1A-116

1A-116CAS号: 1430208-73-3分子式: C16H16F3N3分子量: 307.31描述纯度储存/保存方法靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
1A-116 is a specific Rac1 inhibitor.
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.
生物活性
靶点
Rac1
In vitro(体外研究)
1A-116 shows lesser effect on MCF7::pcDNA.3 cells than on MCF7::C1199 cells. 1A-116 treatment decreases phospho-PAK1 levels in a time-dependent manner. The presence of 1A-116 reverts the PAK1 phosphorylation induced by 4-hydroxytamoxifen (Tam). The presence of 1A-116 also effectively reverts Rac1-PAK1-mediated estrogen receptor (ER) phosphorylation at Ser305. 1A-116 shows a significant increase in antiproliferative activity on F3II cells, showing an IC50 value of 4 µM. A-116 also dramatically impairs Rac1 activation at low micromolar range (1 µM).
In vivo(体内研究)
1A-116 shows lesser effect on MCF7::pcDNA.3 cells than on MCF7::C1199 cells. 1A-116 treatment decreases phospho-PAK1 levels in a time-dependent manner. The presence of 1A-116 reverts the PAK1 phosphorylation induced by 4-hydroxytamoxifen (Tam). The presence of 1A-116 also effectively reverts Rac1-PAK1-mediated estrogen receptor (ER) phosphorylation at Ser305. 1A-116 shows a significant increase in antiproliferative activity on F3II cells, showing an IC50 value of 4 µM. A-116 also dramatically impairs Rac1 activation at low micromolar range (1 µM).