PAK4-IN-2
Based on 1 Customer Validation
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.
- Purity: 99.42%
- CAS No.: 2488706-33-6
- Formula: C18H21ClN6
- Molecular Weight:356.85
-
Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Apoptosis Compound Library
HY-L003
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Kinase Inhibitor Library
HY-L009
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Cytoskeleton Compound Library
HY-L060
-
Heterocyclic Compound Library
HY-L138
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Biological Activity
|
PAK4 2.7 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
>10000 nM
Compound: 5n
|
Cytotoxicity against HEK293T cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay
Cytotoxicity against HEK293T cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay
|
[PMID: 35272236] |
| MDA-MB-231 | IC50 |
825 nM
Compound: 5n
|
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay
|
[PMID: 35272236] |
| MV4-11 | IC50 |
7.8 nM
Compound: 5n
|
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by cell titre glo luminescence assay
|
[PMID: 35272236] |
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.
-
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 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.
-
Cell Line:MV4-11[1]
-
Concentration:10, 50 and 250 nM
-
Incubation Time:48 hours
-
Result:Induced apoptosis in a dose-dependent manner.
-
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.
Chemical Information
-
CAS No. 2488706-33-6
-
Appearance Solid
-
Molecular Weight 356.85
-
Formula C18H21ClN6
-
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
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Data Sheet (278 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
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 |
PAK4-IN-2 Related Classifications
HY-143490 Related Classifications
Powered by Bioz