AR-A014418

Short Summary : GSK3β inhibitor, ATP-competitive and selective

Category : PI3K/Akt/mTOR Signaling|GSK-3

Purity : 0.9899

CAS Number : 487021-52-3

Formula : C12H12N4O4S

Molecular Weight : 308.31

SMILE : COC1=CC=C(C=C1)CNC(=O)NC2=NC=C(S2)[N+](=O)[O-]

Solubility : >15.4mg/mL in DMSO

Storage : Store at -20°C

Description : IC50: 104 27 nMGlycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as diabetes and Alzheimers 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, Gimnez-Cassina A, Hernndez F, Lucas JJ, Daz-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.

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