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N-羟基-4-[(1,2,3,4-四氢-2-甲基-5H-吡啶并[4,3-B]吲哚-5-基)甲基]苯甲酰胺盐酸盐

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  • 供应商：上海经科化学科技有限公司 


    服务热线：400-0199-638 


    QQ:472482400(上海经科）


    微信号：shjkchem 


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    本试剂(N-羟基-4-[(1,2,3,4-四氢-2-甲基-5H-吡啶并[4,3-B]吲哚-5-基)甲基]苯甲酰胺盐酸盐)
    仅供科研实验使用,不得用于其他用途！
     

    简介：
    货 号：LC1-T-5335
    名   称：N-羟基-4-[(1,2,3,4-四氢-2-甲基-5H-吡啶并[4,3-B]吲哚-5-基)甲基]苯甲酰胺盐酸盐
    别   名：Tubastatin A Hydrochloride Salt
    C A S ：1310693-92-5
    分子量    ：371.86
    分子式：C20H21N3O2HCl
    纯   度：HPLC/TLC:>99%
    说   明：
    文   献    ：Tubastatin A is a histone deacetylase (HDAC) 6 inhibitor. It inhibited HDAC6 with an IC50 of 15 nM, also inhibited HDAC1 (IC50 = 16.4 μM) and HDAC8 (IC50 = 0.85 μM), but not other HDACs (IC50 > 30 μM). It induced the acetylation of [alpha]-tubulin and protected primary cortical neurons against glutathione depletion-induced oxidative stress. Butler K.V., et al. "Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A." J. Am. Chem. Soc. 132: 10842-10846 (2010).Tubastatin A restored the expression of primary cilia in cholangiocarcinoma cell lines, decreased cell proliferation, and inhibited anchorage-independent growth. These effects of tubastatin A were blocked by stable transfection of IFT88-shRNA, which prevented cholangiocarcinoma cells from regenerating cilia. Tubastatin A also inhibited the tumor growth in a cholangiocarcinoma animal model. Gradilone S.A., et al. "HDAC6 inhibition restores ciliary expression and decreases tumor growth." Cancer Res. 73: 2259-2270 (2013).HDAC6 inhibition either by HDAC6 knockout or with tubastatin A promoted Foxp3(+) T-regulatory cell inhibitory activity in models of inflammation and autoimmunity. It blocked the development and progression of murine colitis and prevented allograft rejection in mice. de Zoeten E.F., et al. "Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells." Mol. Cell Biol. 31: 2066-2078 (2011).
     
    温馨提示：不可用于临床ZL。
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