추천 제품
Quality Level
분석
≥98% (HPLC)
양식
solid
색상
off-white to tan
solubility
DMSO: ≥20 mg/mL, clear, light yellow
H2O: insoluble
주관자
AstraZeneca
저장 온도
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
일반 설명
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.
애플리케이션
AR-A014418 has been used as an inhibitor of glycogen synthase kinase 3 (GSK3).
생화학적/생리학적 작용
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.
특징 및 장점
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.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
개인 보호 장비
dust mask type N95 (US), Eyeshields, Gloves
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시험 성적서(COA)
이미 열람한 고객
Glycogen synthase kinase 3-specific inhibitor AR-A014418 decreases neuropathic pain in mice: evidence for the mechanisms of action
Neuroscience, 226, 411-420 (2012)
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
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.
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
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
문서
Cancer stem cell media, spheroid plates and cancer stem cell markers to culture and characterize CSC populations.
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