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A3230

AR-A014418

Name: AR-A014418
Brand: SIGMA

≥98% (HPLC), solid

别名:

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

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关于此项目

经验公式（希尔记法）:

C₁₂H₁₂N₄O₄S

化学文摘社编号:

487021-52-3

分子量:

308.31

NACRES:

NA.77

PubChem Substance ID:

329770820

UNSPSC Code:

12352200

MDL number:

MFCD08277040

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

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属性

Quality Level

100

assay

≥98% (HPLC)

form

solid

color

off-white to tan

solubility

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

originator

AstraZeneca

storage temp.

2-8°C

SMILES string

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

说明

General description

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.

Application

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

Biochem/physiol Actions

AR-A014418 is a glycogen synthase kinase 3 (GSK3) inhibitor.

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.

Features and Benefits

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.

存储类别

11 - Combustible Solids

wgk

WGK 3

ppe

dust mask type N95 (US), Eyeshields, Gloves

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Cancer Stem Cells: Targets for Cancer Therapy

Cancer stem cell media, spheroid plates and cancer stem cell markers to culture and characterize CSC populations.

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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。

Focused Ultrasound-Induced Blood-Brain Barrier Opening Enhances GSK-3 Inhibitor Delivery for Amyloid-Beta Plaque Reduction.

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

Glycogen synthase kinase-3 inhibition sensitizes pancreatic cancer cells to TRAIL-induced apoptosis.

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)

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全球贸易项目编号

货号	GTIN
A3230-5MG	04061832433783
A3230-25MG	04061832433776