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 Summenformel: C₃₁H₃₈N₆O₂ Molekulargewicht: 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

Übersicht

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

Synonyme

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

Spezifikationen & Reinheit

Moligand™, in 2mM DMSO

Biochemische und physiologische Mechanismen

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

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Histone-lysine N-methyltransferase EZH2 inhibitor

Produkteigenschaften

• ALogP: 3.9

Namen und Kennungen

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

Zugehörige Ziele (menschlich)

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)