生物活性

• 靶点

  PIK3C3 IC50:25μM

  PI3Kγ IC50:60μM

• 描述Vps34 is one kind of PI3K isoform, which plays an essential role in endosomal trafficking of proteins to the vacuole/lysosome, autophagy and phagocytosis. 3-Methyladenine (3-MA) shows inhibition of Vps34 in vitro, with an IC50 of 25 μM as compared with 60 μM for PI3Kγ. 3-Methyladenine is typically employed at a concentration of 10 mM in cellular studies^[1]. It is usually served as the inhibitor for both autophagy^[1] and type 1 mitophagy through suppression of class III PI3K activity ^[2]. However, now it was found that 3-Methyladenine play a dual role in modulation of autophagy. Prolonged treatment with 3-Methyladenine (5mM) up to 9 h can induce LC3 I to II conversion in wild type MEFs, L929 and 293T cells cultured in full-medium, whereas it is still effective in suppressing LC3 II conversation in cells induced by starvation. And this observation is consistent with result of punctuate formation of GFP-LC3 study. These results demonstrate that prolonged treatment with 3-Methyladenine under nutrient-rich conditions can enhance autophagic flux. This may due to its different temporal patterns of inhibition on Class I and III PI3K^[3].
• 作用机制May due to the specific hydrophobic ring to Vps34 encircles the 3-methyl group of 3-MA.^[1]

• 动物研究
  动物给药方法	Rats: 15 mg/kg[4] Mice: 35 mg/kg[5]
  剂量	Mice: 35 mg/kg[5] Rats: 15 mg/kg[4]
  给药途径	i.v., i.p.