NCGC00244536 is a potent KDM4B inhibitor with an IC 50 of 10 nM.
In Vitro
NCGC00244536 displays high selectivity for the fast-growing AR-negative PC3 cells (IC 50 =40 nM) and over 100-fold selectivity against the immortalized prostate epithelial cell lines PrEC1 and PrEC4. NCGC00244536 effectively inhibits AR-positive cell lines, including LNCaP and VCaP, with IC 50 s in the sub-micromolar range, and abolishes androgen-stimulated LNCaP cell growth. 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 IC 50 s. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Treatment with NCGC00244536 results in significant inhibition of tumor growth and animals do not exhibit any major toxicity and appear to be normal. Histological data clearly indicate that NCGC00244536-treated tumors have significant amount of cell apoptosis, necrosis, and fibrosis . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
