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Radicicol(Monorden,根赤壳菌素)是一种抗真菌抗生素,也是热休克蛋白90(Hsp90)的强效抑制剂(IC50 = 1 μM),通过结合Hsp90的ATP结合口袋,导致Hsp90被蛋白酶体降解。此外,Radicicol还抑制多种肿瘤细胞系的生长和增殖。它还具有抗疟疾活性,并可作为脂肪和肥胖相关蛋白(FTO)的抑制剂。Radicicol通过阻断p38激酶信号通路和NF-κB/Rel抑制iNOS基因表达
Radicicol(Monorden,根赤壳菌素)是一种抗真菌抗生素,也是热休克蛋白90(Hsp90)的强效抑制剂(IC50 = 1 μM),通过结合Hsp90的ATP结合口袋,导致Hsp90被蛋白酶体降解。此外,Radicicol还抑制多种肿瘤细胞系的生长和增殖。它还具有抗疟疾活性,并可作为脂肪和肥胖相关蛋白(FTO)的抑制剂。Radicicol通过阻断p38激酶信号通路和NF-κB/Rel抑制iNOS基因表达
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500 μg | 待估 | 35日内发货 | |
1 mg | ¥ 1,260 | 35日内发货 | |
5 mg | 待估 | 35日内发货 |
产品描述 | Radicicol (Monorden) is an antifungal antibiotic and a potent inhibitor of heat shock protein 90 (Hsp90), which leads to the degradation of Hsp90 by the proteasome by binding to its ATP-binding pocket. In addition, Radicicol inhibits the growth and proliferation of several tumor cell lines. It also has anti-malarial activity and acts as an inhibitor of adipose- and obesity-related proteins (FTO). Radicicol inhibits iNOS gene expression by blocking the p38 kinase signaling pathway and NF-kB/Rel |
靶点活性 | HSP90:1 μM |
体外活性 | Radicicol 对 PDK1 活性的抑制 IC50 值为 230 mM,对 PDK3 的抑制 IC50 值为 400 μM。[1] |
体内活性 | 方法:Radicicol (20 mg/kg/60 mg/kg,腹腔注射,2次给药,间隔1 h) 给小鼠,观察其对小鼠(I/R) 损伤的抑制作用。 结果:Radicicol具有肾脏保护作用,改善肾缺血再灌注 (I/R) 损伤,增加肾损伤小鼠肾脏 HSP70 mRNA 和蛋白。[4] |
别名 | 根赤壳菌素, Monorden |
分子量 | 364.78 |
分子式 | C18H17ClO6 |
CAS No. | 12772-57-5 |
Smiles | C[C@@H]1C[C@@H]2[C@H](O2)/C=C\C=C\C(=O)CC3=C(C(=CC(=C3Cl)O)O)C(=O)O1 |
密度 | 1.364 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 | DMSO: 80 mg/mL (219.31 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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