| BizineLSD1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity ≥ 95.00%
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- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 1591932-50-1 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | N-[4-(2-hydrazinylethyl)phenyl]-benzenebutanamide | ||
| Canonical SMILES | NNCCC(C=C1)=CC=C1NC(CCCC2=CC=CC=C2)=O | ||
| Formula | C18H23N3O | M.Wt | 297.4 |
| Solubility | ≤25mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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).
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个人感觉这个就是厂家的一个噱头，，，听说有人已经在无抗猪肉中发现抗药性细菌，不知是真是假，不过要买的话一定要去信誉的地方。
以上回答，希望对你有用。
