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Chemical Structure| 6823-69-4 Chemical Structure| 6823-69-4

Structure of GW4869
CAS No.: 6823-69-4

Chemical Structure| 6823-69-4

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GW4869 2HCl is a cell permeable, selective and non-competitve inhibitor of N-SMase (neutral sphingomyelinase), which is important in the metabolism of sphingomyelin producing ceramide and phosphocholine and in cell signaling and regulation. GW4869 is an exosome inhibitor.

Synonyms: GW 4869 (hydrochloride hydrate); GW554869A; GW69A

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Product Details of GW4869

CAS No. :6823-69-4
Formula : C30H30Cl2N6O2
M.W : 577.50
SMILES Code : O=C(/C=C/C1=CC=C(C=C1)/C=C/C(NC2=CC=C(C=C2)C3=NCCN3)=O)NC4=CC=C(C=C4)C5=NCCN5.Cl.Cl
Synonyms :
GW 4869 (hydrochloride hydrate); GW554869A; GW69A
MDL No. :MFCD06411564

Safety of GW4869

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
BV2 microglia cell line 2, 5, 10 μM 24 h Inhibit MV release, reduce GLS1 release Mol Neurodegener. 2015 Nov 6;10:61.
CAFs 20 μM Inhibit exosome secretion Neoplasia. 2021 Jul;23(7):692-703.
BMMs 10 μM 18 h Inhibit exosome biogenesis and prevent DNA-induced Ifnb expression Nat Microbiol. 2019 Apr;4(4):701-713.
MEFs 10 μM 18 h Inhibit exosome biogenesis and prevent DNA-induced Ifnb expression Nat Microbiol. 2019 Apr;4(4):701-713.
A549 cells 10 μM 24 hours To investigate the effect of exosome release inhibitor GW4869 on oxidative stress-induced cell migration and invasion. Results showed that GW4869 treatment attenuated oxidative stress-induced cell migration and invasion. J Extracell Vesicles. 2024 Sep;13(9):e12505
monocyte-derived macrophages (MDM) 2, 5, 10 μM 24 h Inhibit MV release, reduce GLS1 release Mol Neurodegener. 2015 Nov 6;10:61.
L02 cells 20 μM 12 h To prevent exosome secretion Cell Death Dis. 2022 Oct 12;13(10):865.
KBM7 SGMS1GT+SGMS1 cells 10 μM 24 h GW4869 treatment significantly reduced ZIKV shedding Nat Commun. 2020 Jul 21;11(1):3652.
Huh7 cells 10 μM 24 h GW4869 treatment reduced viral shedding Nat Commun. 2020 Jul 21;11(1):3652.
M2 macrophages 10 µM 8 h GW4869 successfully blocked the release of extracellular vesicles (EVs) from M2 macrophages, thereby reducing the proliferation, migration, and phenotypic transformation of CFs. Theranostics. 2021 Apr 15;11(13):6315-6333.
cardiomyocytes 10 μM 24 h Inhibit the production of cardiomyocyte-derived EVs and reduce N1 neutrophil polarization J Nanobiotechnology. 2024 Oct 16;22(1):632.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Endometrial cancer xenograft model Intraperitoneal injection 2 mg/kg Every other day until tumor collection Inhibit CAFs-mediated tumor growth Neoplasia. 2021 Jul;23(7):692-703.
Mice Myocardial ischemia/reperfusion injury model Intraperitoneal injection 2.5 mg/kg Single injection, lasting 1 hour Inhibit the production of EVs and reduce myocardial ischemia/reperfusion injury J Nanobiotechnology. 2024 Oct 16;22(1):632.
Mice C57BL/6N mice Intraperitoneal injection 0.3125 or 1.25 µg/g Once per day for five consecutive days Inhibit exosome biogenesis and reduce Ifnb mRNA and Mx1 expression, but not Tnfa mRNA Nat Microbiol. 2019 Apr;4(4):701-713.
Mice Elastase-induced abdominal aortic aneurysm model Intraperitoneal injection 1.25 mg/kg Once daily for 21 days To investigate the effect of GW4869 on the development of abdominal aortic aneurysm, the results showed that GW4869 significantly attenuated elastase-induced AAA expansion and macrophage infiltration. Redox Biol. 2022 Apr;50:102257.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.73mL

0.35mL

0.17mL

8.66mL

1.73mL

0.87mL

17.32mL

3.46mL

1.73mL

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