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Merck

SML2931

Sigma-Aldrich

GSK264220A

≥98% (HPLC)

Synonym(e):

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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€ 82,40
25 MG
€ 267,00

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5 MG
€ 82,40
25 MG
€ 267,00

About This Item

Empirische Formel (Hill-System):
C17H21N3O4S
CAS-Nummer:
Molekulargewicht:
363.43
MDL-Nummer:
UNSPSC-Code:
12352200
NACRES:
NA.77

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Qualitätsniveau

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear

Lagertemp.

2-8°C

SMILES String

[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)

InChIKey

LVOVQRPAMXCXTM-UHFFFAOYSA-N

Biochem./physiol. Wirkung

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.

Piktogramme

Exclamation mark

Signalwort

Warning

H-Sätze

Gefahreneinstufungen

Eye Irrit. 2 - Skin Irrit. 2

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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In der Dokumentenbibliothek finden Sie die Dokumentation zu den Produkten, die Sie kürzlich erworben haben.

Die Dokumentenbibliothek aufrufen

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
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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