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OG-L002

现货
Catalog No.
B1580
LSD1抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,000.00
现货
5mg
¥ 1,030.00
现货
25mg
¥ 3,990.00
现货

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Background

OG-L002 is a specific and potent inhibitor of lysine (K)-specific demethylase 1A (LSD1) with IC50 value of 20 nM [1].
LSD1 is a flavin-dependent monoamine oxidase, which can demethylate lysines. LSD1 plays critical roles in oocyte growth, embryogenesis and tissue-specific differentiation [2].
OG-L002 potently inhibited HSV IE gene expression in both HFF and HeLa cells with IC50 of ~3 μM and ~10 μM, respectively. OG-L002 treatment can potently reduce production of progeny virus (~100-fold) with no significant toxicity in HeLa or HFF cells. In chromatin immunoprecipitation assays, OG-L002 increased the levels of total histone H3K9-me2 and H3 (20- to 30-fold) associated with viral IE promoters, which resulted in decreased viral IE gene expression. In addition, OG-L002 also repressed the expression of adenovirus E1A gene and hCMV IE genes [1].
In a mouse model, OG-L002 repressed primary HSV infection in a dose-dependent manner. Moreover, OG-L002 plays an important role in the viral latency-reactivation cycle in a mouse ganglion explant model [1].
References:
[1]. Liang Y, Quenelle D, Kristie TM, et al. A Novel Selective LSD1/KDM1A Inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency. mBio, 2013, 4(1), e00558-12.
[2]. Pedersen MT, Helin K. Histone demethylases in development and disease. Trends in Cell Biology, 2010, 20 (11): 662-71.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt225.29
Cas No.1357302-64-7
FormulaC15H15NO
Solubility≥22.5mg/mL in DMSO
Chemical Name3-[4-[(1R,2S)-2-aminocyclopropyl]phenyl]phenol
SDFDownload SDF
Canonical SMILESC1C(C1N)C2=CC=C(C=C2)C3=CC(=CC=C3)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验 [1]:

LSD1去甲基化分析

将人重组LSD1蛋白与二甲基化H3K4肽作为底物在各种浓度的先导化合物抑制剂(0至75 μM)或对照反苯环丙胺存在下温育。 通过使用Amplex红色过氧化物/过氧化物酶偶联测定试剂盒在催化过程中释放产生的H2O2来测量去甲基化酶活性,每个反应一式三份进行。在不存在抑制剂的情况下获得最大LSD1去甲基化酶活性,并校正背景荧光。OG-L002的Ki(IC50)计算为半数最大活性。

细胞实验 [1]:

细胞系

HeLa细胞、HFF细胞、MRC-5细胞

溶解方法

该化合物在DMSO中的溶解度> 10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应时间

50 μM处理12小时;

应用

OG-L002抑制HeLa和HFF细胞中的HSV IE基因表达和子代病毒的产生。

动物实验 [1]:

动物模型

小鼠神经节移植模型

剂量

2-40 mg / kg /天; 腹腔内给药15-17天

应用

OG-L002在体内抑制单纯疱疹病毒(HSV)原发感染。

注意事项

请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

1Liang, Y., Quenelle, D., Vogel, J. L., Mascaro, C., Ortega, A. and Kristie, T. M. (2013) A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency. MBio. 4, e00558-00512

生物活性

Description OG-L002是一种有效的和特异性的LSD1抑制剂,IC50值为20 nM。
靶点 LSD1          
IC50 20 nM          

质量控制

化学结构

OG-L002