An inhibitor of PDK1
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BX-517

Item No. 29238

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2,3-dihydro-2-oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-1H-indol-5-yl]-urea
CAS Number
850717-64-5
Synonyms
  • PDK1 Inhibitor II
Molecular Formula
C15H14N4O2
Formula Weight
282.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 14 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/mlEthanol: Partially soluble
λmax
221, 279, 297, 308, 396 nm
SMILES
O=C1/C(C2=CC(NC(N)=O)=CC=C2N1)=C(C3=CC=CN3)/C
InChi Code
InChI=1S/C15H14N4O2/c1-8(11-3-2-6-17-11)13-10-7-9(18-15(16)21)4-5-12(10)19-14(13)20/h2-7,17H,1H3,(H,19,20)(H3,16,18,21)/b13-8-
InChi Key
DFURSNCTQGJRRX-JYRVWZFOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $121

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    10 mg

    $215

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    25 mg

    $388

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    50 mg

    $713

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    Product Description

    BX-517 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50 = 6 nM).1 It binds to the ATP binding pocket of PDK1, inhibits Akt2 activation induced by PDK1 in a cell-free assay (IC50 = 20 nM), and inhibits Akt phosphorylation in PC3 cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Islam, I., Bryant, J., Chou, Y.-L., et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: Design, synthesis and biological activity. Bioorg. Med. Chem. Lett. 17(14), 3814-3818 (2007).

    2. Islam, I., Brown, G., Bryant, J., et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: Optimization of BX-517. Bioorg. Med. Chem. Lett. 17(14), 3819-3825 (2007).