SB202190

• 产品编号：CST-8158S      品牌：CST       原厂货号：8158S
• 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SB202190为冻干粉。对于10 mM浓度贮存液，在5mg冻干粉中加入1.51 ml DMSO。工作浓度和处理时间根据所需的预期效果来确定，在用兴奋剂处理前，用于预处理的浓度一般是5-20 µM，处理1-2小时。能溶于DMSO，在其他溶剂中的溶解度尚未评估。SB202190是一种吡啶咪唑，能通过与ATP竞争来抑制p38 MAP激酶（促细胞分裂剂激活性蛋白激酶,38kDa）活性（1），并且能够通过半胱氨酸蛋白酶(CPP32)样半胱氨酸天冬氨酸蛋白酶的激活来诱导细胞凋亡（2）。SB202190能同时阻断脂多糖（LPS）诱导的基因表达和一氧化氮（NO）诱导的白介素-8 mRNA在单核细胞中的稳定作用（3,4）。用SB202190对细胞进行预处理后，在有茴香霉素（一种MAPK通路诱导物）存在的情况下，也能抑制p38 MAPK的磷酸化（5）。值得注意的是，SB202190抑制的作用机制与SB203580不一样，SB203580通过与ATP结合口袋结合来抑制p38 MAPK的催化活性，而不是通过上游激酶来抑制p38 MAPK的磷酸化（6）。

原厂资料：

Molecular Characterization

C20H14FN3O

Purity

>99%

Directions for Use

SB202190 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1.51 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 5-20 µM for 1-2 hours prior to treating with a stimulator. Soluble in DMSO, solubility in other solvents has not been evaluated.

Background

SB202190, a pyridinyl imidazole, inhibits p38 MAP kinase activity through competition with ATP (1), and has been shown to induce apoptosis through activation of cysteine protease (CPP32)-like caspases (2). SB202190 blocks both lipopolysaccharide (LPS)-induced gene expression and nitric oxide (NO)-induced stabilization of interleukin (IL)-8 mRNA in monocytes (3,4). Pre-treatment of cells with SB202190 has been shown to inhibit phosphorylation of p38 MAPK despite exposure to anisomycin, a known inducer of the MAPK pathway (5). Of note, the mechanism of inhibition of SB202190 is unlike the one seen with SB203580, which inhibits p38 MAPK catalytic activity by binding to the ATP binding pocket, but does not inhibit phosphorylation of p38 MAPK by upstream kinases (6).

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.