NCGC00244536 (KDM4B Inhibitor B3) is a potent KDM4B inhibitor (IC50: 10 nM).

KDM4B:10 nM

NCGC00244536有效地抑制AR阳性细胞系，包括LNCaP和VCaP，其IC50在亚微摩尔范围内，并且能够完全阻断雄激素刺激的LNCaP细胞增长。NCGC00244536对快速增长的AR阴性PC3细胞（IC50：40 nM）显示出高度选择性，并且对永生化的前列腺上皮细胞系PrEC1和PrEC4有超过100倍的选择性。NCGC00244536也在抑制包括乳腺癌细胞系MDA-MB2和MCF-7在内的其他癌症细胞系增长方面表现出强大效力，其IC50在微摩尔范围内。

使用NCGC00244536处理显著抑制了肿瘤生长，且动物未表现出任何主要毒性，看起来保持正常状态。NCGC00244536处理后的肿瘤中，细胞凋亡、坏死和纤维化的数量显著增加。

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.