NCGC00244536-KDM4B-Inhibitor-B3-DataSheet-生命科學(xué)試劑-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作靶點: Histone Demethylase作通路: Epigenetics儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100

2、 mg/mL (261.47 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 NCGC00244536效的 KDM4B 抑制劑

3、，IC50 值為10 nM。IC50 & Target IC50: 10 nM (KDM4B) 1體外研究NCGC00244536 displays high selectivity for the fast-growing AR-negative PC3 cells (IC50=40 nM) and over1/2 Master of Small Molecules 您邊的抑制劑師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.體內(nèi)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