2. Epigenetics
  3. Histone Demethylase
  4. GSK2879552

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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 96 In-stock
Solution
10 mM * 1 mL in DMSO USD 96 In-stock
Solid
1 mg USD 41 In-stock
5 mg USD 88 In-stock
10 mg USD 140 In-stock
25 mg USD 270 In-stock
50 mg USD 450 In-stock
100 mg USD 850 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of GSK2879552:

GSK2879552 Related Antibodies

Top Publications Citing Use of Products

    GSK2879552 purchased from MedChemExpress. Usage Cited in: Cancer Chemother Pharmacol. 2019 Feb;83(2):277-287.  [Abstract]

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

    View All Histone Demethylase Isoform Specific Products:

    View All Isoforms
    KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    KDM1/LSD1

     

    In Vitro

    GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of Sorafenib (HY-10201)-resistant cells and attenuating stemness properties. GSK2879552 depresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in Sorafenib-resistant cells[1].

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

    GSK2879552 Related Antibodies

    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].

    MedChemExpress (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.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)C1=CC=C(CN2CCC(CN[C@H]3[C@H](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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (68.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    C2

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    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.75%

    COA (244 KB) HNMR (281 KB) LCMS (97 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7436 mL 13.7182 mL 27.4363 mL 68.5909 mL
    5 mM 0.5487 mL 2.7436 mL 5.4873 mL 13.7182 mL
    10 mM 0.2744 mL 1.3718 mL 2.7436 mL 6.8591 mL
    15 mM 0.1829 mL 0.9145 mL 1.8291 mL 4.5727 mL
    20 mM 0.1372 mL 0.6859 mL 1.3718 mL 3.4295 mL
    25 mM 0.1097 mL 0.5487 mL 1.0975 mL 2.7436 mL
    30 mM 0.0915 mL 0.4573 mL 0.9145 mL 2.2864 mL
    40 mM 0.0686 mL 0.3430 mL 0.6859 mL 1.7148 mL
    50 mM 0.0549 mL 0.2744 mL 0.5487 mL 1.3718 mL
    60 mM 0.0457 mL 0.2286 mL 0.4573 mL 1.1432 mL
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    GSK2879552 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    GSK28795521401966-69-5GSK 2879552GSK-2879552Histone DemethylaseInhibitorinhibitorinhibit

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