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.

LSD1:20 nM

OG-L002 在HeLa和HFF细胞中强效抑制HSV IE基因表达，其IC50分别约为10μM和3μM。50μM的OG-L002处理导致子代病毒产量减少，且在HeLa或HFF细胞中未显示出显著毒性。此外，50μM的OG-L002增加了病毒IE基因启动子上抑制性染色质的水平，并抑制了hCMV IE基因和腺病毒E1A基因的表达。[1]

OG-L002（6至40 mg/kg）在小鼠模型中以剂量依赖的方式抑制HSV初次感染。此外，OG-L002还能在小鼠神经节解剖模型中抑制HSV从潜伏状态的复发。[1]

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.

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)