1. PI3K/Akt/mTOR
  2. PDK-1

BX795 

Cat. No.: HY-10514 Purity: 99.33%
Handling Instructions

BX795 is a potent and selective PDK1 inhibitor with an IC50 of 6 nM, showing 50-fold selectivity over PKA, PKC, c-Kit, GSK3β etc.

For research use only. We do not sell to patients.

BX795 Chemical Structure

BX795 Chemical Structure

CAS No. : 702675-74-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 94 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
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25 mg USD 288 In-stock
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50 mg USD 444 In-stock
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100 mg USD 600 In-stock
Estimated Time of Arrival: December 31
200 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
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Customer Review

    BX795 purchased from MCE. Usage Cited in: Autophagy. 2017 Jan 2;13(1):133-148.

    HeLa cells are treated with a BX795 TBK1 inhibitor (1 μM) and MG132 (10 μM) for 12 h. Cell lysates are analyzed by immunoblot analysis. Band intensities are measured, and phosphorylated-SQSTM1 values are normalized to total SQSTM1. The combined MG132/BX795 treatment results in a 90% reduction in S403 phosphorylation but has no effect on S349 phosphorylation.

    BX795 purchased from MCE. Usage Cited in: Mol Cell Proteomics. 2018 Sep 14. pii: mcp.RA118.000713.

    Relative A427 cell counts upon 96 hrs siRNA-mediated knockdown of PDPK1 and/or AURKA and/or 72 hrs treatment with 250 nM BX795. Data depicts three biological replicates each performed in technical triplicate.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    BX795 is a potent and selective PDK1 inhibitor with an IC50 of 6 nM, showing 50-fold selectivity over PKA, PKC, c-Kit, GSK3β etc.

    IC50 & Target

    IC50: 2 nM (TBK1), 6 nM (PDK1)

    In Vitro

    BX795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX795 potently inhibits tumor cell growth on plastic with IC50 of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116 and MiaPaca cells, respectively. In soft agar, BX795 displays higher growth inhibition with IC50 of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively[1]. In addition, BX795, as an inhibitor of the TBK1/IKKε, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β[2]. In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation[3]

    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6907 mL 8.4535 mL 16.9070 mL
    5 mM 0.3381 mL 1.6907 mL 3.3814 mL
    10 mM 0.1691 mL 0.8454 mL 1.6907 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1- and PtdIns-3,4-P2-mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contained: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P2-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 h at room temperature, the biotin-labeled peptide is captured from 10 μL of the assay mixture on streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay could sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2. To measure PDK1 activity directly, the final assay mixture (60 μL) contained 50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 0.1 mM EDTA, 0.1% β-mercaptoethanol, 1 mg/mL bovine serum albumin, 10 mM MgOAc, 10 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM substrate peptide (H2N-ARRRGVTTKTFCGT), and 60 ng of purified recombinant human PDK1. After 4 h at room temperature, we add 25 mM EDTA and spotted a portion of the reaction mixture on Whatman P81 phosphocellulose paper. The filter paper is washed three times with 0.75% phosphoric acid and once with acetone. After drying, the filter-bound labeled peptide is quantified using a Fuji phosphorimager.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Cells seeded at a low density (1,500-3,000 cells/well, 0.1 mL/well, 96-well plates) are incubated overnight. Compound treatments are made by adding 10 μL/well of the compound in 1% dimethyl sulfoxide and growth medium (final concentration of dimethyl sulfoxide, 0.1%), followed by brief shaking. Treated cells are incubated for 72 hours, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal. Results are reported as the average±S.E. of two or more replicates.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    591.47

    Formula

    C₂₃H₂₆IN₇O₂S

    CAS No.

    702675-74-9

    SMILES

    O=C(NCCCNC1=C(C=NC(NC2=CC=CC(NC(N3CCCC3)=O)=C2)=N1)I)C4=CC=CS4

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.33%

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    Product Name:
    BX795
    Cat. No.:
    HY-10514
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    BX795

    Cat. No.: HY-10514