1. Epigenetics
  2. Histone Demethylase
  3. GSK2879552

GSK2879552 

Cat. No.: HY-18632 Purity: 99.94%
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GSK2879552 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 Chemical Structure

GSK2879552 Chemical Structure

CAS No. : 1401966-69-5

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 97 In-stock
Estimated Time of Arrival: December 31
5 mg USD 88 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 850 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of GSK2879552:

Top Publications Citing Use of Products

    GSK2879552 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.
    • Biological Activity

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    • Customer Review

    Description

    GSK2879552 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Proliferation 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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.
    Clinical Trial
    Molecular Weight

    364.48

    Formula

    C₂₃H₂₈N₂O₂

    CAS No.

    1401966-69-5

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (137.18 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7436 mL 13.7182 mL 27.4363 mL
    5 mM 0.5487 mL 2.7436 mL 5.4873 mL
    10 mM 0.2744 mL 1.3718 mL 2.7436 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.75 mg/mL (7.54 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.75 mg/mL (7.54 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.75 mg/mL (7.54 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    GSK2879552GSK 2879552GSK-2879552Histone DemethylaseInhibitorinhibitorinhibit

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