Antibodies
OG-L002
- 貨號 Cat. No.
- S7237
- 規格 Size
- 5mgã€25mg
- 品牌 Brand
- Selleckchem
Description
OG-L002
Catalog No.S7237
OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively. | |||||
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| Targets | LSD1 | |||||
| IC50 | 20 nM [1] | |||||
| 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. |
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Cell Assay: [1]
| Cell lines | HeLa and HFF cells |
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| 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). |
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| Dosages | ~50 mg/kg |
| Administration | Intraperitoneal administration |
| Solubility | 1% DMSO/30% polyethylene glycol/1% Tween 80, 20 mg/mL |
References
Chemical Information
| Molecular Weight (MW) | 225.29 |
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| Formula | C15H15NO |
| CAS No. | 1357302-64-7 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 45 mg/mL (199 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 19 mg/mL (84 mM) | ||
| 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 |
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