| 货号 | 5190/50 |
| 别名 | 6-(2,4-Dichlorophenyl)-8-ethyl-2-[[ |
| 供应商 | Tocris |
| 生物活性 | Potent p21-activated kinase (PAK) inhibitor (IC50 values are 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively). Blocks and reverses the DISC1 knockdown-induced reduction in dendritic spine size in cortical neurons. Attenuates dendritic spine elimination and enhances spine generation in DISC1 knockdown mice. Ameliorates autism-like behavioral symptoms in fragile X mental retardation 1 (Fmr1) knockout mice. Brain penetrant and orally bioavailable. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 513.39 |
| 分子式 | C25H23Cl2FN6 |
| 可溶性/溶解性 | Soluble to 20 mM in DMSO |
| 参考文献 | Wanget al (2016) P21-activated kinase inhibitors FRAX486 and IPA3: inhibition of prostate stromal cell growth and effects on smooth muscle contraction in the human prostate. PLoS One 11 e0153312. PMID: 27071060. Dolanet al (2013) Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. Proc.Natl.Acad.Sci.U.S.A. 110 5671. PMID: 23509247. Hayashi-Takagiet al (2013) PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence. Proc.Natl.Acad.Sci.U.S.A. 111 6461. PMID: 24706880. |