KDM4B-IN-B3, also know as NCGC00244536, is a novel KDM4 inhibitor. KDM4B-IN-B3 inhibits the in vivo growth of tumors derived from PC3 cells and ex vivo human PCa explants. Histone lysine demethylase KDM4/JMJD2s are overexpressed in many human tumors including prostate cancer (PCa).
CAS Number: 2003260-55-5
Molecular Weight: 382.45
Chemical Name: 3-(8-Hydroxyquinolin-6-yl)-N-(3-phenylpropyl)benzamide
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 36.67 mg/mL (95.88 mM; Need ultrasonic)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
KDM4B-IN-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. KDM4B-IN-B3 effectively inhibits AR-positive cell lines, including LNCaP and VCaP, with IC50s in the sub-micromolar range, and abolishes androgen-stimulated LNCaP cell growth. KDM4B-IN-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.
Treatment with KDM4B-IN-B3 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 KDM4B-IN-B3-treated tumors have significant amount of cell apoptosis, necrosis, and fibrosis.
- Duan L, et al. KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes. Chem Biol. 2015 Sep 17;22(9):1185-96.
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