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Submit Review5-Iodotubercidin is a potent adenosine kinase inhibitor (IC50 = 26 nM). Also nucleoside transporter inhibitor (IC50 values are < 25 nM, 7 μM and 15 μM for inhibition of [3H]adenosine, [3H]uridine and [3H]formycin B uptake respectively). Strongly stimulates glycogen synthesis in hepatocytes via activation of glycogen synthase. Also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC (IC50 values are 0.4, 3.5, 5-10, 5-10, 10.9 and 27.7 μM respectively). Decreases hippocampal DNA methylation through adenosine kinase inhibition in vivo.
分子量 | 392.15 |
公式 | C11H13IN4O4 |
储存 | Store at -20°C |
纯度 | ≥97% (HPLC) |
CAS Number | 24386-93-4 |
PubChem ID | 97297 |
InChI Key | WHSIXKUPQCKWBY-IOSLPCCCSA-N |
Smiles | O[C@H]([C@H](O)[C@@H](CO)O3)[C@@H]3N1C2=C(C(N)=NC=N2)C(I)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 19.61 | 50 |
以下数据基于产品分子量 392.15。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 5.1 mL | 25.5 mL | 51 mL |
2.5 mM | 1.02 mL | 5.1 mL | 10.2 mL |
5 mM | 0.51 mL | 2.55 mL | 5.1 mL |
25 mM | 0.1 mL | 0.51 mL | 1.02 mL |
参考文献是支持产品生物活性的出版物。
Massillon et al (1994) Identification of the glycogenic compound 5-iodotubercidin as a general protein kinase inhibitor. Biochem.J. 299 123 PMID: 8166629
Parkinson and Geiger (1996) Effects of iodotubercidin on adenosine kinase activity and nucleoside transport in DDT1 MF-2 smooth muscle cells. J.Pharmacol.Exp.Ther. 277 1397 PMID: 8667202
Ugarkar et al (2000) Adenosine kinase inhibitors. 1. Synthesis, enzyme inhibition, and antiseizure activity of 5-iodotubercidin analogues. J.Med.Chem. 43 2883 PMID: 10956196
Williams-Karnesky et al (2013) Epigenetic changes induced by adenosine augmentation therapy prevent epileptogenesis. J.Clin.Invest. 123 3552 PMID: 23863710
If you know of a relevant reference for 5-Iodotubercidin, please let us know.
关键词: 5-Iodotubercidin, 5-Iodotubercidin supplier, Potent, adenosines, kinase, inhibitors, nucleoside, transporters, ENT1, reuptake, Purine, Transporters, Pyrimidine, Equilibrative, Monoamine, Neurotransmitter, ADK, 5-it, inhibits, DNA, methylation, Adenosine, Kinase, Broad, Spectrum, Protein, Inhibitors, Nucleoside, Other, Methyltransferases, 1745, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 5-Iodotubercidin 的部分引用包括:
Bumpus and Johnson (2011) 5-Aminoimidazole-4-carboxyamide-ribonucleoside (AICAR)-stimulated hepatic expression of Cyp4a10, Cyp4a14, Cyp4a31, and other peroxisome proliferator-activated receptor α-responsive mouse genes is AICAR 5'-monophosphate-dependent and AMP-activated Cell Death Dis 339 886 PMID: 21896918
Fassett et al (2011) Adenosine kinase regulation of cardiomyocyte hypertrophy. Am J Physiol Heart Circ Physiol 300 H1722 PMID: 21335462
Rüben et al (2015) Selectivity Profiling and Biological Activity of Novel β-Carbolines as Potent and Selective DYRK1 Kinase Inhibitors. PLoS One 10 e0132453 PMID: 26192590
Visentin et al (2012) Augmentation of reduced folate carrier-mediated folate/antifolate transport through an antiport mechanism with 5-aminoimidazole-4-carboxamide riboside monophosphate. Mol Pharmacol 82 209 PMID: 22554803
Baron et al (2015) The NLRP3 inflammasome is activated by nanoparticles through ATP, ADP and adenosine. Am J Physiol Renal Physiol 6 e1629 PMID: 25654762
Prakasam et al (2012) Modulation of bladder function by luminal adenosine turnover and A1 receptor activation. J Neurosci 303 F279 PMID: 22552934
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