AR-A014418  487021-52-3

ARA014418
分子式：C12H12N4O4S   分子量：308.31
 
產(chǎn)品描述
AR-A014418是一種有效的GSK3抑制劑，IC50為104 +/- 27 nM。（GSK3）是種絲氨酸/蘇氨酸激酶，這種激酶與一些病理相關(guān)，如糖尿病和老年癡呆癥
靶點
 GSK3
 
       
IC50
104 +/- 27 nM
 
       
體外研究
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. Colon cancer HCT116 cells were sensitized to apoptosis by co-treatment with reovirus and a GSK-3beta inhibitor, AR-A014418
體內(nèi)研究
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. 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.
溶解性
DMSO 100 mM，乙醇 5 mM
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO