500580 Sigma-AldrichEzh2 Inhibitor III, GSK126
A cell-permeable structural analog of E1 that acts as an equipotent, SAM-competitive inhibitor of Ezh2/PRC2 inhibitor (Ki = 0.5 to 3 nM against wt & mutant Ezh2-containing PRC2).
More>> A cell-permeable structural analog of E1 that acts as an equipotent, SAM-competitive inhibitor of Ezh2/PRC2 inhibitor (Ki = 0.5 to 3 nM against wt & mutant Ezh2-containing PRC2). Less<<Ezh2 Inhibitor III, GSK126 MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
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, Enhancer of Zested Homolog 2 Inhibitor III, HMTase Inhibitor XIV
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Overview
Key Spec Table
| Empirical Formula |
|---|
| C₃₁H₃₈N₆O₂ |
Products
| Catalogue Number | Packaging | Qty/Pack | |
|---|---|---|---|
| 5.00580.0001 | Glass bottle | 5 mg |
| Description | |
|---|---|
| Overview | A cell-permeable EI1 (Cat. No. 500561) structural analog that acts as an equally potent, SAM-competitive, Ezh2/PRC2 inhibitor (Ki = 0.5 to 3 nM against wt & mutant Ezh2-containing PRC2; [SAM] = 7.5 µM) with similar selectivity over Ezh1/PRC2 (Ki = 89 nM) and other HTMases as EI1. Among panels of 14 HDACs, 11 GPCRs, and 300 kinases, only serotonin 3 receptor, JMJD2d, and CaMK1a are significantly inhibited at much higher concentrations (IC50 ≥4 µM). Shown to inhibit the proliferation of DLBCL (IC50 28 nM to 5.5 µM; 6 d treatment) in vitro and completely suppress Pfeiffer (A677G) and Karpas-422 (Y641N) tumor expansion in mice in vivo (50 mg/kg/d i.p.). Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water. |
| Catalogue Number | 500580 |
| Brand Family | Calbiochem® |
| 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, Enhancer of Zested Homolog 2 Inhibitor III, HMTase Inhibitor XIV |
| References | |
|---|---|
| References | McCabe, M.T., et al. 2012. Nature. 492, 108. |
| Product Information | |
|---|---|
| Form | Brown semi-solid |
| Hill Formula | C₃₁H₃₈N₆O₂ |
| Chemical formula | C₃₁H₃₈N₆O₂ |
| Quality Level | MQ100 |
| Biological Information | |
|---|---|
| Purity | ≥98% by HPLC |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 5.00580.0001 | 04055977244960 |