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: SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.
Synonyme: Enhancer of Zested Homolog 2 Inhibitor III, (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, HMTase Inhibitor XIV
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Übersicht
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Key Spec Table
| Empirical Formula |
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| C₃₁H₃₈N₆O₂ |
Preis & Verfügbarkeit
| Bestellnummer | Verfügbarkeit | Verpackung | St./Pkg. | Preis | Menge | |
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| 5.00580.0001 |
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Glasflasche | 5 mg |
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| Description | |
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| 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 | Enhancer of Zested Homolog 2 Inhibitor III, (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, HMTase Inhibitor XIV |
| References | |
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| References | McCabe, M.T., et al. 2012. Nature. 492, 108. |
| Product Information | |
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| Form | Brown semi-solid |
| Hill Formula | C₃₁H₃₈N₆O₂ |
| Chemical formula | C₃₁H₃₈N₆O₂ |
| Quality Level | MQ100 |
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| Biological Information | |
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| Purity | ≥98% by HPLC |
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| Safety Information according to GHS |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| Bestellnummer | GTIN |
| 5.00580.0001 | 04055977244960 |
Documentation
Ezh2 Inhibitor III, GSK126 SDB
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Literatur
| Übersicht |
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| McCabe, M.T., et al. 2012. Nature. 492, 108. |
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Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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