AR-A014418 AR-AO 14418;GSK-3β Inhibitor VIII;N-[(4-Methoxyphenyl)methyl]-N'-(5-nitro-2-thiazolyl)urea;N-[(4-Methoxyphenyl)Methyl]-N'-(5-nitro-thiazol-2-yl)urea;AR 0133418;GSK 3B Inhibitor VIII;AR 014418;GSK 3β 487021-52-3
AR-A014418 is a selective and effective GSK3β inhibitor with an IC50 value of 104 +/- 27 nM; no significant inhibition on 26 other kinases.
IC50 Value: 104 +/- 27 nM [1]
Target: GSK3β
in vitro: AR-A014418 inhibits GSK3 (IC50 = 104 +/- 27 nM), in an ATP-competitive manner (Ki = 38 nM). AR-A014418 does not significantly inhibit cdk2 or cdk5 (IC50 > 100 microM) or 26 other kinases demonstrating high specificity for GSK3 [1]. Colon cancer HCT116 cells were sensitized to apoptosis by co-treatment with reovirus and a GSK-3beta inhibitor, AR-A014418 [2].
in vivo: Injections of AR-A014418reduced immobility time in rats exposed to the forced swim test, a well-established model for antidepressant efficacy. In addition, the specificity of this effect is supported by our finding that AR-A014418 decreased spontaneous as well as amphetamine-induced activity [3]. AR-A014418 coinjection (10 ng/site, it) inhibited nociception induced by glutamate, N-methyl-D-aspartate (NMDA), (±)-1-aminocyclopentane-trans-1,3-dicarboxylic acid (trans-ACPD), tumor necrosis factor-alpha (TNF-α), and interleukin-1beta (IL-1β) by 47 ± 12%, 48 ± 11%, 31 ± 8%, 46 ± 13%, and 44 ± 11%, respectively [4].
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