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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

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Quality Control

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

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

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In vivo
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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.

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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

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
(Cell-free assay)
20 nM
In vitro
TCN 201 partially inhibits the NMDA-induced intracellular Ca2+ response in a concentration-dependent manner with a pIC50 of 6.4. TCN 201 partially inhibits [3H]CGP 39653 specific binding showing a maximal radioligand displacement of 44%, respectively, and a pIC50 of 6.5. TCN 201 at a concentration of 10 μM does not protect against Tat-induced cell death, in contrast to ifenprodil and memantine. However, this same concentration of TCN 201 prevents Tat-induced synapse loss. TCN 201 inhibits synapse recovery after Tat-induced loss. TCN 201 demonstrates potent but GluN1 co-agonist concentration-dependent inhibition of GluN1/GluN2A NMDAR-mediated responses. TCN 201 causes substantially less inhibition of the TEVC current trace. TCN 201 is around 30-times more potent than TCN 213. In cortical neurones TCN 201 shows only modest antagonism of NMDAR-mediated currents recorded from young (DIV 9-10) neurones where GluN2B expression predominates. In older cultures (DIV 15-18) or in cultures where GluN2A subunits have been over-expressed TCN 201 gives a strong block that is negatively correlated with the degree of block produced by the GluN2B-selective antagonist, ifenprodil. TCN-201 binds to a novel allosteric site located at the dimer interface between the GluN1 and GluN2 agonist binding domains.
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.

References

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