OG-L002

製品コードS7237 バッチS723701

印刷

化学情報

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）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.000mg/ml (4.44mM)	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は、無細胞アッセイにおいて20 nMのIC50を示す強力で特異的なLSD1阻害剤であり、MAO-BおよびMAO-Aに対してそれぞれ36倍および69倍の選択性を示します。
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.
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.
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
キナーゼアッセイ	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 K_i (IC50) of this compound 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

参考

https://pubmed.ncbi.nlm.nih.gov/23386436/

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：

Seclidemstat (SP-2577) Induces Transcriptomic Reprogramming and Cytotoxicity in Multiple Fusion-Positive Sarcomas [ Cancer Res Commun, 2025, 5(9):1584-1598]	PubMed: 40852926
N'-(1-phenylethylidene)-benzohydrazide cytotoxicity is LSD1 independent and linked to Fe-S cluster disruption in Ewing sarcoma [ bioRxiv, 2025, 2025.06.20.660795]	PubMed: 40666939
Potential role of lipophagy impairment for anticancer effects of glycolysis-suppressed pancreatic ductal adenocarcinoma cells [ Cell Death Discov, 2024, 10(1):166]	PubMed: 38580661
Seclidemstat blocks the transcriptional function of multiple FET-fusion oncoproteins [ bioRxiv, 2024, 2024.05.19.594897]	PubMed: 38826330
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

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。