TPOP146-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETPOP146Cat. No.: HY-100697CAS No.: 2018300-62-2分式: CHNO分量: 481.58作靶点: Epigenetic Reader Domain; 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 : 100

2、mg/mL (207.65 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0765 mL 10.3825 mL 20.7650 mL5 mM 0.4153 mL 2.0765 mL 4.1530 mL10 mM 0.2076 mL 1.0382 mL 2.0765 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。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(

3、为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.19 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.19 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90

4、% corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.19 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 TPOP146选择性的CBP/P300苯并西泮溴结构域抑制剂；对CBP和BRD4的Kd值分别为134 nM和5.02 M。IC50 & Target IC50: 134 nM (CBP); 5.02 M (BRD4) 1体外研究 Exposure to 1 M TPOP146 results in a significant decreas

5、e of recovery half-life that is comparable to theconstruct that contained the bromodomain inactivating mutation N1168F, demonstrating that TPOP146targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediatedinteractions of the CBP bromodomain in cellular environm

6、ents 1.PROTOCOLKinase Assay 1 Proteins are buffered in 10 mM HEPES, pH 7.5, 500 mM NaCl and assayed in a 96-well plate at a finalconcentration of 2 M in 20 L volume. Compounds (TPOP146) are added at a final concentration of 10 M.SYPRO Orange (Molecular Probes) is added as a fluorescence probe at a d

7、ilution of 1:1000. Excitation andemission filters for the SYPRO Orange dye are set to 465 and 590 nm, respectively. The temperature israised with a step of 3C per minute from 25 to 96C, and fluorescence readings are taken at each interval1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912.McePdfHeightCaution: Product has not been fully validated for medical applications.For r