您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > I-BET151(GSK1210151A)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
I-BET151(GSK1210151A)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
I-BET151(GSK1210151A)图片
CAS NO:1300031-49-5
规格:98%
分子量:415.44
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Selective BET inhibitor
CAS:1300031-49-5
分子式:C23H21N5O3
分子量:415.44
纯度:98%
存储:Store at -20°C

Background:

I-BET151 (GSK1210151A) is a selective inhibitor of BET with pIC50 value of 6.1 [1].
BET (bromo and extraterminal) is a member of bromodomain family and has been shown to be associated with a variety of diseases (human squamous cell carcinoma and other cancers). BET inhibitor has been implicated as a promising therapy for human cancer treatment [2].
I-BET151 is a selective BET inhibitor and has the similar inhibition function as TMZ. When tested with 6 myeloma cell lines, I-BET151 treatment decreased cells percent in S/G2 phase and increased cell apoptosis in a time- and dose- dependent manner [2]. In globlastoma cell line U87MG, administration of I-BET151 arrested cells in the G1 phase and reduced cell proliferation ability [3].
When treated with myeloma implanted mouse model with I-BET151, it reduced tumor volume in a four- or five- fold compared with control group [2]. In immunocompromised mouse model with U87MG cells xenograft, administration of I-BET151 in a concentration of 10 mg/kg i.p. daily significantly reduced tumor volume compared with saline treated group [3].
参考文献:
[1].    Seal, J., et al., Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett, 2012. 22(8): p. 2968-72.
[2].    Chaidos, A., et al., Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood, 2014. 123(5): p. 697-705.
[3].    Chan, C.H., et al., BET bromodomain inhibition suppresses transcriptional responses to cytokine-Jak-STAT signaling in a gene-specific manner in human monocytes. Eur J Immunol, 2015. 45(1): p. 287-97.