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    GSK-LSD1 2HCl
    GSK-LSD1 2HCl

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0376
    CAS #: 1821798-25-7 (2HCl)Purity ≥98%

    Description: GSK-LSD1 2HCl, the dihydrochloride salt of GSK-LSD1 (GSK-LSD-1), is an irreversible, potent and selective inhibitor of Lysine (K) -specific demethylase 1A (LSD1) with antineoplastic activity. It inhibits LSD1 with an IC50 of 16 nM,  and shows > 1000 fold selectivity for LSD1 over other closely related FAD dependent enzymes such as LSD2, MAO-A, and MAO-B. It displays potent in vitro antiproliferative activity and high in vivo antitumor efficacy. 

    References: Biochim Biophys Acta. 2017 Aug 8;1864(12):2428-2437.; http://www. thesgc.org/chemical-probes/LSD1.

    Related CAS #: 1431368-48-7 (rel-free base)  1821798-25-7 (2HCl)  2102933-95-7 (rel-2HCl)   1431368-50-1 (free base)   1431367-49-5 (rel-HCl)   1431367-51-9 (HCl)       

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    • 香港大学
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    Molecular Weight (MW)289.24
    FormulaC14H22Cl2N2
    CAS No.1431368-48-7(free base)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO:  ≥ 60 mg/mL 
    Water: N/A
    Ethanol: N/A
    SMILESC1(N[[email protected]]2[[email protected]](C3=CC=CC=C3)C2)CCNCC1.Cl.Cl
    Synonyms

    GSK-LSD1 dihydrochloride; GSK-LSD1; GSK-LSD 1; GSK-LSD-1; GSK-LSD1 2HCl; GSK-LSD1 (trans-racemic) dihydrochloride; GSK-LSD1 HCl; rel- N-[(1R,2S)-2-Phenylcyclopropyl]-4-Piperidinamine hydrochloride (1:2)

    InChi Key: PJFZOGMSPBHPNS-WICJZZOFSA-N

    InChi Code: InChI=1S/C14H20N2.2ClH/c1-2-4-11(5-3-1)13-10-14(13)16-12-6-8-15-9-7-12;;/h1-5,12-16H,6-10H2;2*1H/t13-,14+;;/m0../s1

    SMILES Code: [H]Cl.[H]Cl.C1(N[[email protected]]2[[email protected]](C3=CC=CC=C3)C2)CCNCC1 


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: GSK-LSD1 Dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.


    Cell Assay: GSK-LSD1 2HCl irreversibly inhibited LSD1 with IC50 value of 16 nM and is > 1000 fold selective over LSD2, MAO-A and MAO-B, which were related to FAD utilizing enzymes. In cancer cell lines, GSK-LSD1 2HCl changed gene expression with average EC50 value < 5 nM and inhibited cells growth with average EC50 value < 5 nM. GSK-LSD1 2HCl (10 ?M) inhibited human recombinant dopamine transporter, 5-HT1A and 5-HT transporter by 39%, 49% and 74%, respectively. And no activity against other 55 recombinant receptors (GPCR, transporters, ion channels). GSK-LSD1 2HCl can be used as a chemical probe and a part of the SGC epigenetics. 

    In VivoNA
    Animal modelNA
    Formulation & DosageNA
    ReferencesBiochim Biophys Acta. 2017 Aug 8;1864(12):2428-2437.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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