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Bizine
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。
Bizine图片
CAS NO:1591932-50-1
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
Bizine 是一种苯乙肼类似物,是一种有效的选择性 LSD1 抑制剂,b>Ki 为 59 nM。
Cas No.1591932-50-1
化学名N-[4-(2-hydrazinylethyl)phenyl]-benzenebutanamide
Canonical SMILESNNCCC(C=C1)=CC=C1NC(CCCC2=CC=CC=C2)=O
分子式C18H23N3O
分子量297.4
溶解度≤25mg/ml in DMSO;20mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ki(inact) = 59 nM

Bizine is a LSD1 inhibitor.

Lysine-specific demethylase 1 (LSD1), an epigenetic enzyme, can oxidatively cleave methyl groups from monomethyl and dimethyl Lys4 of histone H3 and can also contribute to gene silencing.

In vitro: In a previous study, bizine, a novel phenelzine analogue with a phenyl-butyrylamide appendage, was foundto be a potent in vitro LSD1 inhibitor and was selective against monoamine oxidases A/B and LSD2, the LSD1 homologue. Moreover, in cancer cells, bizine was shown to be effective at modulating bulk histone methylation and the ChIP-seq experiment demonstrated a statistically significant overlap in the H3K4 methylation pattern of genes affected by bizine and those altered in LSD1-/- cells. In addition, the treatment of two cancer cell lines, LNCaP and H460, with bizine led to a reduction in proliferation rate, and bizine also showed additive to synergistic effects on cell growth when used in combination with two tested HDAC inhibitors. Furthermore, neurons exposed to oxidative stress could be protected by the treatment of bizine, indicating its potential applications in neurodegenerative disease [1].

In vivo: Up to now, there is no animal in vivo data reported.

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

Reference:
[1] Prusevich, P. ,Kalin, J.H.,Ming, S.A., et al. A selective phenelzine analogue inhibitor of histone demethylase LSD1. ACS Chem Biol. 9, 1284-1293 (2014).