GSK-LSD1 2HCl

製品コードS7574 バッチS757401

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

C₁₄H₂₂Cl₂N₂

分子量

289.24

CAS No.

2102933-95-7

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

57 mg/mL (197.06 mM)

Water (warmed with 50ºC water bath)

57 mg/mL (197.06 mM)

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%PEG300 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。	2.850mg/ml (9.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 57 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil 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。	0.470mg/ml (1.62mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	GSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B).
in vitro	GSK-LSD1 induces gene expression changes in cancer cell lines with average EC50 of < 5 nM and inhibits cancer cell line growth with average EC50 of < 5 nM. ^[1]
in vivo	GSK-LSD1, a highly selective inhibitor of KDM1A, significantly inhibits thyroid cancer progression and enhances the sensitivity of thyroid cancer to chemotherapy.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	U2OS cells
	濃度	200 μM
	反応時間	12 h
	実験の流れ	Cells were treated with indicated concentration of drug for 12 h.
動物実験	動物モデル	Nude mice
	投薬量	1 mg/kg
	投与方法	i.p.

参考

http://www.thesgc.org/chemical-probes/GSK-LSD1
https://pubmed.ncbi.nlm.nih.gov/28800922/
https://pubmed.ncbi.nlm.nih.gov/35198054/

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：

Perturbing LSD1 and WNT rewires transcription to synergistically induce AML differentiation [ Nature, 2025, 10.1038/s41586-025-08915-1]	PubMed: 40240608
Methylstat sensitizes ovarian cancer cells to PARP-inhibition by targeting the histone demethylases JMJD1B/C [ Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z]	PubMed: 39915607
Quantitation of global histone post-translational modifications reveal anti-inflammatory epigenetic mechanisms of liquiritigenin based on the optimized super-SILAC strategy [ Front Cell Dev Biol, 2025, 13:1566567]	PubMed: 40213392
Transposable elements-mediated recruitment of KDM1A epigenetically silences HNF4A expression to promote hepatocellular carcinoma [ Nat Commun, 2024, 15(1):5631]	PubMed: 38965210
Inhibition of LSD1 induces ferroptosis through the ATF4-xCT pathway and shows enhanced anti-tumor effects with ferroptosis inducers in NSCLC [ Cell Death Dis, 2023, 10.1038/s41419-023-06238-5]	PubMed: 37923740
Insect immunity and its interactions with microorganisms and parasitoids [ Front Immunol, 2023, ]	PubMed: none
Disease-associated KBTBD4 mutations in medulloblastoma elicit neomorphic ubiquitylation activity to promote CoREST degradation [ Cell Death Differ, 2022, 10.1038/s41418-022-00983-4]	PubMed: 35379950
KDM1A promotes thyroid cancer progression and maintains stemness through the Wnt/β-catenin signaling pathway [ Theranostics, 2022, 12(4):1500-1517]	PubMed: 35198054
BmCPV-Derived Circular DNA vcDNA-S7 Mediated by Bombyx mori Reverse Transcriptase (RT) Regulates BmCPV Infection [ Front Immunol, 2022, 13:861007]	PubMed: 35371040
BmCPV-Derived Circular DNA vcDNA-S7 Mediated by Bombyx mori Reverse Transcriptase (RT) Regulates BmCPV Infection [ Front Immunol, 2022, 13:861007]	PubMed: 35371040

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。