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Swainsonine (Tridolgosir) 是一种从黄芪中分离出来的一种生物碱,是一种强效和可逆的α-甘露糖苷酶抑制剂。Swainsonine 具有抗肿瘤活性,可诱导细胞凋亡和细胞周期停滞在 G2/M 期。
Swainsonine (Tridolgosir) 是一种从黄芪中分离出来的一种生物碱,是一种强效和可逆的α-甘露糖苷酶抑制剂。Swainsonine 具有抗肿瘤活性,可诱导细胞凋亡和细胞周期停滞在 G2/M 期。
产品描述 | Swainsonine (Tridolgosir) is an alkaloid isolated from Astragalus membranaceus and is a potent and reversible inhibitor of alpha-mannosidase. swainsonine has antitumour activity and induces apoptosis and cell cycle arrest in the G2/M phase. |
靶点活性 | Golgi α-mannosidase II:0.2 μM, Lysosomal α-mannosidase:0.2 μM |
体外活性 | Swainsonine(0-40 μM;12小时)对U251和LN444细胞表现出抗增殖活性。[2] Swainsonine(30 μM;12小时)诱导凋亡和细胞周期在G2/M阶段停滞,降低了CyclinD1和CDK4蛋白水平,并提高了p16蛋白水平。[2] 此外,Swainsonine(30 μM;12小时)降低了胶质瘤细胞的迁移和侵袭能力。[2] |
体内活性 | Swainsonine(1 mg/kg;腹腔注射;每天两次,持续10天)和cisplatin在小鼠中提高了抗肿瘤效果。[3] |
别名 | 苦马豆素, Tridolgosir |
分子量 | 173.21 |
分子式 | C8H15NO3 |
CAS No. | 72741-87-8 |
Smiles | OC1CN2CCCC(O)C2C1O |
密度 | 1.38 g/cm3 |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 9.0 mg/mL (52.0 mM ), Sonication and heating are recommended. DMSO: 9.0 mg/mL (52.0 mM ), Sonication and heating are recommended. H2O: 3.2 mg/mL (18.5 mM ), Sonication and heating to 60℃ are recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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