제품 이름
GW4869, ≥90% (NMR)
SMILES string
Cl.Cl.O=C(Nc1ccc(cc1)C2=NCCN2)\C=C/c3ccc(\C=C/C(=O)Nc4ccc(cc4)C5=NCCN5)cc3
InChI
1S/C30H28N6O2.2ClH/c37-27(35-25-11-7-23(8-12-25)29-31-17-18-32-29)15-5-21-1-2-22(4-3-21)6-16-28(38)36-26-13-9-24(10-14-26)30-33-19-20-34-30;;/h1-16H,17-20H2,(H,31,32)(H,33,34)(H,35,37)(H,36,38);2*1H/b15-5-,16-6-;;
InChI key
NSFKAZDTKIKLKT-LOLTXFFGSA-N
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
Quality Level
Application
GW4869 has been used:
- as an inhibitor of neutral sphingomyelinase and exosome biogenesis
- to analyse the effects of arsenic trioxide (ATO) treatment for hepatoma carcinoma HCCLM3 cells on ceramide production
- to determine the contributions of p75 neurotrophin receptor (p75NTR) and tropomyosin receptor kinase A (TrkA)- coupled pathways to nerve growth factor (NGF)-induced thermal hypersensitivity in rats
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.
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. GW4869 exhibits cytotoxicity to phosphatidylserine-expressing myeloma cells. It inhibits the secretion of IFN (interferon)-α by plasmacytoid dendritic cells (pDCs).
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
Exosomal miR-940 maintains SRC-mediated oncogenic activity in cancer cells: A possible role for exosomal disposal of tumor suppressor miRNAs
Rashed MH, et al.
Oncotarget, 8(12), 20145-20145 (2017)
Li Chen et al.
FEBS letters, 590(23), 4263-4274 (2016-10-25)
Exosomes mediate intercellular microRNA delivery between hepatic stellate cells (HSC), the principal fibrosis-producing cells in the liver. The purpose of this study was to identify receptors on HSC for HSC-derived exosomes, which bind to HSC rather than to hepatocytes. Our
Yunlong Huang et al.
Cell discovery, 4, 19-19 (2018-05-01)
Zika virus (ZIKV) is a neurotrophic flavivirus that is capable of infecting humans, leading to brain abnormalities during fetal development. The ZIKV infectivity in neural target cells remains poorly understood. Here, we found that ZIKV specifically infected glial fibrillary acidic
Phillip B Munson et al.
Scientific reports, 9(1), 11688-11688 (2019-08-14)
Malignant mesothelioma (MM) is an asbestos-induced cancer arising on the mesothelial surface of organ cavities. MM is essentially incurable without a means of early diagnosis and no successful standard of care. These facts indicate a deep chasm of knowledge that
The cationic small molecule GW 4869 is cytotoxic to high phosphatidylserine-expressing myeloma cells
Vuckovic S, et al.
British Journal of Haematology, 177(3), 423-440 (2017)
문서
지질 신호전달 연구를 위한 생체 활성 저분자
Discover Bioactive Small Molecules for Lipid Signaling Research
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