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质量水平
检测方案
≥98% (HPLC)
形式
solid
颜色
off-white to tan
溶解性
DMSO: ≥20 mg/mL, clear, light yellow
H2O: insoluble
创始人
AstraZeneca
储存温度
2-8°C
SMILES字符串
COc1ccc(CNC(=O)Nc2ncc(s2)[N+]([O-])=O)cc1
InChI
1S/C12H12N4O4S/c1-20-9-4-2-8(3-5-9)6-13-11(17)15-12-14-7-10(21-12)16(18)19/h2-5,7H,6H2,1H3,(H2,13,14,15,17)
InChI key
YAEMHJKFIIIULI-UHFFFAOYSA-N
一般描述
AR-A014418 may have chronic pain-relieving properties. In mice having neuropathic pain, this molecule has been shown to have antihyperalgesic effects. AR-A014418 may modulate proinflammatory cytokines and the catecholaminergic and serotonergic pathways. It has also been studied that AR-A014418 inhibits growth of pancreatic cancer cells.
应用
AR-A014418 has been used as an inhibitor of glycogen synthase kinase 3 (GSK3).
生化/生理作用
Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as diabetes and Alzheimer′s disease. GSK3 inhibitor, AR-A014418, inhibits GSK3 (IC50 = 104 nM), in an ATP-competitive manner (Ki = 38 nM). AR-A014418 does not significantly inhibit cdk2 or cdk5 (IC50 > 100 μM) or 26 other kinases, demonstrating high specificity for GSK3.
特点和优势
This compound is featured on the PKB/Akt page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
WGK
WGK 3
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
The American journal of pathology, 181(4), 1414-1425 (2012-08-07)
Glycogen synthase kinase (GSK) 3β has been identified as a regulator of immune responses. We demonstrated previously that GSK3β inhibition in human brain microvascular endothelial cells (BMVECs) reduced monocyte adhesion/migration across BMVEC monolayers. Herein, we tested the idea that GSK3β
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培养和表征CSC群体的癌症干细胞培养基、球状体培养板和癌症干细胞标志物。
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