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BX795 702675-74-9

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Synonyms ：
Appearance ：
Chemical Formula ：
C23H26IN7O2S
Solubility ：
Molecular Weight ：
591.47
Storage and Stability ：
in stock
CAS No. ：
702675-74-9
Purity ：
98%+
Introduction
BX795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1.

BX-795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX-795 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, BX-795 displays higher growth inhibition with IC50 of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively. [1] In addition, BX-795, as an inhibitor of the TBK1/IKKɛ, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β. [2] In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation. [3]

 
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