(-)-Securinine 是来自叶底珠的一种生物碱,也是GABAA受体拮抗剂。
产品描述
(-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.
体外活性
(-)-Securinine significantly inhibits HeLa cells growth with IC50 values of 7.02±0.52 μg/mL (32.3 μM). (-)-Securinine induces apoptosis in a dose-dependent manner in the tested cells, increases the percentage of ROS positive cells and depolarized cells as well as stimulates the activity of ERK1/2, caspase-9 and -3/7. (-)-Securinine also induces cell cycle arrest in S phase. Real-time PCR analysis shows high expression of tumor necrosis factor receptor superfamily (TNFRSF) genes in the cells stimulated with (-)-Securinine.
体内活性
In the tumor model, tumor growth is significantly impaired with (-)-Securinine treatment indicating that (-)-Securinine has potential as an Acute Myeloid Leukemia (AML) therapeutic. (-)-Securinine treated mice (n=5 mice, bilateral tumors), exhibit an average of more than 75% smaller tumors than vehicle-treated mice at the end of the study period.
Cas No.
5610-40-2
分子式
C13H15NO2
分子量
217.26
别名
一叶秋碱;Securinine
储存和溶解度
DMSO:2 mg/mL (9.21 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years