500580 | Ezh2 Inhibitor III, GSK126

500580
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₃₁H₃₈N₆O₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00580.0001
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          Glass bottle 5 mg
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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
          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

          Documentation

          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 -20°C
          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.
          Toxicity Standard Handling
          ReferencesMcCabe, M.T., et al. 2012. Nature. 492, 108.