逆转素 T1825

Product Introduction
Bioactivity


英文名: Reversine

描述: Reversine 是一种 ATP-竞争性 Aurora kinase 抑制剂，作用于Aurora A、Aurora B 和Aurora C，IC50分别为 400、500 和 400 nM。

细胞实验: Cell viability of different tumor cell lines is assessed using ATPlite 1step. Briefly, 2 × 104?cells for each well are plated in a 96-well plate in presence of crescent quantity of reversine. After 72 h, the plates are recovered and 100 μL ATPlite solution is added to each well. The plates are shaken for 2 min at 700 rpm and luminescence is measured using EnVision Multilabel plate reader. Each sample is analyzed in triplicate.(Only for Reference)

激酶实验: Radioligand Binding Assays: Each tube in the A3 AR competitive binding assay contains 100 μL of membrane suspension (20 μg of protein), 50 μL of [125I]4-amino-3-iodobenzyl)adenosine-5′-N-methyluronamide (0.5 nM), and 50 μL of increasing concentrations of the test ligands in Tris-HCl buffer (50 mM, pH 7.4) containing 10 mM MgCl2 and 1 mM EDTA. Nonspecific binding is determined using 10 mM 5′-N-ethylcarboxamidoadenosine in the buffer. The mixtures are incubated at 25°C for 60 min. Binding reactions are terminated by filtration through Whatman GF/B filters under reduced pressure using a MT-24 cell harvester. Filters are washed three times with 9 mL of ice-cold buffer. Radioactivity is determined using a Beckman γ-counter, and the percent inhibition is calculated.

体外活性: 在携带U14肿瘤的小鼠体内,腹腔注射Reversine（10 mg/kg）能够消退肿瘤细胞.

体内活性: 在稳定转染的中国仓鼠卵巢细胞中,Reversine能够竞争性抑制毛喉素刺激的cAMP产生。在HCT116细胞中,Reversine抑制Aurora靶点,及组蛋白H3的磷酸化。在原代人肿瘤样品中,Reversine能够抑制白血病细胞集落的形成。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 5 mg/mL (12.71 mM)


关键字: inhibit | Inhibitor | Reversine | Autophagy | Aurora Kinase

相关产品: TAK-285 | TCS7010 | MBM-55 | MLN8054 | Ilorasertib hydrochloride | Aurora Kinases-IN-4 | GW779439X | MBM-55S | Hesperadin | ZM-447439

相关库: Anti-Aging Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | GPCR Compound Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library

逆转素 T1825信息由TargetMol中国为您提供，如您想了解更多关于逆转素 T1825报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途