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SML2931

Sigma-Aldrich

GSK264220A

≥98% (HPLC)

Synonyme(s) :

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

Formule empirique (notation de Hill):
C17H21N3O4S
Numéro CAS:
685506-42-7
Poids moléculaire :
363.43
Numéro MDL:
MFCD02679009
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

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)

Clé InChI

LVOVQRPAMXCXTM-UHFFFAOYSA-N

Actions biochimiques/physiologiques

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.

Pictogrammes

Exclamation mark
GHS07

Mention d'avertissement

Warning

Mentions de danger

H315,H319

Classification des risques

Eye Irrit. 2 - Skin Irrit. 2

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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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
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
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