D1692

GW4869

≥90% (NMR), powder, N-SMase inhibitor

• Synonym(s): N,N′-Bis[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-3,3′-p-phenylene-bis-acrylamide dihydrochloride
• Empirical Formula (Hill Notation): C₃₀H₂₈N₆O₂ · 2HCl
• CAS Number: 6823-69-4
• Molecular Weight: 577.50
• UNSPSC Code: 41121800
• PubChem Substance ID: 24724460
• NACRES: NA.77

Properties

• Product Name: GW4869, ≥90% (NMR)
• Quality Level: 100
• assay: ≥90% (NMR)
• form: powder
• storage condition: desiccated; protect from light
• color: light yellow to yellow
• mp: >300 °C
• solubility: DMSO: 0.2 mg/mL
• originator: GlaxoSmithKline
• storage temp.: 2-8°C

Description

General description

GW4869 is a commonly used pharmacological agent, which inhibits exosome generation. It blocks ceramide-mediated inward budding of multivesicular bodies (MVBs) and the release of mature exosomes from MVBs.[1] GW4869 exhibits cytotoxicity to phosphatidylserine-expressing myeloma cells.[2] It inhibits the secretion of IFN (interferon)-α by plasmacytoid dendritic cells (pDCs).[3]

Application

GW4869 has been used:

• as an inhibitor of neutral sphingomyelinase and exosome biogenesis[4][5][6]
• to analyse the effects of arsenic trioxide (ATO) treatment for hepatoma carcinoma HCCLM3 cells on ceramide production[7]
• to determine the contributions of p75 neurotrophin receptor (p75^NTR) and tropomyosin receptor kinase A (TrkA)- coupled pathways to nerve growth factor (NGF)-induced thermal hypersensitivity in rats[8]

Biochem/physiol Actions

A cell-permeable, potent, specific, non-competitive inhibitor of N-SMase (neutral sphingomyelinase)

Features and Benefits

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable
• ppe: Eyeshields, Gloves, type N95 (US)