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5-Iodotubercidin

产品编号 T6745 CAS 24386-93-4

别名: 5-碘代杀结核菌素, 5-ITu, NSC 113939

5-Iodotubercidin (NSC-113939) 是一种 ATP 类似物，有效抑制腺苷激酶，IC50为 26 nM。它可以激活磷酸化酶和糖原合成酶，在离体肝细胞中启动糖原合成。它也抑制 CK1、胰岛素受体酪氨酸激酶、磷酸化酶激酶、PKA、CK2、PKC 和 Haspin 。

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5-Iodotubercidin, CAS 24386-93-4

规格	价格/CNY	货期
1 mg	￥ 315	现货
2 mg	￥ 447	现货
5 mg	￥ 715	现货
10 mg	￥ 1,210	现货
25 mg	￥ 2,790	现货
50 mg	￥ 4,150	现货
100 mg	￥ 5,920	现货
1 mL * 10 mM (in DMSO)	￥ 658	现货

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纯度: 99.98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	5-Iodotubercidin (NSC-113939) is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.
靶点活性	Adenosine kinase:NA
体外活性	5-Iodotubercidin(Itu) is a genotoxic drug that activates the Atm-p53 pathway and has anti-tumor activity. Itu is unique compared to other nucleoside analogs in the way that it induces G2 arrest in a p53 -dependent manner. Moreover, at higher doses, Itu might activate p53-independent pathways, which may cooperate with p53 to kill cells and inhibit tumor growth. Incorporation of Itu metabolite into DNA causes DNA breaks, which triggers the DNA damage response. Itu might be a potential chemotherapeutic drug with distinct working mechanisms[2].
体内活性	5-Iodotubercidin is a potent inhibitor of adenosine kinase in the rat brain. 5-iodotubercidin has potent hypotensive, muscle relaxant, and hypothermic actions in mice, and that these effects could be blocked by theophylline, an adenosine receptor antagonist. 5-iodotubercidin (1 mg/kg, i.p.) administered prior to an ischemic episode, fails to provide a degree of cerebroprotection, assessed either by locomotor or histopathological indices Even though 5-iodotubercidin administration is known to enhance extracellular adenosine levels in brain slices[1].
激酶实验	AK activity is measured in a radiochemical assay. The final reaction volume is 100 μL and contained 70 mM Tris-maleate (pH 7.0), 0.1% (w/v) bovine serum albumin, 1.0 mM MgCl2, 1.0 mM ATP, 1.0 μM [U-14C]adenosine (400-600 mCi/mmol) and various inhibitor concentrations. Inhibitors are prepared as 10 mM stock solutions in DMSO. The final DMSO concentration in the assay is 5% (v/v). Eleven different concentration of the test solutions ranging from 0.001 to 10.0 μM are utilized to determine a dose response curve of the inhibition of the enzyme. Reactions are started by adding the appropriate amount of purified human recombinant AK and incubated for 20 min at 37°C. The reactions are terminated by addition of the potent AKI GP3269. A 30-μL aliquot of each reaction is spotted on DEAE cellulose filter paper (cut in squares of appr 1×1 cm) and air-dried for 30 min. The dry filters are then washed for 3 min in deionized water to remove residual [U-14C]adenosine, rinsed with ethanol and dried at 90°C for 20 min. The filter papers are counted in 5.5 mL of Ready Safe liquid scintillation cocktail using a Beckman LS3801 scintillation counter. Control AK activity is determined from the amount of [14C]AMP formed in the presence of 5% DMSO. The concentration of inhibitor required to inhibit 50% of the AK activity (IC50) is determined graphically from plots of inhibitor concentration versus percent (%) control enzyme activity.
细胞实验	HeLa cells are grown in DME supplemented with 10% fetal bovine serum (FBS) and 2 mM?l-glutamine. Nocodazole is used at a concentration of 3.3 μM unless differently specified. Thymidine (2.5 mM) is used in the asssay. For transfection, FuGENE 6 Transfection Agent is used at a 3:1 ratio with plasmid DNA. Cells are analyzed 24-48 h after transfection.
动物实验	Animal Models: Male Mongolian gerbilsFormulation: salineDosages: 1, 2.5 and 5 mg/kgAdministration: i.p.

别名	5-碘代杀结核菌素, 5-ITu, NSC 113939
分子量	392.15
分子式	C11H13IN4O4
CAS No.	24386-93-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 19.6 mg/mL (50 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.55 mL	12.7502 mL	25.5004 mL	63.7511 mL
	5 mM	0.51 mL	2.55 mL	5.1001 mL	12.7502 mL
	10 mM	0.255 mL	1.275 mL	2.55 mL	6.3751 mL
	20 mM	0.1275 mL	0.6375 mL	1.275 mL	3.1876 mL
	50 mM	0.051 mL	0.255 mL	0.51 mL	1.275 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Phillis JW, et al. Life Sci. 1993, 53(6):497-502. 2. Zhang X, et al. PLoS One. 2013, 8(5):e62527.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

5-Iodotubercidin 24386-93-4 GPCR/G Protein Neuroscience Adenosine Receptor Inhibitor 5Iodotubercidin NSC113939 inhibit 5 Iodotubercidin 5-碘代杀结核菌素 ADK NSC-113939 Adenosine Kinase 5-ITu NSC 113939 inhibitor

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5-Iodotubercidin

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords