PD184352

• 产品编号：CST-12147S      品牌：CST       原厂货号：12147S
• 产品分类：生化试剂 > 生物试剂 > 生物活性小分子 > 抑制剂
• 应用分类：

描述：

提供的PD184352为冻干粉。对于10mM浓度贮存液，在5 mg冻干粉中加入1044.6 µl DMSO。工作浓度和处理时间根据所需的预期效果来确定，一般在用兴奋剂处理前，以0.1-10 µM，处理0.5-1 小时或者单独使用，能作用不同的时间，可持续作用24小时。能溶于DMSO（25 mg/ml）和加热的乙醇（8 mg/ml），难溶于水，在水中的最大溶解度约为5-10µM。PD184352 (CI-1040)是一种非常有效的选择性的非竞争性MEK抑制剂，MEK1的IC50为17nm（1）。用PD184352进行细胞的治疗会抑制MAPK的活化（1-4）并能有效抑制细胞的增殖，包含B-Raf基因V600E突变（2,3）。研究者发现PD184352能有效抑制MEK5，但是效果不如对MEK1的好（4）。

原厂资料：

Molecular Characterization

C17H14ClF2IN2O22

Directions for Use

PD184352 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1044.6 µl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.1-10 µM for 0.5-1 hr prior to treating with a stimulator or is used alone with varying treatment times lasting up to 24 hr. Soluble in DMSO at 25 mg/ml and ethanol at 8 mg/ml with warming; poorly soluble in water with maximum solubility in water at ~5-10 µM.

Background

PD184352 (CI-1040) is a highly potent and selective noncompetitive MEK inhibitor with an IC50 of 17 nM for MEK1 (1). Treatment of cells with PD184352 leads to suppression of MAPK activation (1-4) and potently inhibits the proliferation of cells harboring the B-Raf mutation V600E (2,3). Researchers have shown that PD184352 effectively inhibits MEK5, although not as potently as MEK1 (4).

注意事项：

Storage: Store lyophilized or in solution at -20°C, desiccated.
Protect from light. In lyophilized form, the chemical is stable for
24 months. Once in solution, use within 3 months to prevent loss
of potency. Aliquot to avoid multiple freeze/thaw cycles.