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SAR405

CAS No. : 1523406-39-4

MCE 国际站：SAR405

产品活性：SAR405 是首创的，选择性的，具有ATP竞争性的 PI3K III (PIK3C3) 亚型 Vps34 抑制剂 (IC₅₀=1.2 nM; K_d =1.5 nM)。SAR405 抑制饥饿或 mTOR 抑制诱导的自噬。具有抗癌活性。

研究领域：PI3K/Akt/mTOR  |  Autophagy

作用靶点：PI3K  |  Autophagy

In Vitro: The activity of SAR405 is next evaluated on a dedicated Vps34 cellular assay using a GFP-FYVE–transfected HeLa cell line.
SAR405 prevents autophagy and synergizes with mTOR inhibition in tumor cells. SAR405 prevents autophagosome formation with an IC₅₀ of 42 nM. Treatment of starved cells with SAR405 completely inhibits the conversion to LC3-II in a dose-dependent manner. The effect of SAR405 on autophagy is then investigated. The GFP-LC3 model is used for the HTS and confirmed its activity on starved cells (IC₅₀=419 nM). The conversion of LC3-I into LC3-II is also analyzed by western blotting on wild-type HeLa and H1299 cells.

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