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A3230

Sigma-Aldrich

AR-A014418

≥98% (HPLC), solid

Sinonimo/i:

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

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About This Item

Formula empirica (notazione di Hill):
C12H12N4O4S
Numero CAS:
487021-52-3
Peso molecolare:
308.31
Numero MDL:
MFCD08277040
Codice UNSPSC:
12352200
ID PubChem:
329770820
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥98% (HPLC)

Forma fisica

solid

Colore

off-white to tan

Solubilità

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

Ideatore

AstraZeneca

Temperatura di conservazione

2-8°C

Stringa SMILE

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)
YAEMHJKFIIIULI-UHFFFAOYSA-N

Descrizione generale

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.

Applicazioni

AR-A014418 has been used as an inhibitor of glycogen synthase kinase 3 (GSK3).

Azioni biochim/fisiol

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.

Caratteristiche e vantaggi

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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Dispositivi di protezione individuale

dust mask type N95 (US), Eyeshields, Gloves

Certificati d'analisi (COA)

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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)
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
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
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