货号	规格	价格	上海	北京	珠海	南京	武汉
S81293-1mg	≥99%	￥224.00 S81293-1mg ￥224.00 现货	5 5	-	-	-	-
S81293-2mg	≥99%	￥340.00 S81293-2mg ￥340.00 现货	5 5	-	-	-	-
S81293-5mg	≥99%	￥380.00 S81293-5mg ￥380.00 现货	5 5	-	-	-	-
S81293-10mg	≥99%	￥660.00 S81293-10mg ￥660.00 现货	5 5	-	-	-	-
S81293-25mg	≥99%	￥1120.00 S81293-25mg ￥1120.00 现货	4 4	-	-	-	-
S81293-50mg	≥99%	￥1900.00 S81293-50mg ￥1900.00 2-3天	0 货期：2-3天	-	-	-	-
S81293-100mg	≥99%	￥3200.00 S81293-100mg ￥3200.00 2-3天	0 货期：2-3天	-	-	-	-

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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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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