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BIX 02565

BIX 02565

产品编号 T5428   CAS 1311367-27-7

BIX 02565 是核糖体 S6 激酶 2 (RSK2) 抑制剂,IC50为 1.1 nM。

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BIX 02565 Chemical Structure
BIX 02565, CAS 1311367-27-7
规格 价格/CNY 货期 数量
1 mg ¥ 666 待询
2 mg ¥ 973 待询
5 mg ¥ 1,800 待询
10 mg ¥ 2,810 待询
25 mg ¥ 4,680 待询
50 mg ¥ 6,670 待询
1 mL * 10 mM (in DMSO) ¥ 1,800 现货
产品目录号及名称: BIX 02565 (T5428)
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纯度: 97.44%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 BIX 02565 is a potent inhibitor of ribosomal S6 kinase 2 (RSK2, IC50: 1.1 nM).
靶点活性 PRKD1:35 nM (cell free), RSK2:1.1 nM (cell free), LRRK2:16 nM (cell free)
体外活性 BIX 02565 inhibited RSK2 with IC50 value of 1.1 nM. It also inhibited LRRK2 and PRKD1 with IC50 values of 16 and 35 nM [1]. BIX 02565 elicited >50% inhibition at adrenergic α1A-, α1B-, α1D-, α2A-, β2-, and imidazoline I2 receptors (IC50s: 0.052-1.820 μM) [2].
体内活性 Infusion of BIX 02565 (1, 3, and 10 mg/kg) in the rat CV screen resulted in a precipitous decrease in both mean arterial pressure (MAP; to -65 ± 6 mm Hg below baseline) and heart rate (-93 ± 13 beats/min). In telemetry-instrumented rats, BIX 02565 (30, 100, and 300 mg/kg p.o. QD for 4 days) elicited concentration-dependent decreases in MAP after each dose (to -39 ± 4 mm Hg on day 4 at T(max)); analysis by Demming regression demonstrated strong correlation independent of route of administration and influence of anesthesia [2].
细胞实验 A monolayer of exponentially growing HLR-CREB cells was prepared and transfected using Effectene with RSK2. Cells were plated into 96-well culture plates, and compounds were added 20 to 24 h after transfection. Luciferase expression (48 h) and activity (5 min) were determined using Steady-Glo per manufacturer's instructions, and results were represented as the percentage luciferase activity relative to the control measured in the absence of inhibitors (percentage of control); the IC50 was fitted to a standard four-parameter logistic equation. Each data point represents an average of triplicate observations [2].
动物实验 Mean arterial pressure was assessed in conscious, freely moving male Sprague-Dawley rats (n = 6/group) instrumented with telemetry transmitters similar to that described previously. BIX 02565 (30, 100, and 300 mg/kg p.o. QD) was administered as a solution (10 ml/kg) in a 20% hydroxy-propyl-β-cyclodextran vehicle as described previously. Mean arterial pressure was reported from 2 h before (baseline) and 90 h after the first dose; compound was administered at 0, 24, 48, and 72 h. A blood sample was collected from satellite rats (n = 3/group) at 1-h after dose (Tmax) on days 1 and 4 for analysis of plasma drug concentrations by mass spectrometry [2].
分子量 458.56
分子式 C26H30N6O2
CAS No. 1311367-27-7

存储

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

溶解度

DMSO: 20 mg/mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Kirrane TM, et al. Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity. Bioorg Med Chem Lett. 2012 Jan 1;22(1):738-42. 2. Fryer RM, et al. Mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal S6 kinase 2 inhibitors. Journal of Pharmacology and Experimental Therapeutics (2012), 340(3), 492-500.

文献引用

1. Yuan Y, Xu J, Jiang L, et al. Discovery, Optimization, and Structure–Activity Relationship Study of Novel and Potent RSK4 Inhibitors as Promising Agents for the Treatment of Esophageal Squamous Cell Carcinoma. Journal of Medicinal Chemistry. 2021
BRD7389 S6K-18 Quercitrin LY-2584702 hydrochloride Pluripotin Vistusertib A-443654 GSK-25

相关化合物库

该产品包含在如下化合物库中:
细胞重编程化合物库 PI3K/Akt/mTOR 化合物库 氧化还原化合物库 神经退行性疾病化合物库 MAPK 抑制剂库 抗帕金森病化合物库 糖代谢化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

BIX 02565 1311367-27-7 Autophagy MAPK PI3K/Akt/mTOR signaling LRRK2 S6 Kinase Inhibitor Ribosomal S6 Kinase (RSK) S6K inhibit BIX-02565 BIX02565 inhibitor

 

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