PDK-1

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PDK-1 Inhibitors (5)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1106 OSU-03012 (AR-12) OSU-03012 (AR-12) is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM in a cell-free assay and 2-fold increase in potency over OSU-02067.
  • Mol Cancer Ther, 2014, 13(10):2384-98
  • J Biol Chem, 2014, jbc.M114.595728
  • Mol Cell Endocrinology, 2015, 10.1016/j.mce.2015.04.008
S1274 BX-795 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.
  • Proc Natl Acad Sci USA, 2014, 111(49):17438-43
  • FEBS J, 2014, 281(17):3816-27
  • Virology, 2014, 450-451:182-95
S1275 BX-912 BX912 is a potent and specific PDK1 inhibitor with IC50 of 12 nM, 9- and 105- fold greater selectivity for PDK1 than PKA and PKC in cell-free assays, respectively. In comparison to GSK3β, selectivity for PDK1 is 600-fold.
  • Oncotarget, 2014, 5(21):10732-44
  • J Immunol, 2016, 197(4):1137-47
  • University Gattingen, 2013, 8
S7087 GSK2334470 GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM in a cell-free assay, with no activity at other close related AGC-kinases.
  • Oncotarget, 2014, 5(10):3145-58
S1556 PHT-427 PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with Ki of 2.7 μM and 5.2 μM, respectively.
  • Blood, 2011, 118(10):2840-8
  • Free Radic Res, 2015, 49(9):1095-113
  • Eur J Pharmacol, 2015, 747C:71-87

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1106 OSU-03012 (AR-12) <1 mg/mL 11 mg/mL <1 mg/mL
S1274 BX-795 <1 mg/mL 100 mg/mL <1 mg/mL
S1275 BX-912 <1 mg/mL 94 mg/mL 94 mg/mL
S7087 GSK2334470 <1 mg/mL 90 mg/mL 90 mg/mL
S1556 PHT-427 <1 mg/mL 82 mg/mL 60 mg/mL
Tags: PDK1 kinase | PDK1 assay | PDK1 activation | PDK1 phosphorylation | PDK1 cancer | PDK1 signaling | PDK1 inhibitor review
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