2. Cell Cycle/DNA Damage Cytoskeleton
  3. PAK
  4. IPA-3

IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).

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

IPA-3 Chemical Structure

IPA-3 Chemical Structure

CAS No. : 42521-82-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 55 In-stock
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50 mg USD 286 In-stock
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Customer Review

Based on 16 publication(s) in Google Scholar

IPA-3 Related Antibodies

Top Publications Citing Use of Products

    IPA-3 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 May 9;8(19):31802-31814.  [Abstract]

    Activation of the β-catenin signaling pathway by Fn (F01) can be inhibited by both the TLR4 inhibitor (TAK-242) and PAK1 inhibitor (IPA-3).

    View All PAK Isoform Specific Products:

    View All Isoforms
    PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).

    IC50 & Target[3]

    PAK1

    2.5 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    > 10000 nM
    Compound: IPA-3
    Inhibition of full length PAK5 (unknown origin) expressed in HEK293 cells assessed as phosphate incorporation onto MBP preincubated for 5 mins followed by Cdc42, MBP, and mixture of ATP and [32P]-gamma-ATP addition measured after 20 mins by scintillation
    Inhibition of full length PAK5 (unknown origin) expressed in HEK293 cells assessed as phosphate incorporation onto MBP preincubated for 5 mins followed by Cdc42, MBP, and mixture of ATP and [32P]-gamma-ATP addition measured after 20 mins by scintillation
    		[PMID: 26191365]
    In Vitro

    IPA-3 inhibits Pak1 activation in part by binding covalently to the regulatory domain of Pak1. IPA-3 binds Pak1 covalently in a time- and temperature-dependent manner. IPA-3 prevents binding of the Pak1 activator Cdc42. IPA-3 binds directly to the Pak1 autoregulatory domain. IPA-3 reversibly inhibits PMA-induced membrane ruffling in cells[1]. IPA-3 (2 μM, 5 μM or 20 μM) reduces cell spreading in human primary Schwann and schwannoma cells. IPA-3 treatment significantly reduces the number of adherent Schwann and schwannoma cells in a dose-dependent manner[2]. IPA-3 is a non ATP-competitive, allosteric inhibitor of p21-activated kinase 1 (Pak1). PIR3.5 is the control compound of IPA-3. IPA-3 prevents Cdc42-stimulated Pak1 autophosphorylation on Thr423. IPA-3 also prevents sphingosine-dependent Pak1 autophosphorylation. IPA-3 does not target exposed cysteine residues on Pak1. The disulfide bond of IPA-3 is critical for inhibition of Pak1 and in vitro reduction by the reducing agent dithiothreitol (DTT) abolishes Pak1 inhibition by IPA-3. IPA-3 inhibits activation of Pak1 by diverse activators, but does not inhibit preactivated Pak1. IPA-3 inhibits PDGF-stimulated Pak activation in mouse embryonic fibroblasts[3].

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

    IPA-3 Related Antibodies
    Molecular Weight

    350.45

    Formula

    C20H14O2S2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    OC1=CC=C2C=CC=CC2=C1SSC3=C4C=CC=CC4=CC=C3O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 41.67 mg/mL (118.90 mM; ultrasonic and warming and heat to 60°C; 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 2.8535 mL 14.2674 mL 28.5347 mL
    5 mM 0.5707 mL 2.8535 mL 5.7069 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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 (7.13 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      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 (7.13 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      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

    Purity: 99.43%

    SDS (560 KB)

    COA (257 KB) RP-HPLC (221 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Pak1 (150 nM final) is pre-incubated with MBP (8.3 μM), indicated proteins, and IPA-3 or DMSO in Kinase buffer for 20 minutes at 4°C. Cdc42-GTPγS (3.2 μM) is then added and the reaction is pre-equilibrated 10 minutes at 30°C. Kinase reactions are started by the addition of ATP (to 30 μM) containing [32P]ATP and are incubated 10 min and analyzed by SDS-PAGE and autoradiography.

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

    Human primary schwannoma cells are grown on 96 well plates for 2 days. Cells are left untreated or treated with 5 µM IPA-3, 20 µM IPA-3 or 20 µM PIR-3.5 for 24 hours. The MTS-solution is left on the cells for 3 hours, before the absorbance at 490 nm is measured. The experiments are conducted three times and mean and standard error of the mean is calculated with Excel.

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8535 mL 14.2674 mL 28.5347 mL 71.3369 mL
    5 mM 0.5707 mL 2.8535 mL 5.7069 mL 14.2674 mL
    10 mM 0.2853 mL 1.4267 mL 2.8535 mL 7.1337 mL
    15 mM 0.1902 mL 0.9512 mL 1.9023 mL 4.7558 mL
    20 mM 0.1427 mL 0.7134 mL 1.4267 mL 3.5668 mL
    25 mM 0.1141 mL 0.5707 mL 1.1414 mL 2.8535 mL
    30 mM 0.0951 mL 0.4756 mL 0.9512 mL 2.3779 mL
    40 mM 0.0713 mL 0.3567 mL 0.7134 mL 1.7834 mL
    50 mM 0.0571 mL 0.2853 mL 0.5707 mL 1.4267 mL
    60 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1889 mL
    80 mM 0.0357 mL 0.1783 mL 0.3567 mL 0.8917 mL
    100 mM 0.0285 mL 0.1427 mL 0.2853 mL 0.7134 mL
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    IPA-3 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:

    IPA-342521-82-4IPA3IPA 3PAKp21 activated kinasesInhibitorinhibitorinhibit

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