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WT-161
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。
WT-161图片
CAS NO:1206731-57-8
规格:98%
分子量:458.55
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.
CAS:1206731-57-8
分子式:C27H30N4O3
分子量:458.55
纯度:98%
存储:Store at -20°C

Background:

WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.


WT161 selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin (Ac-α-tubulin) with little effect on global lysine acetylation. WT161 induces significant toxicity in all multiple myeloma cell lines tested, with IC50s between 1.5 and 4.7 uM . WT161 in combination with bortezomib triggers significant accumulation of polyubiquitinated proteins and cell stress, followed by caspase activation and apoptosis. More importantly, this combination treatment is effective in bortezomib-resistant cells and in the presence of bone marrow stromal cells, which have been shown to mediate multiple myeloma cell drug resistance[1].


WT161 shows toxicity at 100 mg/kg i.p., but WT161 is well tolerated at 50 mg/kg i.p.. Bortezomib combined with WT161 demonstrates a significant antitumor effect[1].


参考文献:
[1]. Hideshima T, et al. Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma. Proc Natl Acad Sci U S A. 2016 Nov 15;113(46):13162-13167.