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BRD6688
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。
BRD6688图片
CAS NO:1404562-17-9
规格:98%
分子量:282.3
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
HDAC inhibitor
CAS:1404562-17-9
分子式:C16H18N4O
分子量:282.3
纯度:98%
存储:Store at -20°C

Background:

IC50: 21 nM, 100 nM, and 11.48 μM for HDAC1, 2, and 3, respectively


BRD6688 is an HDAC inhibitor.


A few chromatin modifying enzymes have been implicated in the neurobiology of learning and memory, especially, histone deacetylases (HDACs). HDACs are responsible for catalyzing the posttranslational hydrolysis of acetyl groups from the 3-nitrogen of lysine residues of histone and non-histone proteins.


In vitro: BRD6688 was found to demonstrate kinetic selectivity for HDAC2 against HDAC1, an isoform with 95% similarity within the catalytic binding domain. Moreover, BRD6688 could increase histone acetylation (H4K12 and H3K9) in primary mouse neuronal cultures [1].


In vivo: Mouse in-vivo study showed that BRD6688 was able to increase the histone acetylation (H4K12 and H3K9) in hippocampal CA1 neurons of CK-p25 mice. Moreove, the increased histone acetylation in brain served as a surrogate pharmacodynamic marker of HDAC engagement and was consistent with previously observed brain pharmacokinetic properties. In addition, BRD6688 rescued the cognitive deficits in CK-p25 mice, a model of neurodegeneration, in a Pavlovian fear conditioning behavioral assay [1].


Clinical trial: So far, no clinical study has been conducted.


Reference:
[1] Wagner, F. F.,Zhang, Y.-L.,Fass, D.M., et al. Kinetically selective inhibitors of histone deacetylase 2 (HDAC2) as cognition enhancers. Chem.Sci. 6(1), 804-815 (2015).