1. Epigenetics
  2. Epigenetic Reader Domain
    Histone Methyltransferase

GSK503 

Cat. No.: HY-12856 Purity: 99.29%
Data Sheet SDS 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 $104 In-stock
5 mg $90 In-stock
10 mg $130 In-stock
50 mg $450 In-stock
100 mg $800 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Animal Administration
[2]

Mouse: 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
Molecular Weight

526.67

Formula

C₃₁H₃₈N₆O₂

CAS No.

1346572-63-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 44 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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GSK503
Cat. No.:
HY-12856
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