产品描述
| 溶解性 |
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| 存贮条件 | 储存温度-20°C |
| 产品介绍 | Rocilinostat (ACY-1215)是一种选择性HDAC6抑制剂， IC50为5 nM，作用于HDAC6比作用于HDAC1/2/3(I型HDACs)选择性高10倍以上，对HDAC8具有微弱的作用活性，对HDAC4/5/7/9/11， Sirtuin1和Sirtuin2具有最低限度的作用活性。 |
| 备注 | Rocilinostat (ACY-1215) is a selective HDAC6 inhibitor with IC50 of 5 nM. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtu |
| 生化机理 |
ACY-1215 is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity. ACY-1215 selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through hyperacetylation of Hsp90 and preventing the subsequent aggresomal protein degradation. This leads to an accumulation of unfolded and misfolded ubiquitinated proteins and may eventually induce cancer cell apoptosis, and inhibition of cancer cell growth. HDAC6, a class II HDAC deacetylase located in the cytoplasm, appears to play a key role in the formation and activation of the aggresomes needed for degradation of misfolded proteins. Compared to non-selective HDAC inhibitor, ACY-1215 is able to reduce the toxic effects on normal, healthy cells. |
| 别名 | 2-(二苯基氨基)-N-[7-(羟基氨基)-7-氧代庚基]-5-嘧啶甲酰胺;Rocilinostat;ACY1215;ACY 1215;2-(Diphenylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]-5-pyrimidinecarboxamide |
