WM-8014 - Histone Acetyltransferase 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEWM-8014Cat. No.: HY-102060CAS No.: 2055397-18-5分式: CHFNOS分量: 384.42作靶点: Histone Acetyltransferase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 : 250 mg/mL (650.33 mM)* means

2、 soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.6013 mL 13.0066 mL 26.0132 mL5 mM 0.5203 mL 2.6013 mL 5.2026 mL10 mM 0.2601 mL 1.3007 mL 2.6013 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 WM-8014种 MOZ (属于 histone acetyltransferases) 的抑制剂

3、，IC50 值为 55 nM。IC50 & Target IC50: 55 nM (MOZ) 1体外研究WM-8014 (Compound 36) is an inhibitor of MOZ, with an IC50 of 55 nM. WM-8014 causes cell senescenceand suppresses the proliferation with IC50s of 1.6 M and 551 nM, respectively. WM-8014 also reduces1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEm

4、RNA coding for the MOZ gene Cdc6 by 65.1% 1.PROTOCOLKinase Assay 1 To determine the inhibition of Moz activity by the test compounds, assay reactions are conducted in a volumeof 8 L in 384-well low volume assay plates. The reactions are performed in assay buffer (100 mM Tris-HCl,pH 7.8, 15 mM NaCl,

5、1 mM EDTA, 0.01% Tween-20, 1 mM Dithiothreitol, and 0.02% m/v chicken egg whitealbumin). Reactions are set up with 0.4 M Acetyl coenzyme A (AcCoA), 50 nM N-terminal histone H4peptide (sequence SGRGKGGKGLGKGGAKRHRKV-GGK-biotin), 10 nM MOZ enzyme, and an acetyl-lysinespecific antibody (final dilution

6、1: 10000). 11-point dilution series of the compounds (WM-8014) of theinvention are prepared in DMSO; a volume of 100 nL is transferred using a pin tool into assay platescontaining substrates, before adding enzyme to start the reaction. Positive (no compound) and negative(AcCoA omitted) control react

7、ions are included on the same plates and receive the same amount of DMSOas the compound treated wells. After adding all reagents, the plates are sealed with adhesive seals andincubated for 90 minutes at room temperature 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. ARYL SULFONOHYDRAZIDES. WO2016198507 A1.McePdfHeightCaution: Product has not been fully validated for medical applications.For resear