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260921 DNA Methyltransferase Inhibitor II, SGI-1027 - Calbiochem

260921
Purchase on Sigma-Aldrich

Descripción

Replacement Information

Tabla espec. clave

Empirical Formula
C₂₇H₂₃N₇O

Products

Número de referenciaEmbalaje Cant./Env.
260921-10MG Frasco de vidrio 10 mg
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

DNA Methyltransferase Inhibitor II, SGI-1027 - Calbiochem Ficha datos de seguridad (MSDS)

Título

Ficha técnica de seguridad del material (MSDS) 

DNA Methyltransferase Inhibitor II, SGI-1027 - Calbiochem Certificados de análisis

CargoNúmero de lote
260921

Referencias bibliográficas

Visión general referencias
Datta, J., et al. 2009. Cancer Res. 69, 4277.

Licencias necesarias e Información técnica

Cargo
White Paper - The Message in the Marks: Deciphering Cancer Epigenetics
Ficha técnica

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.