AR-A014418 CAS NO.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].