1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK 525768ACat. No.: HY-13032ACAS No.: 1260530-25-3分式: CHClNO分量: 423.9作靶點: Others作通路: Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 100 mg/mL (235.90 mM)* means soluble, but saturat

2、ion unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3590 mL 11.7952 mL 23.5905 mL5 mM 0.4718 mL 2.3590 mL 4.7181 mL10 mM 0.2359 mL 1.1795 mL 2.3590 mL請根據產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。體內實驗 請根據您的實驗動物和給藥式選擇適當的溶解案，配制前請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現現配，當天使；澄清的儲備液可以根據儲存

3、條件，適當保存；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 (5.90 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 (5.90 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVI

4、TY物活性 GSK 525768AGSK525762A 的活性對映體。GSK 525768A 對 BET 沒有活性。體外研究 GSK 525768A has no activity towards BET 1. GSK 525768A (GSK525768A) is the (R)-enantiomer ofGSK525762A. GSK525762A is shown to regulate levels of the high-density lipid protein apolipoprotein A1(APOA1) in assays monitoring APOA1 release

5、in liver cells, whereas the (R)-enantiomer (GSK 525768A) hasno effect. GSK 525768A directly engages the protein module by forming hydrogen bonds with the conservedasparagine residue in a way that mimics the binding mode of acetylated lysine; this usually results in thebinding of the inhibitor deeper

6、 within the acetylated lysine binding site but without displacing the conservedwater molecules that are present at the bottom of the acetyl-lysine binding cavity 2.戶使本產品發表的科研獻 Patent. US20180263995A1.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Nicodeme E, et al. Suppression

7、 of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23.2. Filippakopoulos P, et al. Targeting bromodomains: epigenetic readers of lysine acetylation. Nat Rev Drug Discov. 2014 May;13(5):337-56.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use o