NCGC00244536 是一种有效的 KDM4B 抑制剂，IC50为 10 nM。

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.

LNCaP cells are treated with 0.1, 0.2, 1, 2.5, 5, 20 μM of NCGC00244536. Cell viability is measured using the MTT assay.

For the xenograft animal model, PC3 cell suspension is injected into 4-6 weeks old severe combined immunodeficient (SCID) mice. When tumors become palpable, animals are randomly grouped for drug treatment. Alzet osmotic minipump containing NCGC00244536 (20 mg/kg)is subcutaneously inserted into each animal, which allowed continuous drug delivery to the tumor site for up to 5 days. Tumor volume is recorded every other days and calculated by using the ellipsoid formula.

2003260-55-5

C25H22N2O2

382.45

KDM4B Inhibitor B3

DMSO:100 mg/mL (261.47 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years