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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 392.15. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.55 mL||12.75 mL||25.5 mL|
|5 mM||0.51 mL||2.55 mL||5.1 mL|
|10 mM||0.26 mL||1.28 mL||2.55 mL|
|50 mM||0.05 mL||0.26 mL||0.51 mL|
References are publications that support the products' biological activity.
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.
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6 Citations for 5-Iodotubercidin
Citations are publications that use Tocris products. Selected citations for 5-Iodotubercidin include:
Prakasam et al (2012) Modulation of bladder function by luminal adenosine turnover and A1 receptor activation. J Neurosci 303 F279 PMID: 22552934
Fassett et al (2011) Adenosine kinase regulation of cardiomyocyte hypertrophy. Am J Physiol Heart Circ Physiol 300 H1722 PMID: 21335462
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
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
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
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
Do you know of a great paper that uses 5-Iodotubercidin from Tocris? If so please let us know.
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