Tubercidin
别名: 7-deaza-adenosine 中文名称：杀结核菌素
Tubercidin (7-deaza-adenosine)，腺苷类似物，是一种核苷抗生素。它可掺入到DNA中，抑制聚合酶，因此抑制DNA复制和RNA、蛋白合成。Tubercidin还具有抗真菌和抗病毒活性。
Tubercidin Chemical Structure
CAS: 69-33-0
客户使用Selleck的发表文献1篇
产品质控
Tubercidin相关产品
| 相关靶点 | tRNA synthetase RdRp DNA synthesis helicase ribonucleotide reductase | 点击展开 |
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| 相关化合物库 | FDA药物库 天然产物库 凋亡分子化合物库 DNA损伤/ DNA修复化合物库 细胞周期化合物库 | 点击展开 |
相关信号通路图
DNA/RNA Synthesis抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| L2 | Growth inhibition assay | 37 uM | Growth inhibition of mouse L2 cells at 37 uM | 17977728 | |
| HeLaS3 | Antiviral assay | 2 days | Antiviral activity against Poliovirus infected in human HeLaS3 cells assessed as inhibition of viral replication treated 1 hr before infection measured after 2 days, IC50=0.03μM | 20964406 | |
| HeLaS3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLaS3 cells after 48 hrs by celltiter-glo assay, IC50=0.4μM | 20964406 | |
| HeLaS3 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HeLaS3 cells after 24 hrs by celltiter-glo assay, IC50=0.819μM | 20964406 | |
| HeLaS3 | Cytotoxicity assay | 7 hrs | Cytotoxicity against human HeLaS3 cells after 7 hrs by celltiter-glo assay, IC50=1.44μM | 20964406 | |
| A549 | Cytostatic assay | 5 days | Cytostatic activity against human A549 cells after 5 days by SRB assay, GI50=0.001μM | 21711054 | |
| HCT116 | Cytostatic assay | 5 days | Cytostatic activity against human HCT116 cells after 5 days by SRB assay, GI50=0.001μM | 21711054 | |
| NCI-H23 | Cytostatic assay | 5 days | Cytostatic activity against human NCI-H23 cells after 5 days by SRB assay, GI50=0.011μM | 21711054 | |
| HCT15 | Cytostatic assay | 5 days | Cytostatic activity against human HCT15 cells after 5 days by SRB assay, GI50=0.011μM | 21711054 | |
| DU145 | Cytostatic assay | 5 days | Cytostatic activity against human DU145 cells after 5 days by SRB assay, GI50=0.018μM | 21711054 | |
| MT4 | Cytostatic assay | 5 days | Cytostatic activity against human MT4 cells after 5 days by SRB assay, GI50=0.021μM | 21711054 | |
| PC3 | Cytostatic assay | 5 days | Cytostatic activity against human PC3 cells after 5 days by SRB assay, GI50=0.048μM | 21711054 | |
| Hs578 | Cytostatic assay | 5 days | Cytostatic activity against human Hs578 cells after 5 days by SRB assay, GI50=0.098μM | 21711054 | |
| MRC5 | Antitrypanosomal assay | 7 days | Antitrypanosomal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 harboring beta-galactosidase infected in human MRC5 cells after 7 days by resazurin dye-based assay, EC50=0.34μM | 30677668 | |
| MRC5 | Cytotoxicity assay | 3 days | Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 3 days by resazurin dye-based assay, EC50=2.23μM | 30677668 | |
| Vero | Function assay | 5 days | Inhibition of RNA-dependent RNA polymerase in Zika virus MR766 infected in African green monkey Vero cells assessed as antiviral activity by measuring reduction in virus-induced cytopathic effect after 5 days by MTS assay, EC50=1.3μM | 31549836 | |
| L1210 | Function assay | Concentration required to decrease the growth rate to 50% of control was evaluated by determining their ability to inhibit growth of L1210 cells in vitro, IC50=0.04μM | 1310744 | ||
