AR-A014418CAS号: 487021-52-3分子式: C12H12N4O4S分子量: 308.31描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
AR-A014418 is a selective and effective GSK3β inhibitor with an IC 50 value of 104 +/- 27 nM; no significant inhibition on 26 other kinases. |
纯度 |
98%
|
储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
|
基本信息 | |
别名 |
AR 0133418;GSK 3β inhibitor VIII;AR 014418
|
外观 |
Powder
|
可溶性/溶解性 |
DMSO : 30.8 mg/mL (100 mM)
Ethanol : 1.5 mg/mL (5 mM) |
生物活性 | |
靶点 |
GSK-3β ,GSK-3β
|
In vitro(体外研究) |
AR-A014418 inhibits tau phosphorylation at a GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human four-repeat tau protein with IC50 of 2.7 μM, and protects cultured N2A cells from death induced by blocking PI3K/PKB pathway. In hippocampal slices, AR-A014418 inhibits neurodegeneration mediated by beta-amyloid peptide. While in NGP and SH-5Y-SY cells, AR-A014418 reduces neuroendocrine markers and suppresses neuroblastoma cell growth.
|
In vivo(体内研究) |
In ALS mouse model with the G93A mutant human SOD1, AR-A014418 (0-4 mg/kg, i.p.) delays the onset of symptoms, improves motor activity, slows down disease progression, and postpons the endpoint of the disease. In addition, AR-A014418 produces inhibition effect on acetic acid- and formalin-induced nociception in mice by modulating NMDA and metabotropic receptor signaling as well as TNF-α and IL-1β transmission in the spinal cord.
|
分子结构图