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500580 Ezh2 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).

Ezh2 Inhibitor III, GSK126 : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 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

500580
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Aperçu

Replacement Information

Tableau de caractéristiques principal

Empirical Formula
C₃₁H₃₈N₆O₂

Products

RéférenceConditionnement Qté
5005800001 Flacon en verre 5 mg
Description
OverviewA 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 Number500580
Brand Family Calbiochem®
SynonymsEnhancer 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
ReferencesMcCabe, M.T., et al. 2012. Nature. 492, 108.
Product Information
FormBrown semi-solid
Hill FormulaC₃₁H₃₈N₆O₂
Chemical formulaC₃₁H₃₈N₆O₂
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Référence GTIN
5005800001 04055977244960

Documentation

Ezh2 Inhibitor III, GSK126 FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

Références bibliographiques

Aperçu de la référence bibliographique
McCabe, M.T., et al. 2012. Nature. 492, 108.
Fiche technique

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.

Revision24-April-2015 JSW
SynonymsEnhancer 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
DescriptionA 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, A677G, Y641F, Y641H, Y641N, Y641S, Y641C 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 receptors, JMJD2d, and CaMK1a are significantly inhibited at much higher concentrations (IC50 = 4, 7.9, and ≥10 µM, respectively). In addition to DLBCL (diffuse large B cell lymphoma; IC50 ranges from 28 nM to 5.5 µM; 6 d treatment), GSK126 is also shown to inhibit the proliferation of other B-NHL (non-Hodgkin's lymphoma) and Hodgkin's lymphoma cell lines, being least active against MC116, HD-MY-Z, WSU-FSCCL, Toledo, NU-DUL-1, and WILL-2 (IC50 >10 µM; 6 d treatment). When administered at a daily i.p. dose of 50 mg/kg GSK126 is reported to completely suppress Pfeiffer (A677G) and Karpas-422 (Y641N) tumor expansion in mice in vivo, while complete tumor eradication can be achieved with higher dosing regimens (150 mg/kg/day or two 300 mg/kg dosages per week).
FormBrown semi-solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₃₁H₃₈N₆O₂
Purity≥98% by HPLC
SolubilityDMSO (10 mg/ml). Use only fresh DMSO for reconstitution.
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesMcCabe, M.T., et al. 2012. Nature. 492, 108.