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Merck

A3230

Sigma-Aldrich

AR-A014418

≥98% (HPLC), solid

别名:

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

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About This Item

经验公式(希尔记法):
C12H12N4O4S
分子量:
308.31
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:

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


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Qichen Hu et al.
ASN neuro, 4(5) (2012-05-26)
Signalling through the IGF1R [type 1 IGF (insulin-like growth factor) receptor] and canonical Wnt signalling are two signalling pathways that play critical roles in regulating neural cell generation and growth. To determine whether the signalling through the IGF1R can interact
Glycogen synthase kinase-3 inhibitor AR-A014418 suppresses pancreatic cancer cell growth via inhibition of GSK-3-mediated Notch1 expression
Selvi K, et al.
Hpb : the Official Journal of the International Hepato Pancreato Biliary Association, 17(9), 770-776 (2015)
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
GSK3beta inhibition promotes synaptogenesis in Drosophila and mammalian neurons
Cuesto G, et al.
PLoS ONE, 10(3), e0118475-e0118475 (2015)
S Fittipaldi et al.
Journal of endocrinological investigation, 42(6), 727-739 (2018-11-28)
Cadmium (Cd) is a widespread environmental pollutant that causes alterations in human health acting as endocrine disruptor. Recent data suggest that cardiovascular system might be a contamination target tissue, since Cd is found in atheromatic plaques. Thus, the purpose of

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