PAK4-IN-2

Name: PAK4-IN-2
Brand: MedChemExpress
SKU: HY-143490
Rating: 4.5 (1 reviews)

Cat. No.: HY-143490 Purity: 99.78%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 2488706-33-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 242	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 242	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 720	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

PAK3

2.7 nM (IC₅₀)

Cellular Effect

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]

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.

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.

2488706-33-6

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
10 mM	0.2802 mL	1.4011 mL	2.8023 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.01 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)

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

Purity: 99.78%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (253 KB) HNMR (427 KB) RP-HPLC (127 KB) LCMS (142 KB)

Handling Instructions (2659 KB)

References

[1]. Wang C, Xia J, Lei Y, et al. Synthesis and biological evaluation of 7H-pyrrolo [2,3-d] pyrimidine derivatives as potential p21-activated kinase 4 (PAK4) inhibitors. Bioorg Med Chem. 2022;60:116700. [Content Brief]

Complete Stock Solution Preparation Table

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

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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PAK4-IN-2

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Purity & Documentation

References

Customer Review

PAK4-IN-2 Related Antibodies

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Complete Stock Solution Preparation Table

PAK4-IN-2 Related Classifications

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