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GSK126

(CAS No:1346574-57-9)

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

CAS No:1346574-57-9

Molecular Weight(MW):526.67

Purity:99.00%

Specification:500MG;1G;5G;10G;50G;100G

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QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	1346574-57-9
Molecular formula(MF)	C₃₁H₃₈N₆O₂
Molecular Weight(MW):	526.67
Alias

Solubility

In vitro	DMSO	3 mg/mL warmed (5.69 mM)
	Water	<1 mg/mL
	Ethanol	<1 mg/mL warmed
In vivo	4% DMSO+corn oil	0.5mg/mL

Biological Activity

Description

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

Targets

EZH2 ^[1]

9.9 nM

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. ^[1] In A687V EZH2-mutant cells, GSK126 treatment results in a global decrease in H3K27me3, robust gene activation, caspase activation, and decreased proliferation. ^[2] 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. ^[3]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
human Pfeiffer cells	CytotoxicÂ assay	72 h	Cytotoxicity against human Pfeiffer cells expressing EZH2 A667G mutant assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=0.18 Î¼M.	24767850
human HeLa cells	Function assay	72 h	Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method, IC50=0.28 Î¼M.	26189078
human U2932 cells	CytotoxicÂ assay	72 h	Cytotoxicity against human U2932 cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=6.7 Î¼M.	24767850
human PC3 cells	CytotoxicÂ assay	72 h	Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=9.4 Î¼M.	24767850
human Daudi cells	CytotoxicÂ assay	72 h	Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=11.2 Î¼M.	24767850
human T98G cells	CytotoxicÂ assay	72 h	Cytotoxicity against human T98G cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=12.6 Î¼M.	24767850
human A549 cells	CytotoxicÂ assay	72 h	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=18.7 Î¼M.	24767850
human U87MG cells	CytotoxicÂ assay	72 h	Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by WST-1 assay, GI50=28.5 Î¼M.	24767850

... Click to View More Cell Line Experimental Data

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. ^[1]