GSK503,1346572-63-1

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GSK503

CAS No. : 1346572-63-1

MCE 国际站：GSK503

产品活性：GSK503是高效特异性的EZH2甲基转移酶抑制剂，K_i^app值为3到27 nM。

研究领域：Epigenetics

作用靶点：Histone Methyltransferase

In Vitro: GSK503 inhibits the methyltransferase activity of wild type and mutant EZH2 with similar potency (K_i^app=3-27 nM) and is structurally related to GSK126 and GSK343. GSK503 is >200 fold selective over EZH1 (K_i^app=636 nM) and >4000 fold selective over other histone methyltransferases.

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. 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.

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