Catalog No.S7237

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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OG-L002 Chemical Structure

OG-L002 Chemical Structure
Molecular Weight: 225.29

Validation & Quality Control

Cited by 1 publications:

Quality Control & MSDS

Product Information

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  • Research Area
  • Inhibition Profile

Product Description

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.
Targets LSD1 [1]
(Cell-free assay)
IC50 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]
Features This selective LSD1 inhibitor was discovered in 2013. Potential for use in viral diseases such as HSV and VZV.

Protocol(Only for Reference)

Kinase Assay: [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 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 Assay: [1]

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.

Animal Study: [1]

Animal Models BALB/c female mice are infected with HSV-2 (strain MS).
Formulation DMSO
Dosages ~50 mg/kg
Administration Intraperitoneal administration

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] MBio. 2013, 4(1), e00558-12.

Chemical Information

Download OG-L002 SDF
Molecular Weight (MW) 225.29


CAS No. 1357302-64-7
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
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 Name [1,1'-Biphenyl]-3-ol, 4'-[(1R,2S)-2-aminocyclopropyl]-4'-((1R,2S)-2-Aminocyclopropyl)biphenyl-3-o

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.

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