KDM4B-IN-B3

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).

Product information

CAS Number: 2003260-55-5

Molecular Weight: 382.45

Formula: C25H22N2O2

Synonym:

NCGC00244536

Chemical Name: 3-(8-Hydroxyquinolin-6-yl)-N-(3-phenylpropyl)benzamide

Smiles: OC1=CC(=CC2=CC=CN=C21)C1=CC(=CC=C1)C(=O)NCCCC1C=CC=CC=1

InChiKey: NYKBXXGHEMXSBB-UHFFFAOYSA-N

InChi: InChI=1S/C25H22N2O2/c28-23-17-22(16-20-12-6-13-26-24(20)23)19-10-4-11-21(15-19)25(29)27-14-5-9-18-7-2-1-3-8-18/h1-4,6-8,10-13,15-17,28H,5,9,14H2,(H,27,29)

Technical Data

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

In Vitro:

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.

In Vivo:

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.

References:

1. 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.

Products are for research use only. Not for human use.