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1260530-25-3

中文名稱 GSK 525768A
英文名稱 GSK-525768A
CAS 1260530-25-3
分子式 C22H22ClN5O2
分子量 423.9
MOL 文件 1260530-25-3.mol
1260530-25-3 結(jié)構(gòu)式 1260530-25-3 結(jié)構(gòu)式

基本信息

中文別名
BROMODOMAIN抑制劑(GSK 525768A)
英文別名
GSK-525768
GSK525768A
GSK 525768A
GSK-525768A
GSK525768A
GSK-525768A
(4R)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide
4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4R)-
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)140-145℃
密度1.35±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)15.71±0.46(Predicted)
形態(tài)粉末
顏色Light yellow to yellow
GSK 525768A價(jià)格(試劑級)
報(bào)價(jià)日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價(jià)格
2024/08/19HY-13032AGSK 525768A
GSK 525768A
1260530-25-32mg2170元
2024/08/19HY-13032AGSK 525768A
GSK 525768A
1260530-25-310mM * 1mLin DMSO3036元
2024/08/19HY-13032AGSK 525768A
GSK 525768A
1260530-25-35mg3255元

常見問題列表

生物活性
GSK 525768A 是 GSK525762A 的無活性對映體。GSK 525768A 對 BET 沒有活性。
體外研究

GSK 525768A has no activity towards BET. GSK 525768A (GSK525768A) is the (R)-enantiomer of GSK525762A. GSK525762A is shown to regulate levels of the high-density lipid protein apolipoprotein A1 (APOA1) in assays monitoring APOA1 release in liver cells, whereas the (R)-enantiomer (GSK 525768A) has no effect. GSK 525768A directly engages the protein module by forming hydrogen bonds with the conserved asparagine residue in a way that mimics the binding mode of acetylated lysine; this usually results in the binding of the inhibitor deeper within the acetylated lysine binding site but without displacing the conserved water molecules that are present at the bottom of the acetyl-lysine binding cavity.

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