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.).
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- Formule: C31H28ClN5O
- Masse moléculaire:522.04
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
Chemical Information
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Masse moléculaire 522.04
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Formule C31H28ClN5O
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PAK4-IN-5 Related Classifications
HY-159897 Related Classifications
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