产品
编 号:F601487
分子式:C19H15F3O5
分子量:380.31
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.

体外研究:
When PS210 induces a stabilization of PDK1 to the temperature gradien, PS210 stabilized the residue Arg131, located opposite to the helix a-B at the other extreme of the helix a-C. Thus, the residues forming part of the phosphate-binding site appear to be a fixed point that allows for the relative movement of the helices in the process of PDK1 activation.
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