NSC117024

NSC117024 is a novel, structure-based, small-molecule cyclin-dependent kinase (CDK) inhibitor developed by researchers at the University of Florida. Identified via in silico molecular docking, NSC117024 targets a conformational pocket on Cyclin-dependent kinase 2 (CDK2) that opens upon p27 binding, forcing the kinase into an inactive conformation. NSC117024 directly inhibits CDK2 activity and reduces the soluble levels of CDK1, CDK2, and CDK4 by inducing their aggregation and translocation to the insoluble cellular fraction. It has demonstrated selective antiproliferative activity against breast cancer cells, particularly the Rb-deficient BT549 cell line, while sparing non-transformed mammary epithelial cells.

Other names

4-(p-methylanilino)-1,2-naphthoquinone4-[(4-methylphenyl)amino]-1,2-naphthalenedione4-[(4-methylphenyl)amino]naphthalene-1,2-dione