2. PI3K/Akt/mTOR
  3. PDK-1
  4. PS48

PS48 is an activator of PDK1 with an AC50 of 8 μM.

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

PS48 Chemical Structure

PS48 Chemical Structure

CAS No. : 1180676-32-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 80 In-stock
25 mg USD 150 In-stock
50 mg USD 220 In-stock
100 mg   Get quote  
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Customer Review

Based on 6 publication(s) in Google Scholar

PS48 Related Antibodies

Top Publications Citing Use of Products

    PS48 purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2017 Sep 21;13(10):1266-1275.  [Abstract]

    Suppression of PDK1/Akt/mTOR pathway by TP in HG-treated HRMCs was also reversed by PS48.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PS48 is an activator of PDK1 with an AC50 of 8 μM.

    IC50 & Target

    AC50: 8 μM (PDK1)[1]
    In Vitro

    PS48 activates full length PDK1 (His-PDK1- FL) and PDK1 50-359[Tyr288Gly;Gln292Ala] (His-PDK1 dm) with AC50s (the concentrations required to reach 50% of the maximal activation) of 7.95±0.2 and 10.0±2.0 μM, respectively. PS48 binds to PDK150–359 with a 1:1 stoichiometry and a binding affinity in the micromolar range (Kd=10.3 μM)[1]. PDK1 activator, PS48, has the ability to reverse the cell proliferation inhibition role of triptolide (TP) in vitro. The inhibition role of TP in cell number is significantly reversed by PS48. TP significantly increases the cell proportion in G0-G1 phase and decreases the cell proportion in G2-M and S phase. However, the effect of TP on cell cycle distribution is all reversed by PS48. In addition, suppression of PDK1/Akt/mTOR pathway by TP in high glucose (HG)-treated human renal mesangial cells (HRMCs) is also reversed by PS48, as well as the expression of Ki-67 and proliferating cell nuclear antigen (PCNA)[2].

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

    PS48 Related Antibodies
    Molecular Weight

    286.75

    Formula

    C17H15ClO2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)/C=C(C1=CC=CC=C1)/CCC2=CC=C(Cl)C=C2
    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 : 100 mg/mL (348.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.4874 mL 17.4368 mL 34.8736 mL
    5 mM 0.6975 mL 3.4874 mL 6.9747 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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 (8.72 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (8.72 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Purity & Documentation
    References
    Kinase Assay
    [1]

    PDK1 activity tests are performed using T308tide as a substrate for PDK1. In brief, PDK1 activity assay is performed at room temperature (22°C) in a 20 μL mix containing 50 mM Tris pH 7.5, 0.05 mg/mL BSA, 0.1% β-mercaptoethanol, 10 mM MgCl2, 100 μM [γ32P]ATP (5-50 cpm/pmol) , 0.003% Brij, 150-500 ng PDK1, and T308tide (from 0.1 to 1 mM). When appropriate, the PDK1 activity assay is performed in a 96 well format and 4 μL aliquots spotted on p81 phosphocellulose papers using ep motion 5070, washed in 0.01% phosphoric acid, dried, and then exposed and analysed using PhosphoImager technology. Activity measurements are performed in duplicates or triplicates with less than 10% difference between replicates. Experiments are repeated at least twice[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [2]

    Human renal mesangial cells (HRMCs) are cultured with 1640 media, containing 10% fetal bovin serum at 37 °C in 5% CO2. Cells are cultured with D-glucose at normal (5.5 mM) or high (25 mM) concentrations in serum-free medium. D-Mannitol (25 mM) is used for a control of osmolality. TP is reconstituted in 0.01% DMSO and freshly diluted with culture medium to 10 ug/L before using. To determine the specific role of PDK1 in TP-potentiated anti-proliferation, 5 μM PS48 (MedChem Express, USA) is applied following the treatment of TP. MTT assay is used to detect cell proliferation. HRMCs are seeded at a density of 1x105/mL into 96-well plates. After 12, 24, 48 and 72 h incubation with different compounds, 20 uL MTT (5 mg/mL) is added to each well. Cells are then cultured for an additional 2 h and subsequently lysed using DMSO (150 uL/well). When the formazan crystals completely dissolve, the optical density (OD) is measured at 570 nm. The arithmetic mean OD of six wells for each group is calculated[2].

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

    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 3.4874 mL 17.4368 mL 34.8736 mL 87.1840 mL
    5 mM 0.6975 mL 3.4874 mL 6.9747 mL 17.4368 mL
    10 mM 0.3487 mL 1.7437 mL 3.4874 mL 8.7184 mL
    15 mM 0.2325 mL 1.1625 mL 2.3249 mL 5.8123 mL
    20 mM 0.1744 mL 0.8718 mL 1.7437 mL 4.3592 mL
    25 mM 0.1395 mL 0.6975 mL 1.3949 mL 3.4874 mL
    30 mM 0.1162 mL 0.5812 mL 1.1625 mL 2.9061 mL
    40 mM 0.0872 mL 0.4359 mL 0.8718 mL 2.1796 mL
    50 mM 0.0697 mL 0.3487 mL 0.6975 mL 1.7437 mL
    60 mM 0.0581 mL 0.2906 mL 0.5812 mL 1.4531 mL
    80 mM 0.0436 mL 0.2180 mL 0.4359 mL 1.0898 mL
    100 mM 0.0349 mL 0.1744 mL 0.3487 mL 0.8718 mL
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    PS48 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.

    Keywords:

    PS481180676-32-7PS 48PS-48PDK-13-Phosphoinositide-dependent protein kinase 1Inhibitorinhibitorinhibit

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