| H.Ep.2 | Function assay | Concentration required to decrease the growth rate to 50% of control was evaluated by determining their ability to inhibit growth of H.Ep.2 cells in vitro, IC50=0.06μM | 1310744 | ||
| HFF cells | Cytotoxicity assay | Cytotoxicity against uninfected human foreskin fibroblast(HFF cells), IC50=0.4μM | 2846837 | ||
| KB cells | Cytotoxicity assay | Cytotoxicity against human neoplastic cell line(KB cells), IC50=0.6μM | 2846837 | ||
| L1210 | Cytotoxicity assay | In vitro cytotoxicity was evaluated against the L1210 Murine leukemic cells, IC50=0.04μM | 2913300 | ||
| HFF cells | Cytotoxicity assay | Cytotoxicity was evaluated against the Human diploid cells (HFF), IC50=0.3μM | 2913300 | ||
| H.Ep.2 | Function assay | Compound was evaluated for cytotoxicity against H.Ep.-2 cells, and concentration required to inhibit the growth of treated cells to 50% of untreated control. , IC50=0.002μM | 6708054 | ||
| L1210 | Function assay | Tested for in vitro cell growth inhibition of L1210 cells, IC50=0.043μM | 8254613 | ||
| H.Ep.2 | Function assay | Tested for in vitro cell growth inhibition of H. Ep. 2 cells, IC50=0.06μM | 8254613 | ||
| HEK293 | Function assay | Stabilization of Pdcd4 expressed in human HEK293 cells assessed as inhibition of TPA-induced degradation by luciferase reporter assay, IC50=0.88μM | 21870828 | ||
| Vero | Function assay | Inhibition of RNA-dependent RNA polymerase in Zika virus MR766 infected in African green monkey Vero cells assessed as antiviral activity by methylene blue staining based by Plaque reduction assay, EC50=1.3μM | 31549836 | ||
| Vero | Function assay | Inhibition of RNA-dependent RNA polymerase in Zika virus MR766 infected in African green monkey Vero cells assessed as antiviral activity by Alexa Fluor 488/DAPI staining based assay, EC50=1.3μM | 31549836 | ||
| Vero | Function assay | Inhibition of RNA-dependent RNA polymerase in Zika virus MR766 infected in African green monkey Vero cells assessed as antiviral activity by measuring reduction in virus-yield, EC50=1.3μM | 31549836 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Tubercidin (7-deaza-adenosine)，腺苷类似物，是一种核苷抗生素。它可掺入到DNA中，抑制聚合酶，因此抑制DNA复制和RNA、蛋白合成。Tubercidin还具有抗真菌和抗病毒活性。 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 连续14天的tubercidin处理对CFU-GM和BFU-E都具有高度毒性作用。在CFU-GM和BFU-E中，tubercidin的IC50分别为3.4±1.7和3.7±0.2 nM。在体外实验中，Tubercidin对髓系和红系人源骨髓组细胞具有浓度依赖式的抑制作用[1]。 | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | 人骨髓细胞 | ||
| 浓度 | 10 nM | |||
| 孵育时间 | 14天 | |||
| 方法 | 从健康人体中获得并分离出人源骨髓细胞。用10 nM tubercidin处理这些细胞，加入（或不加入）不同浓度的NBMPR-P。将细胞这样连续处理14天（37℃，5% C02-95% air）。在倒置显微镜下对CFU-GM和BFU-E进行计数。 | |||
| 体内研究(In Vivo) | ||
| 体内研究活性 | 连续4天，每天向小鼠注射5mg/kg的tubercidin将使小鼠死亡。一些研究表明，tubercidin所导致的死亡可能是由于其对肝脏和肾脏的损害，或者极小可能是对胰脏的损伤。将tubercidin和NBMPR-P共注射可保护小鼠免于死亡[1]。 | |
|---|---|---|
| 动物实验 | Animal Models | CD1小鼠 |
| Dosages | 5 mg/kg | |
| Administration | 腹腔注射 | |
化学信息&溶解度
| 分子量 | 266.25 | 分子式 | C11H14N4O4 |
| CAS号 | 69-33-0 | SDF | Download Tubercidin SDF |
| Smiles | C1=CN(C2=NC=NC(=C21)N)C3C(C(C(O3)CO)O)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 53 mg/mL ( (199.06 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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