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AR-A014418GSK3β inhibitor, ATP-competitive and selective

AR-A014418

Catalog No. A3184
Size Price Stock Qty
Evaluation Sample $28.00 In stock
10mg $68.00 In stock
50mg $189.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

AR-A014418

Biological Activity

Description AR-A014418 is an ATP-competitive, and selective inhibitor of GSK3β with IC50 and Ki of 104 nM and 38 nM
Targets GSK-3          
IC50 104 +/- 27 nM          

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Chemical Properties

Cas No. 487021-52-3 SDF Download SDF
Synonyms AR-AO 14418;AR 0133418;AR 014418;GSK 3β inhibitor
Chemical Name 1-[(4-methoxyphenyl)methyl]-3-(5-nitro-1,3-thiazol-2-yl)urea
Canonical SMILES COC1=CC=C(C=C1)CNC(=O)NC2=NC=C(S2)[N+](=O)[O-]
Formula C12H12N4O4S M.Wt 308.31
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Research Update

2. Glycogen synthase kinase 3-specific inhibitor AR-A014418 decreases neuropathic pain in mice: evidence for the mechanisms of action. Neuroscience. 2012 Dec 13;226:411-20. doi: 10.1016/j.neuroscience.2012.09.020. Epub 2012 Sep 19.
Abstract
AR-A014418 exhibited evidently anti-hyperalgesic effects in mice with neuropathic pain possibly through reducing proinflammatory cytokines and increasing serotonergic and catecholaminergic pathways, in which intraperitoneal administration of AR-A014418 inhibited PSNL-induced mechanical hyperalgesia and PSNL-induced cold hyperalgesia and prevented the increase of TNF-α and IL-1β without affecting IL-ra and IL-10.
4. The antinociceptive effects of AR-A014418, a selective inhibitor of glycogen synthase kinase-3 beta, in mice. J Pain. 2011 Mar;12(3):315-22. doi: 10.1016/j.jpain.2010.06.007. Epub 2010 Aug 12.
Abstract
The treatment of AR-A014418 alone or with formalin inhibited nociception induced by various sources, in which formalin-induced licking was suppressed at the late phase or both phases by AR-A014418 alone of different dosages. The anti-nociceptive effect of AR-A014418 was thought to be induced by glutamatergic system through metabotropic and ionotropic (NMDA) receptors and the inhibition of the cytokine (TNF-α and IL-1β) signaling.

Background

IC50: 104 ± 27 nM

Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as diabetes and Alzheimer’s disease (AD). AR-A014418 is a selective GSK-3 inhibitor.

In vitro: ARA014418 acted as an ATP-competitive manner and did not significantly inhibit cdk2 or cdk5 or 26 other kinases demonstrating high specificity for GSK3. AR-A014418 inhibited tau phosphorylation at a GSK3-specific site (Ser-396) in cells stably expressing human four-repeat tau protein [1].

In vivo: ARA014418 induced behavioural changes that were consistent with the effects of antidepressant drugs. Subacute intraperitoneal injections of AR-A014418 reduced immobility time in rats exposed to the forced swim test, which was a well-established model for antidepressant efficacy. Moreover, the specificity of this effect was supported by our finding that AR-A014418 decreased spontaneous as well as amphetamine-induced activity [2].

Clinical trial: currently no clinical data were available

References:
[1] Bhat R, Xue Y, Berg S, Hellberg S, Orm? M, Nilsson Y, Rades?ter AC, Jerning E, Markgren PO, Borgeg?rd T, Nyl?f M, Giménez-Cassina A, Hernández F, Lucas JJ, Díaz-Nido J, Avila J.  Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J Biol Chem. 2003;278(46):45937-45.
[2] Gould TD, Einat H, Bhat R, Manji HK.  AR-A014418, a selective GSK-3 inhibitor, produces antidepressant-like effects in the forced swim test. Int J Neuropsychopharmacol. 2004;7(4):387-90.