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 GSK2879552,LSD1Inhibitor M60297-2s|产品详情|进口橙子视频旧款采购网




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    上海橙子视频app安卓下载生物科技公司
    Tel:400-968-7988    021-33779008
    GSK2879552,LSD1Inhibitor
    品牌:Xcessbio
    货号:M60297-2s
    规格:2 mg solid
    货期:

    GSK2879552,LSD1Inhibitor

    商品详情 参考文献 相关资料
    Product Information
    Molecular Weight: 437.41
    Formula: C23H28N2O2.2HCl
    Purity: ≥98%
    CAS#: 1401966-69-5
    Solubility: DMSO up to 50 mM; Water up to 50 mM
    Chemical Name: 4-((4-((((1R,2S)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)benzoic acid hydrochloride
    Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

    Biological Activity:

    GSK2879552 is a highly potent, selective and orally bioavailable irreversible inhibitor of Lysine Specific Demethylase 1 (LSD1). It is highly selective over related enzymes such as MAO-A/B. A proliferation screen of cell lines representing a number of tumor types indicated that small cell lung carcinoma (SCLC) is sensitive to GSK2879552’s inhibition. It increases H3K4 methylation selectively at genomic regions bound by LSD1. It demonstrates efficacy in preclinical models of SCLC. Currently GSK2879552 is in phase I clinical trials targeting Acute Myeloid Leukemia (AML) and Relapsed/Refractory Small Cell Lung Carcinoma. 

    How to Use:

    In vitro: GSK2879552 was used at 1 µM in vitro and cellular assays.
    In vivo: GSK2879552 was orally dosed to mice at 1.5-10 mg/Kg once per day.

    Reference:

    • 1. Mohammad HP, et al. A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC. (2015) Cancer Cell. 28(1):57-69. 
    • 2. Maes T, et al. KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease. (2015) Epigenomics. 7(4):609-26.

           
     

    Products are for research use only. Not for human use.

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