mProX™ Human PAK4 Stable Cell Line

Han, Wei. et al. "Design, synthesis and anticancer activity evaluation of 4-(3-1H-indazolyl)amino quinazoline derivatives as PAK4 inhibitors." Bioorganic & medicinal chemistry, 2023.
A series of novel quinazoline derivatives, featuring a 3-1H-indazolylamino moiety, were innovated as potent inhibitors of PAK4 using a scaffold-switching approach. Compounds 27e, 27g, 27i, and 27j displayed robust PAK4 inhibition, with IC50 values of 10, 13, 11, and 9 nM, respectively. In cellular assays, 27e exhibited notable antiproliferative activity against A549 cells, boasting an IC50 of 0.61 μM, slightly outperforming PF-3758309. Further investigations unveiled that 27e induced apoptosis in A549 cells and arrested the cell cycle at G0/G1 phase. A binding model was proposed for 27e and PAK4, suggesting its potential as a novel PAK4-targeted anticancer agent.
Han, Wei. et al. "Design, synthesis and anticancer activity evaluation of 4-(3-1H-indazolyl)amino quinazoline derivatives as PAK4 inhibitors." Bioorganic & medicinal chemistry, 2023.
Pubmed: 37864885   DOI: 10.1016/j.bmc.2023.117501

Di Stefano, Iosè. et al. "New Immunohistochemical Markers for Pleural Mesothelioma Subtyping." Diagnostics (Basel, Switzerland), 2023.
The article introduces the three main subtypes of pleural mesothelioma (PM): epithelioid, biphasic, and sarcomatoid. These subtypes have varying effects on prognosis and treatment. However, accurately subtyping PM can be challenging due to the heterogeneous nature of the tumor. The authors conducted a study using immunohistochemistry (IHC) to assess the expression of five markers in a series of 73 PM cases. The markers, including Mesothelin, Claudin-15, Complement Factor B, Plasminogen Activator Inhibitor 1, and p21-activated Kinase 4, have been previously reported as deregulated among PM subtypes. The results were validated in an independent cohort of 30 PMs. Sensitivity and specificity were evaluated for each marker, and it was found that Mesothelin and Claudin-15 had good performance in distinguishing the epithelioid subtype. The study also showed that all markers had varied expression between the epithelioid and sarcomatoid components in biphasic PM. Overall, the authors suggest that Mesothelin, Claudin-15, and Complement Factor B could be useful in discriminating subtypes, while Plasminogen Activator Inhibitor 1 and p21-activated Kinase 4 can improve component distinction in biphasic PM.
Di Stefano, Iosè. et al. "New Immunohistochemical Markers for Pleural Mesothelioma Subtyping." Diagnostics (Basel, Switzerland), 2023.
Pubmed: 37761312   DOI: 10.3390/diagnostics13182945