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GW4869

Catalog No. T3640 CAS 6823-69-4

Synonyms: GW554869A, GW 4869, GW69A

GW4869 (GW69A) is a selective and non-competitive inhibitor of neutral sphingomyelinase N-SMase (IC50=1 μM). GW4869 also inhibits exosome synthesis/release and is commonly used in exosome-related studies.

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GW4869, CAS 6823-69-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 53.00
2 mg	In stock	$ 74.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 182.00
25 mg	In stock	$ 382.00
50 mg	In stock	$ 573.00
100 mg	In stock	$ 693.00
500 mg	In stock	$ 1,460.00

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Purity: 99.66%

Purity: 98.47%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GW4869 (GW69A) is a selective and non-competitive inhibitor of neutral sphingomyelinase N-SMase (IC50=1 μM). GW4869 also inhibits exosome synthesis/release and is commonly used in exosome-related studies.
Targets&IC50	SMase:1 μM
In vitro	METHODS: Human breast cancer cells MCF-7 were pretreated with GW4869 (10 μM) for 30 min, then incubated with TNF (3 nM) for 6-24 h. Ceramide levels were detected by E. coli diacylglycerol kinase assay. RESULTS: GW4869 significantly inhibited TNF-induced ceramide accumulation, and GW4869 inhibited N-SMase. [1] METHODS: Macrophage RAW264.7 was pretreated with GW4869 (10-20 μM) for 2 h, and then incubated with LPS (1 μg/mL) for 24 h. AchE activity was measured. RESULTS: After pretreatment of macrophages with 10 μM GW4869, LPS-triggered exocytosis was significantly attenuated in macrophages, and the activity of AChE was reduced by 22%. Treatment with 20 μM GW4869 further enhanced this attenuation. [2]
In vivo	METHODS: To detect in vivo activity, GW4869 (2.5 μg/g) was injected intraperitoneally into C57BL/6 mice, and LPS (25 μg/g) was injected 1 h later. RESULTS: Pretreatment of mice with GW4869 attenuated LPS-triggered production of exosomes and pro-inflammatory cytokines in the blood, thereby reducing myocardial inflammation. [2] METHODS: To assay in vivo activity, GW4869 (200 μL of 0.3 mg/mL, 2-2.5 μg/g) was administered intraperitoneally to 5XFAD mice every two days for six weeks. RESULTS: GW4869 reduced amyloid plaque formation in vivo by blocking exosome secretion. [3]
Kinase Assay	B. cereu sphosphatidylcholine-PLC is incubated in the presence or absence of 10 μM GW4869 in a reaction mixture containing 100 mM Tris, pH 7.2, 25% glycerol, 20 mM p-nitrophenyl/phosphorylcholine, and production of p-nitrophenol is quantified spectrophotometrically at 410 nm. Protein phosphatase 2A from bovine kidney is incubated in the presence or absence of GW4869 in buffer containing 50 mM Tris, pH 7.4, 1 mM dithiothreitol, 100 μM MnCl2, and 20% glycerol, and phosphatase activity is measured[1].
Cell Research	GW4869 is routinely stored at ?80?°C as a 1.5 mM stock suspension in Me2SO. Right before use, the suspension is solubilized by the addition of 5% methane sulfonic acid (MSA) (2.5 μl of 5% MSA in sterile double-distilled Water are added to 50 μL of GW4869 stock suspension). Cells are treated with GW4869 for 30 min and then TNF is added in 10 μL/well. At the indicated time points, 25 μL of MTT stock solution are added to each well and incubated at 37?°C in 5% CO2 for 3 h. The cell viability is using the MTT assay[1].

Synonyms	GW554869A, GW 4869, GW69A
Molecular Weight	577.5
Formula	C30H30Cl2N6O2
CAS No.	6823-69-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 14.71 mg/mL (25.46 mM), Sonication is recommended.

References and Literature

1. Luberto C, et al. Inhibition of tumor necrosis factor-induced cell death in MCF7 by a novel inhibitor of neutral sphingomyelinase. J Biol Chem. 2002 Oct 25;277(43):41128-39. 2. Essandoh K, et al. Blockade of exosome generation with GW4869 dampens the sepsis-induced inflammation and cardiac dysfunction. Biochim Biophys Acta. 2015 Nov;1852(11):2362-71. 3. Dinkins MB, et al. Exosome reduction in vivo is associated with lower amyloid plaque load in the 5XFAD mouse model of Alzheimer's disease. Neurobiol Aging. 2014 Aug;35(8):1792-800. 4. . Heat injured stromal cells‐derived exosomal EGFR enhances prostatic wound healing after thulium laser resection through EMT and NF‐κB signaling. The Prostate. 2019 May 24. 5. Ge M, Qiao Z, Kong Y, et al. Exosomes mediate intercellular transfer of non-autonomous tolerance to proteasome inhibitors in mixed-lineage leukemia[J]. Cancer Science. 2020. 6. Ge M, Qiao Z, Kong Y, et al. Exosomes mediate intercellular transfer of non–autonomous tolerance to proteasome inhibitors in mixed‐lineage leukemia[J]. Cancer Science. 2020, 111(4): 1279. 7. Wang X, Chen Q Z, Zan Y X, et al. . Exosomal miR‐145‐5p derived from orthohantavirus‐infected endothelial cells inhibits HTNV infection. The FASEB Journal. 2020, 34(10): 13809-13825.

Citations

1. Han X, de Dieu Habimana J, Li A L, et al. Transcription factor EB-mediated mesenchymal stem cell therapy induces autophagy and alleviates spinocerebellar ataxia type 3 defects in neuronal cells model. Cell death & disease. 2022, 13(7): 1-12. 2. Ge M, Qiao Z, Kong Y, et al. Exosomes mediate intercellular transfer of non-autonomous tolerance to proteasome inhibitors in mixed-lineage leukemia. Cancer Science. 2020 3. Wang X, Chen Q Z, Zan Y X, et al. Exosomal miR‐145‐5p derived from orthohantavirus‐infected endothelial cells inhibits HTNV infection. The FASEB Journal. 2020, 34(10): 13809-13825. 4. Shi F, Deng Z, Zhou Z, et al. Heat injured stromal cells‐derived exosomal EGFR enhances prostatic wound healing after thulium laser resection through EMT and NF‐κB signaling. The Prostate. 2019 May 24 5. Han C, Xia X, Jiao S, et al. Tripartite motif containing protein 37 involves in thrombin stimulated BV-2 microglial cell apoptosis and interleukin 1β release. Biochemical and biophysical research communications. 2019, 516(4): 1252-1257. 6. Cao Z, Li P, Li Y, et al.Encapsulation of Nano‐Bortezomib in Apoptotic Stem Cell‐Derived Vesicles for the Treatment of Multiple Myeloma.Small.2023: 2301748. 7. Wang W, Sun J C, Ye P, et al.miR‐22‐3p in the rostral ventrolateral medulla promotes hypertension through inhibiting β‐arrestin‐1.The Journal of Physiology.2023

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Lipid Metabolism Compound Library Covalent Inhibitor Library Anti-Metabolism Disease Compound Library Anti-Aging Compound Library Anti-Obesity Compound Library Bioactive Compound Library Exosome Compound Library

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Keywords

GW4869 6823-69-4 Metabolism Phospholipase Inhibitor GW554869A GW 4869 GW69A inhibit GW-4869 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.