TPOP146-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETPOP146Cat. No.: HY-100697CAS No.: 2018300-62-2分式: CHNO分量: 481.58作靶點: Epigenetic Reader Domain; Histone Acetyltransferase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 (207.65 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄的儲備液，再依次添加助溶?

3、為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.19 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.19 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90

4、% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (5.19 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 TPOP146選擇性的CBP/P300苯并西泮溴結(jié)構(gòu)域抑制劑；對CBP和BRD4的Kd值分別為134 nM和5.02 M。IC50 & Target IC50: 134 nM (CBP); 5.02 M (BRD4) 1體外研究 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