OG-L002

Catalog No.S7237

OG-L002 Chemical Structure

Molecular Weight(MW): 225.29

OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM in a cell-free assay, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively.

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Choose Selective Histone Demethylase Inhibitors

Biological Activity

Description OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM in a cell-free assay, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively.
Features This selective LSD1 inhibitor was discovered in 2013. Potential for use in viral diseases such as HSV and VZV.
Targets
LSD1 [1]
(Cell-free assay)
20 nM
In vitro

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]

In vivo 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]

Protocol

Kinase Assay:[1]
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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 H2O2 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.
Cell Research:[1]
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  • Cell lines: HeLa and HFF cells
  • Concentrations: ~50 μM
  • Incubation Time: 12 hours
  • Method: 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)
Animal Research:[1]
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  • Animal Models: BALB/c female mice are infected with HSV-2 (strain MS).
  • Formulation: DMSO
  • Dosages: ~50 mg/kg
  • Administration: Intraperitoneal administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 45 mg/mL (199.74 mM)
Ethanol 19 mg/mL (84.33 mM)
Water <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 20 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 225.29
Formula

C15H15NO

CAS No. 1357302-64-7
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Histone Demethylase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID