research use only
Cat.No.S7237
| Related Targets | HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK |
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| Other Histone Demethylase Inhibitors | GSK-J4 Hydrochloride SP2509 GSK-LSD1 2HCl Ladademstat (ORY-1001) Dihydrochloride JIB-04 CPI-455 HCl IOX1 GSK J1 ML324 CPI-455 |
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In vitro |
DMSO
: 45 mg/mL
(199.74 mM)
Ethanol : 19 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 225.29 | Formula | C15H15NO |
Storage (From the date of receipt) | |
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| CAS No. | 1357302-64-7 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | C1C(C1N)C2=CC=C(C=C2)C3=CC(=CC=C3)O | ||
| Features |
This selective LSD1 inhibitor was discovered in 2013. Potential for use in viral diseases such as HSV and VZV.
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| Targets/IC50/Ki |
LSD1
(Cell-free assay) 20 nM
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| 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.
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| Kinase Assay |
LSD1 demethylation assay
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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.
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| 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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