WBZ_4

WBZ_4 is a novel small molecule inhibitor designed as a rational redesign of imatinib to selectively target c-Jun N-terminal kinase 1 (JNK1) and c-Kit while specifically avoiding BCR-Abl kinase. Developed by a collaborative team including researchers from the University of Texas M. D. Anderson Cancer Center and Rice University, the compound was engineered using a "wrapping defect" strategy to exploit de-wetting hot spots—non-conserved sites with low water residence time—thereby increasing specificity. In preclinical studies for epithelial ovarian cancer, WBZ_4 demonstrated the ability to inhibit cell growth and induce apoptosis in a dose-dependent manner. In orthotopic murine models, it significantly reduced tumor growth, showing enhanced efficacy when combined with docetaxel, whereas the parent compound imatinib showed no effect.

Other names

N-5-[4-(4-methyl piperazine methyl)-benzoylamido]-2-methylphenyl-4-[3-(4-methyl)-pyridyl]-2-pyrimidine amine