名称 | 5-Iodotubercidin |
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. |
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. |
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. |
动物实验 | Animal Models: Male Mongolian gerbilsFormulation: salineDosages: 1, 2.5 and 5 mg/kgAdministration: i.p. |
体外活性 | 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]。 |
体内活性 | 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。 |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 19.6 mg/mL (50 mM)
|
关键字 | 5-Iodotubercidin | Inhibitor | 5Iodotubercidin | NSC113939 | inhibit | 5 Iodotubercidin | ADK | NSC-113939 | Adenosine Kinase |
相关产品 | Theophylline | Theobromine | Doxofylline |
相关库 | 抑制剂库 | 经典已知活性库 | 激酶抑制剂库 | 抗病毒库 | GPCR靶点分子库 | 神经退行性疾病化合物库 | 膜蛋白靶向化合物库 | 酪氨酸激酶分子库 |