PI-103
| 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 |
| 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 | ||
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mTOR complex-2 stimulates acetyl-CoA and de novo lipogenesis through ATP citrate lyase in HER2/PIK3CA-hyperactive breast cancer
购于瀚香生物(Biochempartner)的PI-103(CAS:371935-74-9)被引用 |
结构式
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