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Merck
CN

S3442

Sigma-Aldrich

SB 216763

>98% (HPLC)

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别名:
3-(2,4-二氯苯基)-4-(1-甲基-1H-吲哚-3-基)-1H-吡咯-2,5-二酮
经验公式(希尔记法):
C19H12N2O2Cl2
分子量:
371.22
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

>98% (HPLC)

颜色

orange

溶解性

DMSO: soluble 20 mg/mL
H2O: insoluble

创始人

GlaxoSmithKline

储存温度

−20°C

SMILES字符串

Cn1cc(C2=C(C(=O)NC2=O)c3ccc(Cl)cc3Cl)c4ccccc14

InChI

1S/C19H12Cl2N2O2/c1-23-9-13(11-4-2-3-5-15(11)23)17-16(18(24)22-19(17)25)12-7-6-10(20)8-14(12)21/h2-9H,1H3,(H,22,24,25)

InChI key

JCSGFHVFHSKIJH-UHFFFAOYSA-N

基因信息

应用

使用 SB-216763 抑制人脑微血管内皮细胞系 和大肠癌细胞中的 GSK-3β。

生化/生理作用

SB-216763 是一种与 ATP 竞争并强效抑制 α和 βGSK-3 的同工酶。作为神经保护剂,它防止 PI3-激酶途径诱导的神经细胞死亡。它还可以延迟预处理,减少梗死面积,防止心肌缺血。
强效、选择性、细胞渗透性糖原合成酶激酶-3 (GSK-3) 抑制剂。

特点和优势

《受体分类和信号转导》手册的 GSK-3PKB/Akt 页面有该化合物的介绍。想要浏览手册的其他页面, 请单击此处
该化合物是激酶磷酸酶生物学研究的特色产品。 点击此处 ,发现更多特色激酶磷酸酶生物学产品。前往 sigma.com/discover-bsm 了解更多关于其他研究领域的生物活性小分子。
该化合物由 GlaxoSmithKline 开发。要浏览其他制药公司开发的化合物列表批准的药物/候选药物的列表, 点击这里

法律信息

根据GlaxoSmithKline的协议出售用于研究目的

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves


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Giulia Rossana Gulino et al.
Environmental health perspectives, 124(6), 776-784 (2015-12-20)
Chrysotile asbestos accounts for > 90% of the asbestos used worldwide, and exposure is associated with asbestosis (asbestos-related fibrosis) and other malignancies; however, the molecular mechanisms involved are not fully understood. A common pathogenic mechanism for these malignancies is represented
Shuzhen Guo et al.
Stroke, 40(2), 652-655 (2008-11-01)
We recently reported that delayed lithium therapy can improve stroke recovery in rats by augmenting neurovascular remodeling. We tested the hypothesis that lithium can promote the expression of growth factors in brain endothelial cells and astrocytes. Human brain microvascular endothelial
Eric R Gross et al.
American journal of physiology. Heart and circulatory physiology, 294(3), H1497-H1500 (2008-01-29)
Previous studies in our laboratory suggest that an acute inhibition of glycogen synthase kinase 3 (GSK3) by SB-216763 (SB21) is cardioprotective when administered just before reperfusion. However, it is unknown whether the GSK inhibitor SB21 administered 24 h before ischemia
Jonathan S Miller et al.
PloS one, 9(2), e88026-e88026 (2014-02-08)
The Akt - GSK3 signaling pathway has been recently implicated in psychostimulant-induced behavioral and cellular effects. Here, the ability of cocaine to regulate the activity of Akt and GSK3 was investigated by measuring the phosphorylation states of the two kinases.
D A Cross et al.
Journal of neurochemistry, 77(1), 94-102 (2001-03-30)
The phosphatidylinositol 3-kinase (PI 3-kinase)/protein kinase B (PKB; also known as Akt) signalling pathway is recognized as playing a central role in the survival of diverse cell types. Glycogen synthase kinase-3 (GSK-3) is a ubiquitously expressed serine/threonine protein kinase that

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