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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 MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

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500580
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₃₁H₃₈N₆O₂

Pricing & Availability

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      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
      Catalogue Number GTIN
      5.00580.0001 04055977244960

      Documentation

      Ezh2 Inhibitor III, GSK126 SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      McCabe, M.T., et al. 2012. Nature. 492, 108.
      Data Sheet

      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.