3-Methyladenine是一种选择性PI3K抑制剂,抑制Vps34和PI3Kγ的IC50分别为25 μM和60 μM;永久性抑制I型PI3K,短暂的抑制III型PI3K。
Inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase); also inhibits the autophagic sequestration of cell proteins in rat hepatocytes. 3-MA is a synthetic intermediate and a cell-permeable autophagic sequestration blocker that protects cerebellar granule cells from apoptosis post serum/potassium deprivation. Blocks apoptosis in cerebellar granule cells (CGCs) following serum and potassium deprivation.
30% Propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)
1-10 mM
400 nM Intracerebral ventricular
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Miller S, et al. Autophagy. 2010, 6(6), 805-807.
[2] Canu et al (2005) Role of the autophagic-lysosomal system on low potassium-induced apoptosis in cultured cerebellar granule cells. J.Neurochem. 92 1228.
[3] Blommaart et al (1997) The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes. Eur.J.Biochem. 243 240.
[4] Seglen and Gordon (1982) 3-methyladenine: specific inhibitor of autophagic/lysosomal protein degradation in isolated rat hepatocytes. Proc.Natl.Acad.Sci. USA 79 1889.
分子式 C6H7N5 |
分子量 149.15 |
CAS号 5142-23-4 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 10 mg/mL |
Water 5 mg/mL |
Ethanol |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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