product name OG-L002
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. OG-L002 potently inhibited HSV IE gene expression in both HFF and HeLa cells with IC50 of ~3 μM and ~10 μM, respectively. In chromatin immunoprecipitation assays, OG-L002 increased the levels of total histone H3K9-me2 and H3 (20- to 30-fold) associated with viral IE promoters, which resulted in decreased viral IE gene expression.
References: Nature. 2012 Aug 16;488(7411):404; Trends Cell Biol. 2010 Nov;20(11):662-71.
225.29
Formula
C15H15NO
CAS No.
1357302-64-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 45 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: 45 mg/mL (199.7 mM)
Solubility (In vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 20 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19428236
| In Vitro |
In vitro activity: 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 Kinase Assay: 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 Cell Assay: 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. |
|---|---|
| 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. |
| Animal model | BALB/c female mice are infected with HSV-2 (strain MS). |
| Formulation & Dosage | Dissolved in DMSO; 50 mg/kg; i.p. |
| References | Nature. 2012 Aug 16;488(7411):404; Trends Cell Biol. 2010 Nov;20(11):662-71. |
