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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Effect of treatment on equine herpesvirus type 1 (EHV-1) viral load during lytic infection of primary equine fetal kidney cells. At 24 hpi, reduced EHV-1 DNA copies per cell were detected in the presence of ganciclovir (**p = 0.0005) or OG-L002 (*p = 0.005), and markedly when both treatments (***p < 0.0001) were applied simultaneously in comparison with DMSO control vehicle. Combined treatment decreased the number of EHV-1 DNA copies in comparison to treatment with ganciclovir alone (p = 0.01) or OG-L002 alone (p = 0.001). Lines represent mean values.
Front Vet Sci, 2018, 5:34. OG-L002 purchased from Selleck.
Hepa1c1c7 cells were seeded in 6 well plates. The following day, cells were treated with either 100 nM of Dex for 1 hours, 5mM of VPA for 2 hours, the respective LSD1 inhibitor, or a combination. In terms of LSD1 inhibitor treatment, cells were dosed with 50 uM (Ampd3) or 100 uM (Hbegf) of OG-L002 for 24 hours. Cells were then harvested, and isolated RNA underwent RT-qPCR using intron-exon primers to measure expression of nascent transcripts. For each of the LSD1 inhibitors used, a representative GR activated (Ampd3) and repressed (Hbegf) gene was analyzed. Error bars represent SEM. Statistical analysis using a paired t test was performed, but none of the results demonstrated significance.
The University of Arizona, 2016. OG-L002 purchased from Selleck.
Purity & Quality Control
Choose Selective Histone Demethylase Inhibitors
|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.|
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. 
|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. |
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.
|In vitro||DMSO||45 mg/mL (199.74 mM)|
|Ethanol||19 mg/mL (84.33 mM)|
|In vivo||Add solvents to the product individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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.
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