Home Epigenetics Histone Demethylase inhibitor - LSD1 inhibitor OG-L002

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OG-L002 Histone Demethylase inhibitor

Cat.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.
OG-L002 Histone Demethylase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 225.29

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S723701 DMSO]45 mg/mL]false]Ethanol]19 mg/mL]false]Water]Insoluble]false Purity: 99.8%
99.8

Chemical Information, Storage & Stability

Molecular Weight 225.29 Formula

C15H15NO

 Storage (From the date of receipt)
CAS No. 1357302-64-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1C(C1N)C2=CC=C(C=C2)C3=CC(=CC=C3)O

Solubility

In vitro
Batch:

DMSO : 45 mg/mL (199.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Features
This selective LSD1 inhibitor was discovered in 2013. Potential for use in viral diseases such as HSV and VZV.
Targets/IC50/Ki
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. This compound treatment (50 μM ) results in the reduced production of progeny virus with no significant toxicity in HeLa or HFF cells. It (50 μM ) increases the levels of repressive chromatin on viral IE gene promoters. In addition, this chemical also represses the expression of hCMV IE genes and adenovirus E1A gene. [1]
Kinase Assay
LSD1 demethylation assay
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 this compound is calculated as half-maximal activity.
In vivo

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

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