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
Quality Level
originator
GlaxoSmithKline
storage temp.
2-8°C
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).
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.
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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
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
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)
Elevated Wall Tension Leads to Reduced miR-133a in the Thoracic Aorta by Exosome Release
Akerman AW, et al.
Journal of the American Heart Association, 8(1), e010332-e010332 (2019)
The TrkA receptor mediates experimental thermal hyperalgesia produced by nerve growth factor: modulation by the p75 neurotrophin receptor
Khodorova A, et al.
Neuroscience, 340, 384-397 (2017)
문서
지질 신호전달 연구를 위한 생체 활성 저분자
Discover Bioactive Small Molecules for Lipid Signaling Research
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