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Merck
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文件

A3230

Sigma-Aldrich

AR-A014418

≥98% (HPLC), solid

同義詞:

N-(4-Methoxybenzyl)-N′-(5-nitro-1,3-thiazol-2-yl)urea

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About This Item

經驗公式(希爾表示法):
C12H12N4O4S
CAS號碼:
分子量::
308.31
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

solid

顏色

off-white to tan

溶解度

DMSO: ≥20 mg/mL, clear, light yellow
H2O: insoluble

起源

AstraZeneca

儲存溫度

2-8°C

SMILES 字串

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 密鑰

YAEMHJKFIIIULI-UHFFFAOYSA-N

一般說明

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.

應用

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.

特點和優勢

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves


分析證明 (COA)

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Miyuki Yoshiya et al.
Frontiers in neural circuits, 7, 191-191 (2013-12-19)
Modulation of synapses under acute stress is attracting much attention. Exposure to acute stress induces corticosterone (CORT) secretion from the adrenal cortex, resulting in rapid increase of CORT levels in plasma and the hippocampus. We tried to test whether rapid
Po-Hung Hsu et al.
Scientific reports, 8(1), 12882-12882 (2018-08-29)
Alzheimer's disease (AD) is a neurodegenerative disease that is the leading cause of age-related dementia. Currently, therapeutic agent delivery to the CNS is a valued approach for AD therapy. Unfortunately, the CNS penetration is greatly hampered by the blood-brain barrier
Shadi Mamaghani et al.
PloS one, 7(7), e41102-e41102 (2012-07-26)
Tumor necrosis factor-related apoptosis inducing ligand (TRAIL) induces apoptosis in a variety of cancer cell lines with little or no effect on normal cells. However, its effect is limited as some cancers including pancreatic cancer show de novo resistance to
Glycogen synthase kinase 3-specific inhibitor AR-A014418 decreases neuropathic pain in mice: evidence for the mechanisms of action
Mazzardo-Martins L, et al.
Neuroscience, 226, 411-420 (2012)
Slava Rom et al.
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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