PAK4-IN-5

Cat. No.: HY-159897: FAQs
Data Sheet Handling Instructions

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PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC₅₀: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD₅₀: >500 mg/kg for mice (p.o.).

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

PAK4-IN-5 Chemical Structure

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•Related Small Molecules:

•Related Proteins:

View All PAK Isoform Specific Products:

View All Isoforms

PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

View All LIM Kinase (LIMK) Isoform Specific Products:

View All Isoforms

LIMK1 LIMK2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PAK4

7.68 nM (IC₅₀)

PAK1

1872.01 nM (IC₅₀)

In Vitro

PAK4-IN-5 inhibits cell proliferation with IC₅₀s of 1.87 (A-549), 1.56 (NCI-H1975), 1.21 (MDA-MB-231), 2.33 (SK-BR-3), 28.68 μM (Beas-2B), 26.68 μM (MCF-10A), respectively^[1].

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

Molecular Weight

522.04

Formula

C₃₁H₂₈ClN₅O

SMILES

CN1CCN(C2=CC=C(C3=CC=C(N=C(C4=CC=C(C(NC5=CC=CC(Cl)=C5)=O)C=C4)N6)C6=C3)C=C2)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Hao S, et al. Design, synthesis and biological evaluation of novel benzimidazole-derived p21-activited kinase 4 (PAK4) inhibitors bearing a 4-(4-methylpiperazin-1-yl)phenyl scaffold as potential antitumor agents. Eur J Med Chem. 2024 Oct 17;280:116971.

[2]. Meng FH. Design, synthesis and biological evaluation of novel benzimidazole-derived p21-activited kinase 4 (PAK4) inhibitors bearing a 4-(4-methylpiperazin-1-yl)phenyl scaffold as potential antitumor agents. Eur J Med Chem. 2024 Oct 17;280:116971.

PAK4-IN-5 Related Classifications

Cancer

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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-5PAKLIM Kinase (LIMK)ApoptosisReactive Oxygen Speciesp21 activated kinasesLIMKsMDA-MB-231breast cancerInhibitorinhibitorinhibit

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