NCGC00244536

NCGC00244536 is a potent KDM4B inhibitor (IC50: 10 nM) .NCGC00244536 effectively inhibits AR-positive cell lines, including LNCaP and VCaP, with IC50s in the sub-micromolar range, and abolishes androgen-stimulated LNCaP cell growth. NCGC00244536 displays high selectivity for the fast-growing AR-negative PC3 cells (IC50: 40 nM) and over 100-fold selectivity against the immortalized prostate epithelial cell lines PrEC1 and PrEC4. NCGC00244536 is also potent in inhibiting the growth of other cancer cell lines, including the breast cancer cell lines MDA-MB2 and MCF-7, with micromolar IC50s.Treatment with NCGC00244536 results in significant inhibition of tumor growth and animals do not exhibit any major toxicity and appear to be normal. NCGC00244536-treated tumors have a significant amount of cell apoptosis, necrosis, and fibrosis.