GSK-525768A-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK 525768ACat. No.: HY-13032ACAS No.: 1260530-25-3分式: CHClNO分量: 423.9作靶点: Others作通路: Others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 mg/mL (235.90 mM)* means soluble, but saturat

2、ion unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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，配制前请先配制澄清的储备液，再依次添加助溶剂(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；澄清的储备液可以根据储存

3、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 (5.90 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 (5.90 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVI

4、TY物活性 GSK 525768AGSK525762A 的活性对映体。GSK 525768A 对 BET 没有活性。体外研究 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.户使本产品发表的科研献 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