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CAS No.: 6823-69-4

GW4869 Catalog No. CSN20418

Synonyms: GW 4869 (hydrochloride hydrate);GW-69A;GW-554869A

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.

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实验方案

技术信息

生物活性

描述The activation of neutral magnesium-dependent sphingomyelinase (N-SMase) has been observed after the stimulation of p75 neurotropin receptor. GW4869 dihydrochloride is a noncompetitive inhibitor of N-SMase in vitro with an IC50 value of 1μM. In MCF7 breast cancer cells, GW4869 at 10μM partially but significantly suppressed TNF-induced sphingomyelin hydrolysis, while 20μM of this inhibitor completely inhibited the loss of sphingomyelin. The addition of GW4869 at 10 and 20μM also completely inhibited the initial accumulation of ceramide. The presence of GW4869 at 10 and 20μM successfully reduced TNF-induced cell death and significantly protected cells from nuclear condensation after TNF treatment in a dose-dependent manner. The same doses of GW4869 also reduced the number of cells that were positive for chromatin condensation. Preincubation of MCF7 cells with 10μM GW4869 partially blocked TNF-caused cleavage of PARP, whereas 20μM of this compound completely prevented the cleavage. Moreover, 10 and 20μM of GW4869 significantly protected the release of cytochrome c from mitochondria into the cytosol in a dose-dependent manner^[3]. In 5XFAD mice, intraperitoneal injection of GW4869 (2 – 2.5µg/g body weight) every 48h for six weeks decreased the levels of brain and serum exosomes, brain ceramide, and Aβ1-42 plaque load as compared to the DMSO-treated group^[4].
动物研究
剂量
Rat: 4 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Rat: 4 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Vuckovic S, Vandyke K, et al. The cationic small molecule GW4869 is cytotoxic to high phosphatidylserine-expressing myeloma cells. Br J Haematol. 2017 May;177(3):423-440.
[2] Kolmakova A, Kwiterovich P, et al. Apolipoprotein C-I induces apoptosis in human aortic smooth muscle cells via recruiting neutral sphingomyelinase. Arterioscler Thromb Vasc Biol. 2004 Feb;24(2):264-9.
[3] Luberto C, Hassler DF, Signorelli P, Okamoto Y, Sawai H, Boros E, Hazen-Martin DJ, Obeid LM, Hannun YA, Smith GK. 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.
[4] Dinkins MB, Dasgupta S, Wang G, Zhu G, Bieberich E. 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7316 mL
- 8.6580 mL
- 17.3160 mL
- 5 mM
- 0.3463 mL
- 1.7316 mL
- 3.4632 mL
- 10 mM
- 0.1732 mL
- 0.8658 mL
- 1.7316 mL

技术信息

CAS号

6823-69-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H30Cl2N6O2

运输

蓝冰

分子量

577.50

别名

GW 4869 (hydrochloride hydrate);GW-69A;GW-554869A;GW-4869 2HCl

溶解度

DMSO	1.0 mg/mL (1.7 mM) warming
Water	insoluble

动物实验配方

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