1. Epigenetics
  2. Histone Methyltransferase
  3. GSK503

GSK503 

Cat. No.: HY-12856 Purity: 98.99%
Handling Instructions

GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.

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

GSK503 Chemical Structure

GSK503 Chemical Structure

CAS No. : 1346572-63-1

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 125 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 156 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 960 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK503 purchased from MCE. Usage Cited in: Oncotarget. 2017 Apr 25;8(35):58654-58667.

    Treatment of RCC cells with an EZH2 inhibitor (GSK503) upregulates modulators of the Hippo pathway and SAV1 expression at the mRNA and protein levels.
    • Biological Activity

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    • References

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    Description

    GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.

    IC50 & Target

    Ki: 3 to 27 nM (EZH2)[1]

    In Vitro

    GSK503 inhibits the methyltransferase activity of wild type and mutant EZH2 with similar potency (Kiapp=3-27 nM) and is structurally related to GSK126 and GSK343. GSK503 is >200 fold selective over EZH1 (Kiapp=636 nM) and >4000 fold selective over other histone methyltransferases[1].

    In Vivo

    In a melanoma mouse model, conditional EZH2 ablation as much as treatment with the GSK503 stabilizes the disease through inhibition of growth and virtually abolishes metastases formation without affecting normal melanocyte biology[2]. GSK503 displays favorable pharmacokinetics in mice. GSK503, but not vehicle, prevents the formation of germinal center after SRBC or NP-KLH immunization, phenocopying the Ezh2 null phenotype. GSK503 treatment leads to reduced numbers of GC B-cells by flow cytometry, reduces number and volume of GCs by immunohistochemistry, and impairs formation high affinity antibodies[1].

    Molecular Weight

    526.67

    Formula

    C₃₁H₃₈N₆O₂

    CAS No.

    1346572-63-1

    SMILES

    O=C(C1=CC(C2=CC=C(N3CCN(C)CC3)N=C2)=CC4=C1C(C)=CN4C(C)C)NCC5=C(C)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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 44 mg/mL (83.54 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8987 mL 9.4936 mL 18.9872 mL
    5 mM 0.3797 mL 1.8987 mL 3.7974 mL
    10 mM 0.1899 mL 0.9494 mL 1.8987 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: ≥ 2.5 mg/mL (4.75 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [2]

    Mice: To pharmacologically inhibit Ezh2 activity, Tyr::N-RasQ61K Ink4a-/- and C57Bl/6 mice are subjected to treatment with GSK503, which is diluted (15 mg/mL) in 20% Captisol solution. Efficient Ezh2 inhibition is achieved by daily intraperitoneal injections of 150 mg/kg GSK503 over 35 consecutive days. Mice are monitored during and after treatment to measure GSK503-induced reversible weight loss. C57Bl/6 and Foxn1nu/nu mice engrafted with melanoma cells are subjected to TM and GSK503 treatment as described above[2].

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

    References
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    Keywords:

    GSK503GSK 503GSK-503Histone MethyltransferaseInhibitorinhibitorinhibit

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    Product Name:
    GSK503
    Cat. No.:
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