GSK126 | 2282

A potent, highly selective, S-adenosyl-methionine(SAM)-competitive, small-molecule inhibitor of EZH2 methyltransferase activity. GSK126 is highly selective against other methyltransferases and multiple other protein classes, even 150-fold more selective for the closest EZH1 (Kiapp = 89 nM) and more than 1,000-fold selective for 20 other human methyltransferases, including both SET-domain-containing and non-SET domain-containing methyltransferases. It decreases global H3K27me3 levels and reactivates silenced polycomb repressive complex 2 (PRC2) target genes.

GSK126 is a potent, highly selective, S-adenosyl-methionine(SAM)-competitive, small-molecule inhibitor of EZH2 methyltransferase activity.

2282 | GSK126 DataSheet

Alternate Name/Synonyms: (S)-1-(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

Appearance: Crystalline solid

Formulation: N/A

CAS Number: 1346574-57-9

Structure Available?: Yes

Peptide sequence: No

Salt Form: No

Molecular Formula: C₃₁H₃₈N₆O₂

Molecular Weight: 526.67

Cell-Permeable?: Yes

Purity: 100% by chiral HPLC & >99% by HPLC

Solubilities: DMSO (~50 mg/ml)

Handling: Protect from light and moisture

Country of Origin: USA

Tag Line: A potent EZH2 inhibitor

MDL Number: N/A

PubChem CID: 68210102

SMILES: CCC(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

InChi: InChI=1S/C31H38N6O2/c1-6-22(5)37-18-20(3)29-25(30(38)34-17-26-19(2)13-21(4)35-31(26)39)14-24(15-27(29)37)23-7-8-28(33-16-23)36-11-9-32-10-12-36/h7-8,13-16,18,22,32H,6,9-12,17H2,1-5H3,(H,34,38)(H,35,39)/t22-/m0/s1

InChi Key: FKSFKBQGSFSOSM-QFIPXVFZSA-N