260921 DNA Methyltransferase Inhibitor II, SGI-1027 - Calbiochem

260921
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₇H₂₃N₇O

Pricing & Availability

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260921-10MG
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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable quinoline compound that is shown to inhibit human DNMT1 (IC50 = 6 and 12.5 µM, respectively, with Hemimethylated DNA or Poly(dI-dC) as the substrate), murine DNMT3a & 3b (IC50 = 8 and 7.5 µM, respectively, with Poly(dI-dC) as the substrate), as well as CpG DNA methylase M.SssI (IC50 = 13.5 and 16 µM, respectively, with Poly(dI-dC) as the substrate and 75 or 150 nM AdoMet) of mycoplasma Spiroplasma sp. strain MQ1, presumably by competing with AdoMet (S-adenosyl-L-methionine , SAM) for the enzyme's cofactor binding site. Shown to be 2-, 3-, and 5-fold more effective than Decitabine (Cat. No. 189825), respectively, in reactivating p16 mRNA (2.5 µM for 7 days), MLH1 mRNA (2.5 µM for 7 days), and p16 protein expression (1.0 or 2.5 µM for 12 days) in human colon carcinoma RKO cultures by reducing CpG island hypermethylation found in the promoter regions of TSGs (tumor suppressor genes) without inducing genome-wide hypomethylation or caspase-3 activation.
      Catalogue Number260921
      Brand Family Calbiochem®
      SynonymsN-(4-(2-Amino-6-methylpyrimidin-4-ylamino)phenyl)-4-(quinolin-4-ylamino)-benzamide, S-1027, DNA MTase Inhibitor II
      References
      ReferencesDatta, J., et al. 2009. Cancer Res. 69, 4277.
      Product Information
      FormPale yellow powder
      Hill FormulaC₂₇H₂₃N₇O
      Chemical formulaC₂₇H₂₃N₇O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥88% 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 reconstiution, 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

      DNA Methyltransferase Inhibitor II, SGI-1027 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      DNA Methyltransferase Inhibitor II, SGI-1027 - Calbiochem Certificates of Analysis

      TitleLot Number
      260921

      References

      Reference overview
      Datta, J., et al. 2009. Cancer Res. 69, 4277.

      Technical Info

      Title
      White Paper - The Message in the Marks: Deciphering Cancer Epigenetics (EMD)
      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.

      Revision28-February-2011 RFH
      SynonymsN-(4-(2-Amino-6-methylpyrimidin-4-ylamino)phenyl)-4-(quinolin-4-ylamino)-benzamide, S-1027, DNA MTase Inhibitor II
      DescriptionA cell-permeable quinoline compound that is shown to inhibit human DNMT1 (IC50 = 6 and 12.5 µM, respectively, with Hemimethylated DNA or Poly(dI-dC) as the substrate), murine DNMT3a & 3b (IC50 = 8 and 7.5 µM, respectively, with Poly(dI-dC) as the substrate), as well as CpG DNA methylase M.SssI (IC50 = 13.5 and 16 µM, respectively, with Poly(dI-dC) as the substrate and 75 or 150 nM AdoMet) of mycoplasma Spiroplasma sp. strain MQ1, presumably by competing with AdoMet (S-adenosyl-L-methionine , SAM) for the enzyme's cofactor binding site. Shown to be 2-, 3-, and 5-fold more effective than Decitabine (Cat. No. 189825), respectively, in reactivating p16 mRNA (2.5 µM for 7 days), MLH1 mRNA (2.5 µM for 7 days), and p16 protein expression (1.0 or 2.5 µM for 12 days) in human colon carcinoma RKO cultures by reducing CpG island hypermethylation found in the promoter regions of TSGs (tumor suppressor genes) without inducing genome-wide hypomethylation or caspase-3 activation.
      FormPale yellow powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₇H₂₃N₇O
      Structure formulaStructure formula
      Purity≥88% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage -20°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstiution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesDatta, J., et al. 2009. Cancer Res. 69, 4277.