PAK1 Inhibitor

2,2′-Dihydroxy-6,6′-dinaphthyl disulfide (PIR-3.5) is a PAK1 inhibitor.

AZ13711265 is an orally active PAK1 inhibitor with high selectivity. AZ13711265 has IC₅₀ values of 0.58 nM and 0.11 µM for PAK1 and pPAK1, respectively. AZ13711265 has low lipophilicity and low clearance, and can be used as an in vivo probe compound for PAK1. AZ13711265 can be used in the study of cancer.

Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.

YDH-704 is a PAK1/HDAC10 inhibitor, with IC₅₀ values of 0.05 μM and 0.02 μM against human targets, respectively. YDH-704 blocks PAK1-mediated oncogenic signaling pathways, inhibits the proliferation and migration of tumor cells, suppresses the epigenetic regulatory function of HDAC10, downregulates PD-L1 expression, and regulates polyamine metabolism. YDH-704 reduces MDSC/Treg infiltration, enhances the infiltration and activation of CD8⁺ T cells, and inhibits tumor growth and lung metastasis. YDH-704 can be used for research on triple-negative breast cancer.

ZINC194100678 is a potent PAK1 inhibitor with an IC₅₀ value of 8.37 μM. ZINC194100678 can inhibit MDA-MB-231 cell proliferation. ZINC194100678 can be used for researching anticancer.

ZMF-10 is a highly potent PAK1 inhibitor, with IC₅₀s of 174 nM, 1.038 μM and 1.372 μM for PAK1, PAK2 and PAK3, respectively. ZMF-10 can inhibit PAK1 activity to affect PAK1-regulated apoptosis, ER-Stress and migration in MDA-MB-231 cells. ZMF-10 can be used for researching anticancer.

PAK1-IN-2 (Compound 35) is a selective PAK1 inhibitor with a K_i of 7.3 nM. PAK1-IN-2 can inhibit MEK phosphorylation. PAK1-IN-2 has significant inhibitory effects on PAK1/4 amplified cancer cell lines. PAK1-IN-2 can be used in the study of cancer.

AK963/40708899 is a potent PAK1 inhibitor. AK963/40708899 suppresses the proliferation of human gastric cancer cells by downregulation of PAK1-NF-κB-cyclinB1 pathway. AK963/40708899 induces cell cycle arrest at G2 phase and reduces the migration and invasion. AK963/40708899 inhibits the formation of filopodia and promots cell adhesion which in turn inhibits invasive potential of gastric cells by negatively regulating PAK1-LIMKl-cofilin and PAK1-ERK-FAK pathways.