推薦產品
品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
[S](=O)(=O)(N3CCCCC3)c1[o]c(c(c1)NC(=O)Nc2ccccc2)C
InChI
1S/C17H21N3O4S/c1-13-15(19-17(21)18-14-8-4-2-5-9-14)12-16(24-13)25(22,23)20-10-6-3-7-11-20/h2,4-5,8-9,12H,3,6-7,10-11H2,1H3,(H2,18,19,21)
InChI 密鑰
LVOVQRPAMXCXTM-UHFFFAOYSA-N
生化／生理作用
GSK264220A is a potent, active site-targeting, covalent inhibitor against endothelial lipase (EL or LIPG; IC50 = 130 nM) and lipoprotein lipase (LPL or LIPD; IC50 = 100 nM). GSK264220A reduces NeuT expression - or CoCl2 treatment-induced intracellular triacylglycerol & lipid droplets (TAG & LD) increase in MCF-7 (16 & 32 nM) and suppresses LPL-depenent melanoma survival (by ~50% at 18.75 μM; WM852, WM1361). When applied in mice in vivo (30 mg/kg ip.), GSK264220A21 enhances lipid nanoparticles-mediated siRNAs delivery & gene-silencing efficacy.
Potent, active site-targeting, covalent inhibitor against endothelial lipase (EL, LIPG) and lipoprotein lipase (LPL, LIPD) in vitro and in vivo.
訊號詞
Warning
危險聲明
危險分類
Eye Irrit. 2 - Skin Irrit. 2
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
從最近期的版本中選擇一個：
Cristina Cadenas et al.
International journal of cancer, 145(4), 901-915 (2019-01-18)
Endothelial lipase (LIPG) is a cell surface associated lipase that displays phospholipase A1 activity towards phosphatidylcholine present in high-density lipoproteins (HDL). LIPG was recently reported to be expressed in breast cancer and to support proliferation, tumourigenicity and metastasis. Here we
Yusuke Sato et al.
Molecular therapy : the journal of the American Society of Gene Therapy, 24(4), 788-795 (2015-12-19)
While a variety of short interfering RNA (siRNA) delivery compounds have been developed, a deep understanding of the key parameters that determine the quality of siRNA delivery are not known with certainty. Therefore, an understanding of the factors required for
Paul M Keller et al.
Journal of biomolecular screening, 13(6), 468-475 (2008-06-21)
Endothelial lipase (EL) is a 482-amino-acid protein from the triglyceride lipase gene family that uses a Ser-His-Asp triad for catalysis. Its expression in endothelial cells and preference for phospholipids rather than triglycerides are unique. Animal models in which it is
Krista B Goodman et al.
Bioorganic & medicinal chemistry letters, 19(1), 27-30 (2008-12-09)
Endothelial lipase (EL) activity has been implicated in HDL catabolism, vascular inflammation, and atherogenesis, and inhibitors are therefore expected to be useful for the treatment of cardiovascular disease. Sulfonylfuran urea 1 was identified in a high-throughput screening campaign as a
Leslie E Lupien et al.
The Journal of pharmacology and experimental therapeutics, 371(1), 171-185 (2019-07-14)
It is well recognized that many cancers are addicted to a constant supply of fatty acids (FAs) and exhibit brisk de novo FA synthesis. Upregulation of a key lipogenic enzyme, fatty acid synthase (FASN), is a near-universal feature of human
我們的科學家團隊在所有研究領域都有豐富的經驗，包括生命科學、材料科學、化學合成、色譜、分析等.
聯絡技術服務