260921 | DNA Methyltransferase Inhibitor II, SGI-1027 - Calbiochem

260921
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₇H₂₃N₇O

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.