现货,ITF2357 (Givinostat) ,CAS号: 732302-99-7,美国进口, HDAC-HSP-Aurora , HDAC , HDAC 抑制剂,selleck,S2170

信号转导通路: HDAC-HSP-Aurora >> HDAC >> HDAC 抑制剂 >> ITF2357 (Givinostat)http://www.selleck.cn/itf2357-givinostat-S2170.html

技术数据:

分子量(MW): 475.97

化学式:

C24H27N3O4.HCl.H2O

 

溶解度: DMSO ≥95mg/mL Water ≥2mg/mL Ethanol ≥9mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 732302-99-7

生物活性

 

 

ITF2357 (Givinostat) is a noverl HDAC inhibitor with IC50 of 10, 7.5 and 16 nM for maize HDAC preparations HD2, HD-1B and HD-1A, respectively. ITF2357 (Givinostat) inhibits both class I and class II HDAC. ITF2357 (Givinostat) induces apoptosis of MM and acute myelogenous leukemia (AML) cells and this apoptosis takes place following induction of p21 and down-modulation of Bcl-2 and Mcl-1 proteins. When tested on normal cells, ITF2357 (Givinostat) inhibits the production of pro-inflammatory cytokines such as IL-1, IL-6, tumor necrosis factor (TNF)-α, and interferon (IFN)-γ by peripheral blood mononuclear cells and of IL-6 and vascular endothelium growth factor (VEGF) by mesenchymal stromal cells. ITF2357 (Givinostat) reduced the total intracellular IL-1α synthesis in freshly obtained PBMCs with 50% inhibition at concentrations below 25 nM. [1][2][3][4]

 

 

 

参考文献

The oral histone deacetylase inhibitor ITF2357 reduces cytokines and protects islet beta-cells in vivo and in vitro Eli C. Lewis,Lykke Blaabjerg,et al. Molecular Medicine ;Lewis,. et al page 1

Pleiotropic anti-myeloma activity of ITF2357: inhibition of interleukin-6 receptor signaling and repression of miR-19a and miR-19b Katia Todoerti,Valentina Barbui,et al. Haematologica 2010;95:260-269

Histone deacetylase inhibitor ITF2357 is neuroprotective, improves functional recovery, and induces glial apoptosis following experimental traumatic brain injury Naama A. Shein,Nikolaos Grigoriadis,et al. The FASEB Journal December 2009;23:4266-4275

http://en.wikipedia.org/wiki/Givinostat http://en.wikipedia.org/wiki/Givinostat ;

 

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