IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate Induced massive loss of viable tumor cells and dead rounded cells accumulation.
Induced cell death through apoptosis (shown by fragmented DNA in tumor sections).
Decreased nuclear Stat5a/b content by 60%, 78%, and 90% at 25, 50, and 100 mg/kg, respectively.
[1]. Zhiyong Liao, et al. Structure-Based Screen Identifies a Potent Small Molecule Inhibitor of Stat5a/b with Therapeutic Potential for Prostate Cancer and Chronic Myeloid Leukemia. Mol Cancer Ther. 2015 Aug;14(8):1777-93.