PI-103

  • 化学数据
CAS号 371935-74-9 货号 BCP01923
中文名 PI-103
英文名 PI-103
中文别名
英文别名 PI 103;PI103;
分子式 C19H16N4O3 分子量 348.36
  • 用途
生物活性 PI-103 potently inhibits both the rapamycin-sensitive (mTORC1) and rapamycin-insensitive (mTORC2) complexes of the protein kinase mTOR. PI-103 inhibits constitutive and growth factor-induced PI3K/Akt, as well as mTORC1 activation. In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells. PI-103 inhibits p110α >200-fold more potently than p110β. PI-103 also potently blocks production of PI(3,4)P2 and PIP3 in adipocytes and PIP3 in myotubes.PI-103 inhibits phosphorylation of Akt with an IC95 100-fold lower than that for LY294002. Strikingly, PI-103 completely protects animals from insulin-stimulated decline in blood glucose. PI-103 has additive proapoptotic effects with etoposide in blast cells and in immature leukemic cells.
上下游产品 371935-79-4(PI-103 Hydrochloride) PI-103(PI-103氢溴酸盐)
信号通路 Cell Cycle/DNA Damage PI3K/Akt/mTOR 
靶 点 DNA PK PI3K mTOR 

结构式

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