GSK126 GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases.
In vitro

In vitro, GSK126 most potently inhibits H3K27me3, followed by H3K27me2 in both EZH2 wild-type and mutant DLBCL cell lines. GSK126 also effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines, and induces transcriptional activation of EZH2 target genes in sensitive cell lines. In A687V EZH2-mutant cells, GSK126 treatment results in a global decrease in H3K27me3, robust gene activation, caspase activation, and decreased proliferation. In parental H2087 cells, GSK126 inhibits the expression of VEGF-A and phosphorylated Ser(473)-AKT, and thus causes the inhibition of cell proliferation, migration and metastasis.

In vivo

In mice bearing KARPAS-422 and Pfeiffer xenografts, GSK126 (150 mg/kg/d, i.p.) decreases global H3K27me3, increases gene expression, and thus causes marked tumour regression.
Cell Data

cell lines：

Concentrations：0~10 μM

Incubation Time：6 days

Powder Purity:≥99%

规格

英文别名

GSK2816126A, GSK2816126 | 1-(S)-sec-butyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide

规格或纯度

Moligand™, 2mM in DMSO

英文名称

GSK126

生化机理

GSK126（GSK2816126A，GSK2816126）是一种强效、高选择性的 EZH2 甲基转移酶抑制剂，IC50 为 9.9 nM，对 EZH2 的选择性大于其他 20 种人类甲基转移酶的 1000 倍。

储存条件

-80℃储存

运输条件

特低温运输

作用类型

抑制剂

作用机制

组蛋白-赖氨酸 N-甲基转移酶 EZH2 抑制剂

名称和识别符

分子类型

小分子

Isomeric SMILES

CC[C@H](C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C

分子量

526.67

Reaxy-Rn

21957292

Reaxys-RN link address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21957292&ln=

高级数据

产品属性

ALogP	3.9

关联靶点（人）

EZH2 Tclin 组蛋白赖氨酸N-甲基转移酶EZH2(Histone-lysine N-methyltransferase EZH2) (14 活性数据)

点击查看靶蛋白信息： EZH2

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

输入批号以搜索分析图谱:

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溶液计算器