OG-L002

製品コードS7237 バッチS723701

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H15NO
分子量 225.29 CAS No. 1357302-64-7
Solubility (25°C)* 体外 DMSO 45 mg/mL (199.74 mM)
Ethanol 19 mg/mL (84.33 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG 300 5%Tween80 50% ddH2O
1.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 20 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify; add 50 μL Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]
特徴 This selective LSD1 inhibitor was discovered in 2013. Potential for use in viral diseases such as HSV and VZV.

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 HeLa and HFF cells
濃度 ~50 μM
反応時間 12 hours
実験の流れ 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.
動物実験 動物モデル BALB/c female mice are infected with HSV-2 (strain MS).
投薬量 ~50 mg/kg
投与方法 Intraperitoneal administration

カスタマーフィードバック

Data from [Data independently produced by , , Cell Death Dis, 2018, 9(10):1038]

Data from [Data independently produced by , , Front Vet Sci, 2018, 5:34]

Data from [Data independently produced by , , The University of Arizona, 2016]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Evaluation of Histone Demethylase Inhibitor ML324 and Acyclovir against Cyprinid herpesvirus 3 Infection [ Viruses, 2023, 15(1)163] PubMed: 36680202
LSD1-mediated demethylation of OCT4 safeguards pluripotent stem cells by maintaining the transcription of PORE-motif-containing genes [ Sci Rep, 2021, 11(1):10285] PubMed: 33986438
Chromatin binding of FOXA1 is promoted by LSD1-mediated demethylation in prostate cancer [ Nat Genet, 2020, 52(10):1011-1017] PubMed: 32868907
Targeted DNA oxidation by LSD1-SMAD2/3 primes TGF-β1/ EMT genes for activation or repression [ Nucleic Acids Res, 2020, gkaa599] PubMed: 32697292
Chronic IL-1β-induced inflammation regulates epithelial-to-mesenchymal transition memory phenotypes via epigenetic modifications in non-small cell lung cancer. [ Sci Rep, 2020, 10(1):377] PubMed: 31941995
Hdac1 Regulates Differentiation of Bipotent Liver Progenitor Cells During Regeneration via Sox9b and Cdk8. [ Gastroenterology, 2019, 156(1):187-202] PubMed: 30267710
Eradication of Central Nervous System Leukemia of T-Cell Origin with a Brain-Permeable LSD1 Inhibitor [Saito S Clin Cancer Res, 2018, 10.1158/1078-0432] PubMed: 30518632
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] PubMed: 30135193
Increasing G9a automethylation sensitizes B acute lymphoblastic leukemia cells to glucocorticoid-induced death [Poulard C Cell Death Dis, 2018, 9(10):1038] PubMed: 30305606
Lysine-specific demethylase 1 inhibitors prevent teratoma development from human induced pluripotent stem cells. [ Oncotarget, 2018, 9(5):6450-6462] PubMed: 29464084

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。