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

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.

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CAS 番号 : 702675-74-9

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 103 在庫あり
Solid
5 mg $79 在庫あり
10 mg $145 在庫あり
25 mg $317 在庫あり
50 mg $488 在庫あり
100 mg $660 在庫あり
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カスタマーレビュー

Based on 38 publication(s) in Google Scholar

Other Forms of BX795:

BX795 関連抗体

Top Publications Citing Use of Products

顧客検証

WB

    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 Apr: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 Apr: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.

    IKK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    IKK-α IKK-β IKK IKKε TBK1

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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)

    Cellular Effect
    Cell Line Type Value Description References
    HeLa CC50
    46 3
    Compound: 73; BX795
    Cytotoxicity against human HeLa cells
    Cytotoxicity against human HeLa cells
    		[PMID: 33539089]
    HeLa CC50
    46 3
    Compound: 73; BX795
    Cytotoxicity against human HeLa cells
    Cytotoxicity against human HeLa cells
    		[PMID: 33539089]
    体外実験

    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.

    BX795 関連抗体
    分子量

    591.47

    分子式

    C23H26IN7O2S
    CAS 番号
    Appearance

    Solid

    Color

    White to light brown

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 33.33 mg/mL (56.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    一般には略語で表示されます：C1V1 = C2V2

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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    Please enter the basic information of animal experiments:

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    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.84%

    COA (244 KB) HNMR (277 KB) RP-HPLC (245 KB) LCMS (93 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6907 mL 8.4535 mL 16.9070 mL 42.2676 mL
    5 mM 0.3381 mL 1.6907 mL 3.3814 mL 8.4535 mL
    10 mM 0.1691 mL 0.8454 mL 1.6907 mL 4.2268 mL
    15 mM 0.1127 mL 0.5636 mL 1.1271 mL 2.8178 mL
    20 mM 0.0845 mL 0.4227 mL 0.8454 mL 2.1134 mL
    25 mM 0.0676 mL 0.3381 mL 0.6763 mL 1.6907 mL
    30 mM 0.0564 mL 0.2818 mL 0.5636 mL 1.4089 mL
    40 mM 0.0423 mL 0.2113 mL 0.4227 mL 1.0567 mL
    50 mM 0.0338 mL 0.1691 mL 0.3381 mL 0.8454 mL
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    BX795 Related Classifications

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    Keywords:

    BX795702675-74-9BX 795BX-795PDK-1IKKAutophagy3-Phosphoinositide-dependent protein kinase 1IκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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    製品番号:
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