NCGC00244536-KDM4B-Inhibitor-B3-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENCGC00244536Cat. No.: HY-101799CAS No.: 2003260-55-5Synonyms: KDM4B Inhibitor B3分式: CHNO分量: 382.45作靶点: Histone Demethylase作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100

2、 mg/mL (261.47 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.6147 mL 13.0736 mL 26.1472 mL5 mM 0.5229 mL 2.6147 mL 5.2294 mL10 mM 0.2615 mL 1.3074 mL 2.6147 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 NCGC00244536效的 KDM4B 抑制剂

3、，IC50 值为10 nM。IC50 & Target IC50: 10 nM (KDM4B) 1体外研究NCGC00244536 displays high selectivity for the fast-growing AR-negative PC3 cells (IC50=40 nM) and over1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE100-fold selectivity against the immortalized prostate epithelial cell lines PrEC1 and PrEC4. N

4、CGC00244536effectively inhibits AR-positive cell lines, including LNCaP and VCaP, with IC50s in the sub-micromolarrange, and abolishes androgen-stimulated LNCaP cell growth. NCGC00244536 is also potent in inhibiting thegrowth of other cancer cell lines, including the breast cancer cell lines MDA-MB2

5、 and MCF-7, withmicromolar IC50s 1.体内研究 Treatment with NCGC00244536 results in significant inhibition of tumor growth and animals do not exhibitany major toxicity and appear to be normal. Histological data clearly indicate that NCGC00244536-treatedtumors have significant amount of cell apoptosis, ne

6、crosis, and fibrosis 1.PROTOCOLCell Assay 1 LNCaP cells are treated with 0.1, 0.2, 1, 2.5, 5, 20 M of NCGC00244536. Cell viability is measured usingthe MTT assay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mouse: For xenograft animal model,

7、 PC3 cell suspension is injected into 4-6 weeks old severe combinedAdministration 1 immunodeficient (SCID) mice. When tumors become palpable, animals are randomly grouped for drugtreatment. Alzet osmotic minipump containing NCGC00244536 (20 mg/kg)is subcutaneously inserted intoeach animal, which all

8、owed continuous drug delivery to the tumor site for up to 5 days. Tumor volume isrecorded every other days and calculated by using the ellipsoid formula 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Duan L, et al. KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR andBMYB-Regulated Genes. Chem Biol. 2015 Sep 17;22(9):1185-96.McePdfHeightCaution: Product has not been fully validated for medical appli