2. Epigenetics Autophagy
  3. Histone Methyltransferase Autophagy
  4. GSK343

GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.

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

GSK343 Chemical Structure

GSK343 Chemical Structure

CAS No. : 1346704-33-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 79 In-stock
Solution
10 mM * 1 mL in DMSO USD 79 In-stock
Solid
1 mg USD 31 In-stock
5 mg USD 66 In-stock
10 mg USD 106 In-stock
25 mg USD 218 In-stock
50 mg USD 370 In-stock
100 mg USD 647 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 29 publication(s) in Google Scholar

GSK343 Related Antibodies

Top Publications Citing Use of Products

    GSK343 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Mar 27.  [Abstract]

    GSK343 (1, 2.5, 5, 10 μM; 72 h) reduces the level of H3K27me3 in wild-type and CXCdel+/− Karpas-422 cells.

    GSK343 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2023 Apr 10;119:110155.  [Abstract]

    GSK343 (2.5 mg/kg; i.p.; 32 weeks) reduces extensive IgG deposition in the kidneys of lupus mice.(once every other day for the first 16 weeks, then twice a week for 8 weeks, and finally once a week for 8 weeks)

    GSK343 purchased from MedChemExpress. Usage Cited in: Theranostics. 2019 Jan 24;9(3):761-777.  [Abstract]

    Immunoblot analysis of the indicated proteins in lysates from cells as in G with α-Tubulin as loading control with or without the treatment of GSK343.

    GSK343 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2018 Jul;16(1):1231-1236.  [Abstract]

    EZH2 protein expression in T24 cells treated with methyl jasmonate alone or in combination with GSK343 is analyzed using western blot analysis.

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.

    IC50 & Target

    EZH2

     

    In Vitro

    GSK343, which contains an n-propyl group at the 4-position of the pyridone, has EZH2 Kiapp=1.2±0.2 nM. In this 6-day proliferation assay, among the cell lines evaluated in this study, the prostate cancer cell line LNCaP is the most sensitive to EZH2 inhibition, with growth IC50 value of 2.9 μM for GSK343[1]. GSK343 is found to have half maximal inhibitory concentration values of 13 μM in HeLa cells and 15 μM in SiHa cells[2].

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

    GSK343 Related Antibodies
    In Vivo

    Compare with the controls, GSK343 (5 mg/kg)-treated mice exhibits significantly inhibited tumor growth. The average tumor volume and weight of the GSK343-treated cohort is remarkably reduced. As early as 20 days post-implantation, a significant reduction in tumor growth is observed in the GSK343-treated cohort relative to the control cohort; this difference persisted through the remainder of the study. In addition, compare with the control cohort, the GSK343-treated animals in the xenograft model show a remarkable increase in messenger RNA levels of E-cadherin but a significant decrease in vimentin messenger RNA levels[2].

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

    541.69

    Formula

    C31H39N7O2
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(C1=CC(C2=CC(N3CCN(C)CC3)=NC=C2)=CC4=C1C=NN4C(C)C)NCC5=C(CCC)C=C(C)NC5=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 15.62 mg/mL (28.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8461 mL 9.2304 mL 18.4607 mL
    5 mM 0.3692 mL 1.8461 mL 3.6921 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    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: ≥ 1.56 mg/mL (2.88 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.56 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.6 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: ≥ 1.56 mg/mL (2.88 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.56 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.6 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: 99.88%

    COA (255 KB) LCMS (266 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Activity against EZH2 is assessed using 5 member PRC2 complex (Flag-EZH2, EED, SUZ12, AEBP2, RbAp48). The assay protocol may be summarized as follows: 10 mM stocks of GSK343 are prepared from solid in 100% DMSO. An 11 point serial dilution master plate is prepared in 384 well format (1:3 dilution, columns 6 and 18 are equal volume DMSO controls) and dispensed to assay ready plates using acoustic dispensing technology to create a 100 nL stamp of GSK343 and DMSO controls. The assay additions consisted of equal volume additions of 10 nM EZH2 and the substrate solution (5 μg/mL HeLa nucleosomes and 0.25 μM [3H]-SAM) dispensed into assay plates using a multi-drop combi dispense. Reaction plates are incubated for 1 hr and quenched with an equal volume addition of 0.5 mg/mL PS-PEI Imaging Beads (RPNQ0098) containing 0.1 mM unlabeled SAM. The plates are sealed, dark adapted for 30 minutes, and a 5 minute endpoint luminescence image is acquired using a Viewlux imager. Plate statistics such as Z’ and signal to background as well as dose response curves are analyzed using ActivityBaseXE. The in vitro biochemical activity of EZH1 is assessed as part of a 5 member PRC2 complex using a 384 well SPA assay identical to EZH2. Buffer components, reagent dispensing, GSK343 plate preparation, quench conditions and data analysis are identical for EZH1 and EZH2 with final assay concentrations of 20 nM EZH1, 5 μg/mL HeLa nucleosomes and 0.25 μM [3H]-SAM. Further data analysis, pIC50 pivots and visualizations are enabled by TIBCO Spotfire[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    To account for varying doubling rates among cancer cell lines, the optimal cell seeding is determined empirically for all cell lines by examining their growth in a 384-well plate over 6 days with a wide range of seeding densities. Cells are then plated at the optimal seeding density and allowed to adhere overnight. Cells are treated in duplicate with a 20-point 2-fold dilution series of GSK343 or 0.147% DMSO (vehicle control) and incubated for 6 days at 37°C in 5% CO2. Cells are then lysed with 25 μL CellTiter-Glo per well and chemiluminescence is quantified with a TECAN Safire2 microplate reader. In addition, an untreated plate of cells is harvested at the time of GSK343 addition (T0) to quantify the starting number of cells. CTG values after 6 days of treatment are expressed as a percent of the T0 value and plotted against GSK343 concentration. Data are fit with a 4-parameter equation to generate a concentration response curve and the concentration of GSK343 required to inhibit 50% of growth (gIC50) is determined[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    Six-week-old female nude BALB/c mice are used. To study the effect of the EZH2 inhibitor GSK343, 5 mg/kg in 100-μL phosphate-buffered saline is injected intraperitoneally every other day into BALB/c nude mice (n=6) after the tumor volume reaches 100 mm3. In this analysis, the negative control group (n=6) received saline. After 40 days, the mice are killed, and the subcutaneous tumors are surgically excised, weighed, photographed, sectioned, and fixed in 10% formalin. The expression levels of E-cadherin, N-cadherin, and vimentin in the tumours are measured by real-time reverse transcription polymerase chain reaction.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8461 mL 9.2304 mL 18.4607 mL 46.1519 mL
    5 mM 0.3692 mL 1.8461 mL 3.6921 mL 9.2304 mL
    10 mM 0.1846 mL 0.9230 mL 1.8461 mL 4.6152 mL
    15 mM 0.1231 mL 0.6154 mL 1.2307 mL 3.0768 mL
    20 mM 0.0923 mL 0.4615 mL 0.9230 mL 2.3076 mL
    25 mM 0.0738 mL 0.3692 mL 0.7384 mL 1.8461 mL
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    GSK343 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:

    GSK3431346704-33-3GSK 343GSK-343Histone MethyltransferaseAutophagyInhibitorinhibitorinhibit

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