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PAK4-IN-5

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.) [1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; LIM Kinase (LIMK) ; PAK; Reactive Oxygen Species (ROS)

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pak4-in-5.html

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

Molecular Formula

C31H28ClN5O

Molecular Weight

522.04

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

PAK1; PAK4

Frequently Asked Questions

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