NCGC00244536 (B3) is a potent, speciifc lysine demethylase 4B (KDM4B, JMJD2B) inhibitor with an IC50 of 10 nM, inhibits LNCaP cell growth with IC50s in the μM range, shows no or weak activity for KDM5A/JARID1A.
NCGC00244536 (B3) displays much weaker acitvities against KDM4A, 4C, and 4D.
NCGC00244536 (B3) 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 (B3) effectively inhibits AR-positive cell lines, including LNCaP and VCaP, with IC50s in the sub-micromolar range.
NCGC00244536 (B3) 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.
NCGC00244536 (B3) (20 mg/kg) induces significant inhibition of tumor growth in xenograft model with tumors derived from injection of PC3 cells.