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GSK8815,≥98% (HPLC)

别名:8-[[(3S,4S,5R)-3-[(4,4-Difluorocyclohexyl)methoxy]-5-methoxy-4-piperidinyl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1,7-naphthyridin-2(1H)-one, 8-((3S,4S,5R)-3-((4,4-Difluorocyclohexyl)methoxy)-5-methoxypiperidin-4-ylamino)-3-methyl-5-(5-methylpyridin-3-yl)-1,7-naphthyridin-2(1H)-one

Empirical Formula (Hill Notation): C28H35F2N5O3 分子量: 527.61
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): SML2112
增值税发票 √ 免费送货 √ 订货电话:010-68689484
$449.65

说明

生化/生理作用

GSK8815 is an aqueous soluble (326 μM) naphthyridone that serves as a negative control for the more active diastereomer GSK8814 in ATAD2/ATAD2B inhibition studies. Comparing to GSK8814, GSK8815 is ineffective in cell-based assays and exhibits greatly reduced affinity toward ATAD2 & ATAD2B bromodomain in cell-free binding assays (pKd for ATAD2 = 5.5/GSK8815 vs. 8.1/GSK8814 by ITC; pIC50 against ATAD2 BD/ATAD2B BD = 5.5/5.5 with GSK8815 vs. 7.3/7.7 with GSK8814 in competitive ligand binding assays by TR-FRET).
 
GSK8815 是一种水溶性 (326 μM) 萘啶酮,在 ATAD2/ATAD2B 抑制研究中用作活性更高的非对映异构体 GSK8814 的阴性对照。 与 GSK8814 相比,GSK8815 在基于细胞的测定中无效,并且在无细胞结合测定中对 ATAD2 和 ATAD2B 溴结构域的亲和力大大降低(ATAD2 的 pKd = 5.5/GSK8815 vs. 8.1/GSK8814,ITC;pIC50 对 ATAD2B/ATAD2B 在通过 TR-FRET 进行的竞争性配体结合测定中,BD = 5.5/5.5(使用 GSK8815 对比使用 GSK8814 的 7.3/7.7)。
 

属性

测定

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

−20°C

SMILES string

O=C(N1)C(C)=CC2=C1C(N[C@H]3[C@H](OCC4CCC(F)(F)CC4)CNC[C@H]3OC)=NC=C2C5=CN=CC(C)=C5

 

安全信息

WGK Germany

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16