现货,JNJ-26481585,CAS号:875320-29-9,美国进口, HDAC-HSP-Aurora,HDAC ,HDAC 抑制剂和化合物,selleck,S1096

信号转导通路: HDAC-HSP-Aurora >> HDAC >> HDAC 抑制剂和化合物 >> JNJ-26481585http://selleck.cn/jnj-26481585-S1096.html

技术数据:

分子量(MW): 394.476

化学式:

C21H26N6O2

 

溶解度: DMSO ≥79mg/mL Water ≥50mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 875320-29-9

生物活性

 

 

JNJ-26481585 is an orally bioavailable, second-generation, hydroxamic acid-based HDAC inhibitor with an IC50 of 2.43 nM for 5T33MMvt cells. JNJ-26481585 has potential antineoplastic activity. HDAC inhibitor JNJ-26481585 inhibits HDAC leading to an accumulation of highly acetylated histones, which may result in an induction of chromatin remodeling; inhibition of the transcription of tumor suppressor genes; inhibition of tumor cell division; and the induction of tumor cell apoptosis. [1] In vitro, JNJ-26481585 induced caspase cascade activation and upregulation of p21, resulting in apoptosis and cell cycle arrest in the myeloma cells at low nanomolar concentrations. When the 5T2MM-bearing mice were treated with JNJ-26481585, there were a reduction of the tumor load and a significant decrease in angiogenesis. [2]

 

 

 

 

 

参考文献

Bortezomib Alone or in Combination with the Histone Deacetylase Inhibitor JNJ-26481585: Effect on Myeloma Bone Disease in the 5T2MM Murine Model of Myeloma Miguel Lemaire, Janine Arts, et al. Cancer Res 2009;69:5307-5311

The effects of JNJ-26481585, a novel hydroxamate-based histone deacetylase inhibitor,on the development of multiple myeloma in the 5T2MM and 5T33MM murine models S Deleu,M Lemaire,et al. Leukemia 2009;23:1894–1903

 

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