2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. PAK Apoptosis
  4. PAK4-IN-2

PAK4-IN-2 is a highly potent PAK4 inhibitor with IC50 value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer.

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

PAK4-IN-2 Chemical Structure

PAK4-IN-2 Chemical Structure

CAS No. : 2488706-33-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 242 In-stock
Solution
10 mM * 1 mL in DMSO USD 242 In-stock
Solid
5 mg USD 220 In-stock
10 mg USD 360 In-stock
25 mg USD 720 In-stock
50 mg USD 1200 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

PAK4-IN-2 Related Antibodies

Top Publications Citing Use of Products

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

  • Biological Activity

  • Purity & Documentation

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Description

PAK4-IN-2 is a highly potent PAK4 inhibitor with IC50 value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer[1].

IC50 & Target

PAK3

2.7 nM (IC50)

In Vitro

PAK4-IN-2 (compound 5n) (0-10 μM; 72 hours) exhibits cell growth inhibition potency in hematoma tumor MV4-11 and solid tumor cell line MDA-MB-231, shows less sensitivity in normal human renal epithelial cell 239 T cell[1].
PAK4-IN-2 (5-50 nM; 48 hours) causes a majority of cells in G0/G1 phase with decreasing S-phase populations[1].
PAK4-IN-2 (10-250 nM; 48 hours) induces apoptosis in a dose-dependent manner[1].
PAK4-IN-2 (50-800 nM; 24 hours) markedly reduces the expression levels of p-PAK4(Ser474) in concentration dependently[1].

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

PAK4-IN-2 Related Antibodies

Cell Proliferation Assay

Cell Line: MV4-11, MDA-MB-231 and 293T[1]
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Exhibited significant cell growth inhibition potency in hematoma tumor MV4-11 (IC50 = 7.8 ± 2.8 nM), and moderate potent anti-proliferative effect in solid tumor cell line MDA-MB-231 (IC50 = 825 ± 106 nM), less sensitivity in normal human renal epithelial cell 239 T cell (IC50 > 10000 nM).

Cell Cycle Analysis

Cell Line: MV4-11[1]
Concentration: 5, 10 and 50 nM
Incubation Time: 48 hours
Result: Caused a majority of cells in G0/G1 phase with decreasing S-phase populations.

Apoptosis Analysis

Cell Line: MV4-11[1]
Concentration: 10, 50 and 250 nM
Incubation Time: 48 hours
Result: Induced apoptosis in a dose-dependent manner.

Western Blot Analysis

Cell Line: MV4-11[1]
Concentration: 50, 200 and 800 nM
Incubation Time: 24 hours
Result: Markedly reduced the expression levels of p-PAK4(Ser474) in concentration dependently.
Molecular Weight

356.85

Formula

C18H21ClN6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(NC2=NC(N[C@H]3CC[C@@H](N)CC3)=C4C(NC=C4)=N2)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (280.23 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 2.8023 mL 14.0115 mL 28.0230 mL
5 mM 0.5605 mL 2.8023 mL 5.6046 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 (protect from light). 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 (7.01 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 (7.01 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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

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 (protect from light). 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 2.8023 mL 14.0115 mL 28.0230 mL 70.0574 mL
5 mM 0.5605 mL 2.8023 mL 5.6046 mL 14.0115 mL
10 mM 0.2802 mL 1.4011 mL 2.8023 mL 7.0057 mL
15 mM 0.1868 mL 0.9341 mL 1.8682 mL 4.6705 mL
20 mM 0.1401 mL 0.7006 mL 1.4011 mL 3.5029 mL
25 mM 0.1121 mL 0.5605 mL 1.1209 mL 2.8023 mL
30 mM 0.0934 mL 0.4670 mL 0.9341 mL 2.3352 mL
40 mM 0.0701 mL 0.3503 mL 0.7006 mL 1.7514 mL
50 mM 0.0560 mL 0.2802 mL 0.5605 mL 1.4011 mL
60 mM 0.0467 mL 0.2335 mL 0.4670 mL 1.1676 mL
80 mM 0.0350 mL 0.1751 mL 0.3503 mL 0.8757 mL
100 mM 0.0280 mL 0.1401 mL 0.2802 mL 0.7006 mL
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PAK4-IN-2 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:

PAK4-IN-22488706-33-6PAKApoptosisp21 activated kinasesAnticancerCell cycleMV4-11MDA-MB-231Inhibitorinhibitorinhibit

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