2. Cell Cycle/DNA Damage Cytoskeleton
  3. PAK
  4. NVS-PAK1-1

NVS-PAK1-1, a chemical probe, is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.

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

CAS No. : 1783816-74-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of NVS-PAK1-1:

NVS-PAK1-1 Related Antibodies

Top Publications Citing Use of Products

    NVS-PAK1-1 purchased from MedChemExpress. Usage Cited in: PLoS One. 2024 Jul 31;19(7):e0305121.  [Abstract]

    NVS-PAK1-1 (0-10 μM; 72 h) inhibited HEI-193 cell viability by CellTiter-Glo.

    NVS-PAK1-1 purchased from MedChemExpress. Usage Cited in: PLoS One. 2024 Jul 31;19(7):e0305121.  [Abstract]

    NVS-PAK1-1 (2, 5 μM; 4, 72 h) decreased the protein expression of phospho-PAK1/2 (S144/S141) in HEI-193 cells.

    NVS-PAK1-1 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Jun 11.

    Measure of protein expression by median fluorescence intensity (MFI) of CD137 or CD69 surface markers in flow cytometry of T cells treated with NVS-PAK1-1 (10uM or 20uM) or DMSO for 5 days.

    View All PAK Isoform Specific Products:

    View All Isoforms
    PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NVS-PAK1-1, a chemical probe, is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM[1].

    IC50 & Target

    IC50: 5 nM (PAK1)[1]
    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    0.25 μM
    Compound: 3, NOV-3
    Growth inhibition of human A549 cells
    Growth inhibition of human A549 cells
    		[PMID: 28814374]
    In Vitro

    NVS-PAK1-1 demonstrates high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 Kd of 7 nM and a PAK2 Kd of 400 nM. NVS-PAK1-1 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases. NVS-PAK1-1 at 6-20 μM inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Consistent with the observation, NVS-PAK1-1 inhibits proliferation of Su86.86 cell line only above a concentration of 2 μM. In contrast, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, inhibition of downstream signaling and cell proliferation at a significantly lower 0.21 μM concentration are achieved[1].

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

    NVS-PAK1-1 Related Antibodies
    In Vivo

    NVS-PAK1-1 shows a relatively poor stability in rat liver microsomes (RLM) and this would limit its application for in vivo studies (t1/2 in RLM 3.5 min)[1].

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

    479.93

    Formula

    C23H25ClF3N5O
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    FC1=CC2=C(C=C1)N(CC(F)F)C3=C(C=C(Cl)C=C3)C(N[C@H]4CCN(C(NC(C)C)=O)C4)=N2
    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 : 100 mg/mL (208.36 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 2.0836 mL 10.4182 mL 20.8364 mL
    5 mM 0.4167 mL 2.0836 mL 4.1673 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 (5.21 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 (5.21 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.

    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: 99.85%

    SDS (393 KB)

    COA (253 KB) HNMR (169 KB) RP-HPLC (244 KB) MS (179 KB)

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

    Inhibition of PAK1 kinase activity is measured using the Caliper assay. The assay is performed using 384-well microtiter plates. Compounds (NVS-PAK1-1) are tested as 8-point dose responses. The assays are prepared by addition of 50 nL of compound solution in 90% DMSO directly into the empty plate. Subsequently, 4.5 µL of the enzyme solution is added to each well and the resulting solution is pre-incubated at 30°C for 60 min, followed by addition of 4.5 µL of the peptide/ATP-solution. After 60 min incubation at 30°C, reactions are terminated by addition of 16 μL per well of the stop solution. Plates with terminated kinase reactions are transferred to the Caliper LC3000 workstations for reading. Product formation is measured in a microfluidic mobility shift assay. IC50 values are derived from percent inhibition values at different compound concentrations by non-linear regression analysis[1].

    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 2.0836 mL 10.4182 mL 20.8364 mL 52.0909 mL
    5 mM 0.4167 mL 2.0836 mL 4.1673 mL 10.4182 mL
    10 mM 0.2084 mL 1.0418 mL 2.0836 mL 5.2091 mL
    15 mM 0.1389 mL 0.6945 mL 1.3891 mL 3.4727 mL
    20 mM 0.1042 mL 0.5209 mL 1.0418 mL 2.6045 mL
    25 mM 0.0833 mL 0.4167 mL 0.8335 mL 2.0836 mL
    30 mM 0.0695 mL 0.3473 mL 0.6945 mL 1.7364 mL
    40 mM 0.0521 mL 0.2605 mL 0.5209 mL 1.3023 mL
    50 mM 0.0417 mL 0.2084 mL 0.4167 mL 1.0418 mL
    60 mM 0.0347 mL 0.1736 mL 0.3473 mL 0.8682 mL
    80 mM 0.0260 mL 0.1302 mL 0.2605 mL 0.6511 mL
    100 mM 0.0208 mL 0.1042 mL 0.2084 mL 0.5209 mL
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    NVS-PAK1-1 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:

    NVS-PAK1-11783816-74-9PAKp21 activated kinasesInhibitorinhibitorinhibit

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