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5-Iodotubercidin
Cat No.
CEI-1192
Description
5-Iodotubercidin is a potent inhibitor of adenosine kinase.
Product Overview
5-Iodotubercidin (Itu) is a purine derivative and hence an inhibitor of adenosine kinase with an IC50 value of 26 nM. Adenosine kinase is important in regulating the intracellular and extracellular concentrations of adenosine and hence diverse physiological actions of adenosine. In various cells such as cancer cells, persisted AMPK activation could result in apoptosis. In nude mice with colon carcinoma xenograft, Itu at a dose of 2.5 mg/kg resulted in rapid tumor regression compared with the control group. At the dose of 0.625 mg/kg, Itu still inhibited tumor growth, but p53-/-tumors were resistant to Itu at this lowered dose. In male Wistar rat hepatocytes, incubation with Itu resulted in concentrations of AMP and ATP at 0.39 ± 0.06 and 1.51 ± 0.10 μmol/g cell wet mass, respectively; while control incubation at 0.27 ± 0.05 and 2.25 ± 0.33 μmol/g cell wet mass, respectively. Addition of 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) and Itu simultaneously resulted in almost the same effect of Itu alone. It was probable that Itu inhibited adenosine kinase and blocked the synthesis of 5-aminoimidazole-4-carboxamide ribonucleotide (ZMP) from AICAR. ZAM is a structural AMP analogue and hence mimics the effect of AMP on the AMP-activated protein kinase (AMPK) activation.
CAS No.
24386-93-4
Molecular Weight
392.15
Purity
0.9826
Storage
Store at -20°C
Synonyms
NSC 113939; 5-ITu
Targets
Adenosine kinase
IC50
26 nM; 7 μM; 15 μM
Molecular Formula
C11H13IN4O4
Chemical Name
(2R,3R,4S,5R)-2-(4-amino-5-iodopyrrolo[2,3-d]pyrimidin-7-yl)-5-(hydroxymethyl)oxolane-3,4-diol
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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