp2 cancer cell lines, the IC50 of 8.0 ± 0.03 and 8.4 ± 0.01 uM, respectively. It can inhibit NO production in mouse peritoneal macrophages with inhibitory ratios ranging from 39.8±7.7 to 68.2±4.5%.

4-[2-(3,5-Dimethoxyphenyl)ethyl]phenyl 6-O-(6-deoxy-α-L-mannopyranosyl)-β-D-glucopyranoside showed cytotoxic activities to Hela and hep2 cell lines.