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.

Adenosine kinase:NA

5-Iodotubercidin（Itu）是一种具有抗肿瘤活性的基因毒性药物，能够激活Atm-p53途径。与其他核苷类似物相比，Itu独特之处在于它以p53依赖的方式诱导G2阶段阻滞。此外，在较高剂量下，Itu可能激活p53独立途径，这可能与p53合作，杀死细胞并抑制肿瘤生长。Itu代谢产物整合到DNA中会导致DNA断裂，从而触发DNA损伤响应。Itu可能是一种具有独特作用机制的潜在化疗化合物[2]。

5-Iodotubercidin是一种在大鼠大脑中强效的腺苷激酶抑制剂。该化合物在小鼠中表现出显著的降血压、肌肉松弛及降低体温作用，这些效果可被茶碱（一种腺苷受体拮抗剂）阻断。尽管已知5-Iodotubercidin (1 mg/kg, i.p.)在缺血发作前使用可以增强脑片段中的细胞外腺苷水平，但其在通过运动或组织病理学指标评估时，未能提供任何脑保护作用。

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.

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.

Animal Models: Male Mongolian gerbilsFormulation: salineDosages: 1, 2.5 and 5 mg/kgAdministration: i.p.