GSK126 - Moligand™, in 2mM DMSO , Histone-lysine N-methyltransferase EZH2 inhibitor, CAS No.1346574-57-9, Histone-lysine N-methyltransferase EZH2 inhibitor

CAS: 1346574-57-9 Cat. No.: G408987 Molecular Weight: 526.67

GRADE & PURITY Moligand™, in 2mM DMSO

Synonyms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

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%

Specifications

Synonyms

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

Specifications & Purity

Moligand™, in 2mM DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Histone-lysine N-methyltransferase EZH2 inhibitor

Product Properties

• ALogP: 3.9

Names and Identifiers

• 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
• Molecular Weight: 526.67
• Reaxy-Rn: 21957292
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21957292&ln=

Associated Targets(Human)

EZH2 Tclin Histone-lysine N-methyltransferase EZH2 (14 Activities)

Discover Target: EZH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)