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S81293

GSK503

MedMol 99%
  • 英文名:
  • GSK503
  • 别名:
  • CAS号:
  • 1346572-63-1
  • 分子式:
  • C31H38N6O2
  • 分子量:
  • 526.6724
  • 核磁/质谱:
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MedMol S81293-1mg 99% ¥224.40元 5 - - - EA 加入购物车
MedMol S81293-2mg 99% ¥340.00元 5 - - - EA 加入购物车
MedMol S81293-5mg 99% ¥544.00元 5 - - - EA 加入购物车
MedMol S81293-10mg 99% ¥816.00元 5 - - - EA 加入购物车
MedMol S81293-25mg 99% ¥1904.00元 4 - - - EA 加入购物车
源叶(MedMol) S81293-50mg 99% ¥2720.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S81293-100mg 99% ¥4420.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.
  • 靶点: EZH2;HistoneMethyltransferase
  • 体外研究:
    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
  • 体内研究:
    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
  • 参考文献:
    1. Béguelin W, et al. EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation. Cancer Cell. 2013 May 13;23(5):677-92. 2. Zingg D, et al. The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors. Nat Commun. 2015 Jan 22;6:6051.
  • 溶解性: soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.899 ml 9.494 ml 18.987 ml
    5 mM 0.38 ml 1.899 ml 3.797 ml
    10 mM 0.19 ml 0.949 ml 1.899 ml
    50 mM 0.038 ml 0.19 ml 0.38 ml
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