GSK126 (GSK-126, GSK 126)是一种有效的、高选择性、S腺苷甲硫氨酸（S-adenosyl-methionine）竞争性的EZH2甲基转移酶抑制剂（Ki = 0.57 nM，IC₅₀ = 9.9 nM）。GSK126有效降低H3K27me3水平，并再次激活沉默的PRC2靶标基因。而且，GSK126有效抑制EZH2突变型DLBCL细胞系的增殖，显著抑制移植瘤小鼠中EZH2突变型DLBCL细胞系生长。GSK126通过下调VEGF-A表达，从而抑制肿瘤细胞迁移，并抑制血管生成。GSK126与5-aza-dC联合使用时，表现出更强的抑制体内肿瘤生长的作用。

参考文献

[1] McCabe MT, et al.EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature 492(7427): 108-112 (2012).

[2] Ott HM, et al. A687V EZH2 Is a Driver of Histone H3 Lysine 27 (H3K27) Hypertrimethylation. Mol Cancer Ther. 13(12): 3062-3073 (2014).

[3] Takeshima H, et al. Identification of coexistence of DNA methylation and H3K27me3 specifically in cancer cells as a promising target for epigenetic therapy. Carcinogenesis. 36(2): 192-201 (2015).

[4] Chen YT, et al. The novel EZH2 inhibitor, GSK126, suppresses cell migration and angiogenesis via down-regulating VEGF-A. Cancer Chemotherapy and Pharmacology 77(4): 757-765 (2016).

粉末直接保存于-20 ºC，有效期2年。溶于DMSO。建议分装后-20ºC避光保存，避免反复冻存，至少可存放6个月。