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GSK503

  Cat. No.:  DC8044   Featured
Chemical Structure
1346572-63-1
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More than 5000 active chemicals with high quality for research!
Field of application
GSK503 is a specific EZH2 methyltransferase inhibitor.
Cas No.: 1346572-63-1
Chemical Name: GSK-503，GSK 503
Synonyms: GSK-503，GSK 503
SMILES: N(C(C)C)1C2=C(C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C3=CC=C(N4CCN(C)CC4)N=C3)=C2)C(C)=C1
Formula: C31H38N6O2
M.Wt: 526.3
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.
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].
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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