SML2931

Sigma-Aldrich

GSK264220A

≥98% (HPLC)

Sinónimos:
1-[[5-Methyl-4-[[(phenylamino)carbonyl]amino]-2-furanyl]sulfonyl]piperidine, GSK 264220A, N-[2-Methyl-5-(1-piperidinylsulfonyl)-3-furanyl]-N′-phenylurea
Empirical Formula (Hill Notation):
C17H21N3O4S
Número de CAS:
Peso molecular:
363.43
MDL number:
En este momento no podemos mostrarle ni los precios ni la disponibilidad

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

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.

pictograms

Exclamation mark

signalword

Warning

WGK Germany

WGK 3

Flash Point F

Not applicable

Flash Point C

Not applicable

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...
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...
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...
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...
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...

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