1. PI3K/Akt/mTOR NF-κB Autophagy
  2. PDK-1 IKK Autophagy
  3. BX795

BX795 

Cat. No.: HY-10514 Purity: 98.93%
COA Handling Instructions

BX795 est un inhibiteur de PDK1 qui est puissant et sélectif, avec un IC50 de 6 nM. BX795 est également un inhibiteur de TBK1 et IKKɛ qui est puissant et relativement spécifique, avec un IC50 de 6 et 41 nM, respectivement. BX795 bloque la phosphorylation de S6K1, Akt, PKCδ et GSK3β, et a une sélectivité plus faible sur PKA, PKC, c-Kit, GSK3β etc. BX795 module l'autophagie.

BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.

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

BX795 Chemical Structure

BX795 Chemical Structure

CAS No. : 702675-74-9

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 103 In-stock
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10 mM * 1 mL in DMSO USD 103 In-stock
Solid
5 mg USD 79 In-stock
10 mg USD 145 In-stock
25 mg USD 317 In-stock
50 mg USD 488 In-stock
100 mg USD 660 In-stock
200 mg USD 1188 In-stock
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Customer Review

Based on 26 publication(s) in Google Scholar

Top Publications Citing Use of Products

    BX795 purchased from MedChemExpress. Usage Cited in: Nature. 2022 Oct;610(7933):761-767.  [Abstract]

    HeLa cells pretreated with DMSO or 2 µM BX795 for 24 h are stimulated with 2.5 µM diABZI or not and analysed by Western blot.

    BX795 purchased from MedChemExpress. Usage Cited in: Fitoterapia. 2019 Feb 4;134:14-22.  [Abstract]

    BT474 cells are exposed to protoapigenone, apigenin and BX-795 using different administration combination and analyzed by Western blot, β-actin was used as internal control.

    BX795 purchased from MedChemExpress. Usage Cited in: Fitoterapia. 2019 Feb 4;134:14-22.  [Abstract]

    MDA-MB-231 cells are exposed to protoapigenone, apigenin and BX-795 using different administration combination and analyzed by Western blot, β-actin was used as internal control.

    BX795 purchased from MedChemExpress. Usage Cited in: Mol Cell Proteomics. 2018 Dec;17(12):2434-2447.   [Abstract]

    Relative A427 cell counts upon 96 hrs siRNA-mediated knockdown of PDPK1 and/or AURKA and/or 72 hrs treatment with 250 nM BX795.

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

    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.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy[1][2][3][4].

    IC50 & Target[1][2]

    PDK1

    6 nM (IC50)

    TBK1

    6 nM (IC50)

    IKKε

    41 nM (IC50)

    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].

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

    Molecular Weight

    591.47

    Appearance

    Solid

    Formula

    C23H26IN7O2S

    CAS No.
    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 33.33 mg/mL (56.35 mM; Need ultrasonic)

    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.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.23 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.23 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.06%

    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
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    BX795 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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