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PDK-1
3-Phosphoinositide-dependent protein kinase 1
PDK-1 (3-Phosphoinositide-dependent protein kinase 1), a member of the protein A, G and C (AGC) family of proteins, is a Ser/Thr
protein kinase. PDK-1, is the pivotal node in the PI3K pathway, has a key role in insulin and growth-factor signalling through
phosphorylation and subsequent activation of a number of other AGC kinase family members, such as protein kinase B.
PDK-1 is responsible for the regulation of cell proliferation and migration and it also has been found to play a key role in different
cancers, pancreatic and breast cancer amongst others. Many cancer-driving mutations induce activation of PDK-1 targets including
Akt, S6K (p70 ribosomal S6 kinase) and SGK. Thus, PDK1 is a critical activator of multiple pro-survival and oncogenic protein
kinases, for which it has garnered considerable interest as an oncology drug target.
www.MedChemE 1
PDK-1 Inhibitors Activators
(R)-PS210 BX-320
Cat. No.: HY-13856 Cat. No.: HY-10515
(R)-PS210, the R enantiomer of PS210 (compound BX-320 is a selective, ATP-competitive, orally
4h-eutomer), is a substrate-selective allosteric acitive, and direct PDK1 inhibitor with an IC50
activator of PDK1 with an AC50 value of 1.8 μM. of 30 nM in a direct kinase assay format. BX-320
(R)-PS210 targets to the PIF-binding pocket also induces apoptosis. Anticancer effect.
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