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Merck
CN

A3230

AR-A014418

≥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:
分子量:
308.31
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
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Quality Level

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

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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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
Summer L Thompson et al.
PloS one, 14(2), e0211239-e0211239 (2019-02-06)
Serotonin-1B receptors (5-HT1BRs) modulate perseverative behaviors and prepulse inhibition (PPI) in humans and mice. These inhibitory G-protein-coupled receptors signal through a canonical G-protein-coupled pathway that is modulated by GSK-3β, and a noncanonical pathway mediated by the adaptor protein β-arrestin2 (Arrb2).
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)



全球贸易项目编号

货号GTIN
A3230-5MG04061832433783
A3230-25MG04061832433776