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BX795

CAS No. : 702675-74-9

MCE 国际站：BX795

产品活性：BX795 是一种有效的、选择性的 PDK1 抑制剂，IC₅₀ 值为 6 nM。同时，BX795 为有效、相对特异性的TBK1 和 IKK? 的抑制剂，IC₅₀ 值分别为 6 和 41 nM。BX795 抑制 S6K1，Akt，PKCδ 和 GSK3β 的磷酸化。BX795 对 PKA，PKC，c-Kit，GSK3β 选择性较低。BX795 可调节自噬 (autophagy)。

研究领域：PI3K/Akt/mTOR  |  NF-κB  |  Autophagy

作用靶点：PDK-1  |  IKK  |  Autophagy

In Vitro: BX795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX795 potently inhibits tumor cell growth on plastic with IC₅₀ of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116, and MiaPaca cells, respectively.
In soft agar, BX795 displays higher growth inhibition with IC₅₀ of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively.
In addition, BX795, as an inhibitor of the TBK1/IKKε, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β. In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion, and thromboxane generation.

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