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Merck
모든 사진(1)

문서

SML2931

Sigma-Aldrich

GSK264220A

≥98% (HPLC)

동의어(들):

1-[[5-Methyl-4-[[(phenylamino)carbonyl]amino]-2-furanyl]sulfonyl]piperidine, GSK 264220A, N-[2-Methyl-5-(1-piperidinylsulfonyl)-3-furanyl]-N′-phenylurea

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About This Item

실험식(Hill 표기법):
C17H21N3O4S
CAS Number:
Molecular Weight:
363.43
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°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 key

LVOVQRPAMXCXTM-UHFFFAOYSA-N

생화학적/생리학적 작용

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.

픽토그램

Exclamation mark

신호어

Warning

유해 및 위험 성명서

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

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
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
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
Fiona Henderson et al.
Cancer research, 79(9), 2136-2151 (2019-03-14)
Alterations in lipid metabolism in cancer cells impact cell structure, signaling, and energy metabolism, making lipid metabolism a potential diagnostic marker and therapeutic target. In this study, we combined PET, desorption electrospray ionization-mass spectrometry (DESI-MS), nonimaging MS, and transcriptomic analyses

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