A3230

AR-A014418

Name: AR-A014418
Brand: SIGMA
Price: 902 PLN

≥98% (HPLC), solid

Synonim(y):

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

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Informacje o tej pozycji

Wzór empiryczny (zapis Hilla):

C₁₂H₁₂N₄O₄S

Numer CAS:

487021-52-3

Masa cząsteczkowa:

308.31

NACRES:

NA.77

PubChem Substance ID:

329770820

UNSPSC Code:

12352200

MDL number:

MFCD08277040

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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)

SMILES string

COc1ccc(CNC(=O)Nc2ncc(s2)[N+]([O-])=O)cc1

InChI key

YAEMHJKFIIIULI-UHFFFAOYSA-N

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

Quality Level

100

Powiązane kategorie

Bioactive Small Molecule Inhibitors

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Ta pozycja	G5547	D1944	555562
Sigma-Aldrich A3230 AR-A014418	Sigma-Aldrich G5547 GSK837149A	Sigma-Aldrich D1944 D4476	Sigma-Aldrich 555562 Rho Kinase Inhibitor XIII, RKI-1447
form solid	form solid	form solid	form solid
assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. −20°C
solubility DMSO: ≥20 mg/mL, clear, light yellow, H₂O: insoluble	solubility DMSO: >10 mg/mL, H₂O: insoluble	solubility DMSO: ~20 mg/mL, H₂O: insoluble	solubility DMSO: 100 mg/mL
originator AstraZeneca	originator GlaxoSmithKline	originator GlaxoSmithKline	originator -

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.[1] It has also been studied that AR-A014418 inhibits growth of pancreatic cancer cells.[2]

Application

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

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.

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Klasa składowania

11 - Combustible Solids

wgk

WGK 3

ppe

dust mask type N95 (US), Eyeshields, Gloves

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Signalling through the type 1 insulin-like growth factor receptor (IGF1R) interacts with canonical Wnt signalling to promote neural proliferation in developing brain.

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

GSK3beta inhibition promotes synaptogenesis in Drosophila and mammalian neurons

Cuesto G, et al.

PLoS ONE, 10(3), e0118475-e0118475 (2015)

Glycogen synthase kinase 3β inhibition prevents monocyte migration across brain endothelial cells via Rac1-GTPase suppression and down-regulation of active integrin conformation.

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

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

Corticosterone rapidly increases thorns of CA3 neurons via synaptic/extranuclear glucocorticoid receptor in rat hippocampus.

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

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