505052 Ezh2/Ezh1 Inhibitor, UNC1999 - Calbiochem

505052
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₃₃H₄₃N₇O₂

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      Glass bottle 5 mg
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      Description
      OverviewA cell-permeable GSK126 structural analog that acts as a potent, SAM-, but not substrate-, competitive inhibitor against Ezh1 and Ezh2 (IC50 = 5 and 45 nM against PRC2 complex containing Ezh2 or Ezh1 in H3 peptide methylation assays; [SAM] = 5 µM), while exhibiting much reduced or little potency toward panels of 15 other methyltransferases, 50 kinases, as well as 43 GPCRs, transporters, and ion channels, although high affinity binding is observed with Sigma-2 receptor S2R/PGRMC1 (Ki = 65 nM) with unknown impact toward its function. Cellular H3K27me3 level is shown to be largely reduced in MCF10A, MCF7, and DB cells with no significant effect on proliferation upon a 3-day UNC1999 treatment (ICmax = 3 to 5 µM), while complete cell death is reported in the EZH2 Y641N-harboring DB cell line upon an 8-day 5 µM drug exposure. Both its oral bioavailability in mice and enhanced Ezh1 potency can greatly complement the Ezh2-selective GSK126 in in vitro and in vivo studies.
      Catalogue Number505052
      Brand Family Calbiochem®
      SynonymsEnhancer of Zested Homolog 1 Inhibitor, 1-Isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1H-indazole-4-carboxamide, Ezh1 Inhibitor, Ezh2 Inhibitor IV, HMTase Inhibitor XII, Histone Lysine Methyltransferase XII, Enhancer of Zested Homolog 2 Inhibitor IV
      References
      ReferencesKonze, K.D., et al. 2013. ACS Chem. Biol. 8, 1324.
      Product Information
      FormWhite powder
      Hill FormulaC₃₃H₄₃N₇O₂
      Chemical formulaC₃₃H₄₃N₇O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetEzh2
      Secondary targetEzh1
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      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 +2°C to +8°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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Ezh2/Ezh1 Inhibitor, UNC1999 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Konze, K.D., et al. 2013. ACS Chem. Biol. 8, 1324.
      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.

      Revision18-December-2013 JSW
      SynonymsEnhancer of Zested Homolog 1 Inhibitor, 1-Isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1H-indazole-4-carboxamide, Ezh1 Inhibitor, Ezh2 Inhibitor IV, HMTase Inhibitor XII, Histone Lysine Methyltransferase XII, Enhancer of Zested Homolog 2 Inhibitor IV
      DescriptionA cell-permeable GSK126 structural analog that acts as a potent, SAM-, but not substrate-, competitive inhibitor against Ezh1 and Ezh2 (IC50 = 5, 20, 20, 45 nM against PRC2 complex containing Ezh2 wt, Ezh2 Y641F, Ezh2 Y641N, or wt Ezh1 in H3 peptide methylation assays; [SAM] = 5 µM), while exhibiting much reduced or little potency toward panels of 15 other methyltransferases (IC50 >10 µM), 50 kinases (≤20% inhibition at 10µM), as well as 43 GPCRs, transporters, and ion channels, although high affinity binding is observed with Sigma-2 receptor S2R/PGRMC1 (Ki = 65 nM) with unknown impact toward its function. Cellular H3K27me3 level is shown to be largely reduced in MCF10A, MCF7, and DB cells with no significant effect on proliferation upon a 3-day UNC1999 treatment (ICmax = 3 to 5 µM), while complete cell death is reported in the EZH2 Y641N-harboring DLBCL line DB cell culture upon an 8-day 5 µM drug exposure. Exhibits good bioavailability in mice with the plasma drug concentration maintained above 100 nM for 20 h and 24 h, respectively, following a single 50 mg/kg oral or i.p. dosage (Cmax = 4.7 and >9.7 µM, respectively). Both its oral bioavailability and enhanced Ezh1 potency can greatly complement the Ezh2-selective GSK126 in in vitro and in vivo studies.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₃₃H₄₃N₇O₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesKonze, K.D., et al. 2013. ACS Chem. Biol. 8, 1324.