OG-L002 HCl |
| رقم الكتالوجGC11792 |
LSD1 inhibitor,potent and specific
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1357298-75-9
Sample solution is provided at 25 µL, 10mM.
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OG-L002 is a specific and potent inhibitor of lysine (K)-specific demethylase 1A (LSD1) with IC50 value of 20 nM [1].
LSD1 is a flavin-dependent monoamine oxidase, which can demethylate lysines. LSD1 plays critical roles in oocyte growth, embryogenesis and tissue-specific differentiation [2].
OG-L002 potently inhibited HSV IE gene expression in both HFF and HeLa cells with IC50 of ~3 μM and ~10 μM, respectively. OG-L002 treatment can potently reduce production of progeny virus (~100-fold) with no significant toxicity in HeLa or HFF cells. 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. In addition, OG-L002 also repressed the expression of adenovirus E1A gene and hCMV IE genes [1].
In a mouse model, OG-L002 repressed primary HSV infection in a dose-dependent manner. Moreover, OG-L002 plays an important role in the viral latency-reactivation cycle in a mouse ganglion explant model [1].
References:
[1]. Liang Y, Quenelle D, Kristie TM, et al. A Novel Selective LSD1/KDM1A Inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency. mBio, 2013, 4(1), e00558-12.
[2]. Pedersen MT, Helin K. Histone demethylases in development and disease. Trends in Cell Biology, 2010, 20 (11): 662-71.
| Kinase experiment [1]: | |
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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. |
| Cell experiment [1]: | |
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Cell lines |
HeLa, HFF cells, MRC-5 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
50 μM for 12 hr; |
|
Applications |
OG-L002 inhibited HSV IE gene expression and progeny virus production in both HeLa and HFF cells. |
| Animal experiment [1]: | |
|
Animal models |
Mouse ganglion explant model |
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Dosage form |
2 to 40 mg/kg /day; intraperitoneal administration for 15-17 days |
|
Applications |
OG-L002 repressed herpes simplex virus (HSV) primary infection in vivo. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: 1Liang, Y., Quenelle, D., Vogel, J. L., Mascaro, C., Ortega, A. and Kristie, T. M. (2013) A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency. MBio. 4, e00558-00512 | |
| Cas No. | 1357298-75-9 | SDF | |
| Chemical Name | 4'-((1R,2S)-2-aminocyclopropyl)-[1,1'-biphenyl]-3-ol hydrochloride | ||
| Canonical SMILES | OC1=CC=CC(C2=CC=C([C@H]3C[C@@H]3N)C=C2)=C1.Cl | ||
| Formula | C15H16ClNO | M.Wt | 261.75 |
| الذوبان | ≥ 26.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8204 mL | 19.1022 mL | 38.2044 mL |
| 5 mM | 764.1 μL | 3.8204 mL | 7.6409 mL |
| 10 mM | 382 μL | 1.9102 mL | 3.8204 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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 as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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