PAK4-IN-2

• CAT Number: I043912
• CAS Number: 2488706-33-6
• Molecular Formula: C18H21ClN6
• Molecular Weight: 356.85
• Purity: ≥95%
• Synonyms: 4-N-(4-aminocyclohexyl)-2-N-(3-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
• InChI: InChI=1S/C18H21ClN6/c19-11-2-1-3-14(10-11)23-18-24-16-15(8-9-21-16)17(25-18)22-13-6-4-12(20)5-7-13/h1-3,8-10,12-13H,4-7,20H2,(H3,21,22,23,24,25)
• InChIKey: CJLQQZSGCYBOSS-UHFFFAOYSA-N
• SMILES: C1CC(CCC1N)NC2=NC(=NC3=C2C=CN3)NC4=CC(=CC=C4)Cl

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[1].
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].

Reference

[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.
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