Name: BX517(PDK1 inhibitor2)
Price: 241.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    BX-517 is a potent and selective inhibitor of PDK1 that binds to the ATP binding pocket
    of the protein (IC50 = 6 nM). BX-517 also blocks activation of Akt in tumor cells with 10-fold more potent (IC50 = 0.1–1.0 μM) than its analogs tested at the highest dose tested (10 μM). [1] The phosphoinositide-dependent kinase-1 (PDK1) is a Ser/Thr kinase that is a crucial activator of a range of protein kinases in the AGC kinase super-family that play key roles in the progression of cancer and for the activation of Akt, S6 kinase, and protein kinase C. [2]
    
    1. Islam I, Brown G, Bryant J et al. Indolinone based phosphoinositide-dependentkinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517. Bioorg Med Chem Lett.2007 Jul 15;17(14):3819-25.
    2. Islam I, Bryant J, Chou YL etc. Indolinone based phosphoinositide-dependent kinase-1 (PDK1)inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8.
- Properties
  - Alternative Name
    
    (Z)-N-(3-(1-(1H-pyrrol-2-yl)ethylidene)-2-hydroxy-3H-indol-5-yl)carbamimidic acid
    
    CAS Number
    
    850717-64-5
    
    Molecular Formula
    
    C15H14N4O2
    
    Molecular Weight
    
    282.3
    
    Appearance
    
    A solid
    
    Purity
    
    98.61%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥8.55 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

BX517(PDK1 inhibitor2)

BX517(PDK1 inhibitor2)

Background

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