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:
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
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
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
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
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)
Huilan Xie et al.
Journal of dental sciences, 17(2), 802-810 (2022-06-28)
Glycogen synthase kinase-3β (GSK3β) inhibitor enhances bone formation, while dental pulp stem cells (DPSC) are potentially used to repair bone defects. The present study aimed to investigate the effect of AR-A014418 (AR, a specific glycogen synthase kinase-3β inhibitor) on the
商品
Cancer stem cell media, spheroid plates and cancer stem cell markers to culture and characterize CSC populations.
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。
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