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GeA-69
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GeA-69图片
CAS NO:2143475-98-1
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
GeA-69 是一种选择性变构 PARP14 大结构域 2 (MD2) 抑制剂,Kd值为 2.1 μM。

产品描述

GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).

体外活性

The macrodomain recruitment was significantly decreased in cells pre-treated with 50 μM GeA-69 and completely prevented in cells exposed to 250 μM GeA-69.

激酶实验

Binding experiments were carried out on a VP-ITC microcalorimeter. All experiments were performed in 50 mM HEPES (pH 7.4), 300 mM NaCl, 5 % glycerol, 0.5 mM TCEP at 12 °C, a reference power of 12 μCal/sec and a stirring speed of 307 rpm. The titrations were conducted using an initial injection of 2 μL followed by 28 identical injections of 10 μL with duration of 4 sec (per injection) and a spacing of 240 sec between injections. Competition experiments were performed on an iTC200 instrument at 20 °C, a reference power of 12 μCal/sec and a stirring speed of 1000 rpm. Following an initial injection of 0.2 μL, 20 identical injections of 2 μL were run with a duration of 4 sec (per injection) and a spacing of 150 sec between injections. Data analysis was carried out using Origin software with the MicroCal plugin. Thermodynamic parameters were calculated using ΔG = ΔH ? TΔS = ?RTlnKB, where ΔG, ΔH, and ΔS are the changes in free energy, enthalpy, and entropy of binding, respectively. In all cases, a single binding site model was employed.

Cas No.

2143475-98-1

分子式

C20H16N2O

分子量

300.361

储存和溶解度

DMSO:120 mg/mL (399.53 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years