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OG-L002
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。
OG-L002图片
CAS NO:1357302-64-7
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
OG-L002 是一种高度选择性的LSD1有效抑制剂,IC50为 0.02 μM。它抑制HSV IE基因的表达,还是单胺氧化酶抑制剂,对 MAO-A 和 MAO-B 的IC50分别为 1.38 μM 和 0.72 μM。

产品描述

OG-L002 is an effective and selective LSD1 inhibitor (IC50: 20 nM), showing 69- and 36-fold selectivity over MAO-A and MAO-B, respectively.

体外活性

OG-L002 potently inhibits HSV IE gene expression in both HeLa and HFF cells with IC50 of ~10 μM and ~3 μM , respectively. OG-L002 treatment (50 μM ) results in the reduced production of progeny virus with no significant toxicity in HeLa or HFF cells. OG-L002 (50 μM ) increases the levels of repressive chromatin on viral IE gene promoters. In addition, OG-L002 also represses the expression of hCMV IE genes and adenovirus E1A gene. [1]

体内活性

OG-L002 (6 to 40 mg/kg) represses HSV primary infection in a dose-dependent manner in a mouse model. Moreover, OG-L002 also represses HSV reactivation from latency in a mouse ganglion explant model. [1]

激酶实验

LSD1 demethylation assay: Human recombinant LSD1 protein is incubated with dimethylated H3K4 peptide as the substrate in the presence of various concentrations of lead compound inhibitors (0 to 75 μM ) or control tranylcypromine. The demethylase activity is measured by the release of Water2 produced during the catalytic process, using the Amplex red peroxide/peroxidase-coupled assay kit. Each reaction is done in triplicate. The maximum LSD1 demethylase activity is obtained in the absence of inhibitor and corrected for background fluorescence. The Ki (IC50) of OG-L002 is calculated as half-maximal activity.

细胞实验

HeLa or HFF cells are treated with the indicated concentrations of saponin (positive control) or compound OG-L002 for 12 hours. Cytotoxicity is determined using conditions recommended by the manufacturer and expressed as ratios to the cytotoxicity of the DMSO control.(Only for Reference)

Cas No.

1357302-64-7

分子式

C15H15NO

分子量

225.291

储存和溶解度

Ethanol:16 mg/mL (71 mM)
DMSO:42 mg/mL (186.4 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years