1. Epigenetics
  2. Histone Demethylase
  3. GSK2879552 dihydrochloride

GSK2879552 dihydrochloride 

Cat. No.: HY-18632A
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GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.

For research use only. We do not sell to patients.

GSK2879552 dihydrochloride Chemical Structure

GSK2879552 dihydrochloride Chemical Structure

CAS No. : 1902123-72-1

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Top Publications Citing Use of Products

    GSK2879552 dihydrochloride purchased from MCE. Usage Cited in: Cancer Chemother Pharmacol. 2019 Feb;83(2):277-287.

    The protein expression of LSD1, PRB and H3K4me2 is detected through Western blot with GSK2879552 treatment in different cells.
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    Description

    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity[1][2].

    In Vitro

    GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 depresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells[1].

    Cell Viability Assay[2].

    Cell Line: 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines.
    Concentration: 0-10000 nM.
    Incubation Time: 6 days.
    Result: Inhibited cell proliferation.

    RT-PCR[1].

    Cell Line: Resistant HCC cells (PLC/PRF/5 and Huh7).
    Concentration: 0, 1, 2 μM.
    Incubation Time: 24 h.
    Result: Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9, Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4.
    In Vivo

    GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice[2].

    Animal Model: NCI-H526 and NCI-H1417 xenografts[2].
    Dosage: 1.5 mg/kg.
    Administration: PO daily for 25-35 days.
    Result: There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.
    Molecular Weight

    437.40

    Formula

    C₂₃H₃₀Cl₂N₂O₂

    CAS No.

    1902123-72-1

    SMILES

    O=C(O)C1=CC=C(CN2CCC(CN[[email protected]]3[[email protected]](C4=CC=CC=C4)C3)CC2)C=C1.[H]Cl.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    Keywords:

    GSK2879552GSK 2879552GSK-2879552Histone DemethylasestemcellSCLCInhibitorinhibitorinhibit

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    Product name:
    GSK2879552 dihydrochloride
    Cat. No.:
    HY-18632A
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