Catalog No.S7276 Synonyms: DNA Methyltransferase Inhibitor II
Molecular Weight(MW): 461.52
SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B in cell-free assays, respectively.
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Following the incubation of the unmethylated DNA probe with DNMTase in the presence of spotted DNMTIs, Cy5 intensity values were measured before ( I0 ) and after ( I30 ) of endonuclease cleavage. Each data set was normalized to the initial fluorescence signal within the corresponding block and the resulting ratio describes the net CpG sites remained uncleaved (盨.D., n = 64). The red line represents the inhibitory threshold determined as two standard deviations below the averaged 'unspotted' ratio. On-chip visualization of the corresponding remaining Cy5 signal is placed on the bottom of each column.
Lab Chip 2014 14(13), 2354-62. SGI-1027 purchased from Selleck.
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Choose Selective DNA Methyltransferase Inhibitors
|Description||SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B in cell-free assays, respectively.|
|Features||Potential for use in epigenetic cancer therapy.|
SGI-1027 inhibits DNA methylation by directly inhibiting DNMTs, and results in selective degradation of DNMT1 in a wide variety of human cancer cell lines. SGI-1027 exhibits minimal or no cytotoxic effect in rat hepatoma H4IIE cells.  SGI-1027 (0-100 μM) exhibits a moderate pro-apoptotic effect on U937 human leukemia cell line with no relevant changes on the cell cycle. 
DNA methyltransferase (CpG methyltransferase) assay:DNA methylase activity is assayed by measuring the incorporation of 3H1-methyl group from Ado-Met into DNA using DE-81 ion exchange filter binding assay with some modifications. Human recombinant DNMT1, recombinant mouse Dnmt3a/ Dnmt3b (500 ng) is incubated with 500 ng of poly(dI-dC) or hemimethylated DNA duplex and 75 or 150 nM (0.275μCi or 0.55μCi) of [methyl-3H]-Sadenosylmethionine (Ado-Met) in a total volume of 50 μl at 37°C for 1hr. or M. Sss I is assayed in the supplier’s buffer. SGI-1027 or decitabine is added at indicated concentrations. Each reaction is performed in duplicate and included controls with no inhibitor or no DNA. The reaction is stopped by soaking reaction mixture onto a Whatman DE-81 ion exchange filter disc, washed (five times, 10 min each, with 0.5M Na-phosphate buffer; pH 7.0) dried and counted in a scintillation counter. The background radioactivity (no DNA control) is subtracted from the values obtained with reaction mixtures containing DNA and the radioactivity obtained in the reaction without any inhibitor is considered as 100% activity. IC50 is determined by interpolation from the plot of percent activity versus inhibitor concentration. To determine the nature of inhibition of DNMTase activity by SGI-1027, DNMT1 enzyme activityis measured in presence of a fixed concentration of inhibitor (0, 2.5, 5, and 10μM) while one of the two (Ado-Met or DNA) was varied in a particular reaction mixture. At a fixed concentration of DNA (500 ng) varying concentrations of Ado-Met used are from 25-500 nM, respectively. Similarly, final DNA concentrations are varied from (25-500ng) at 75 nM Ado-Met.
|In vitro||DMSO||92 mg/mL (199.34 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||DNA Methyltransferase Inhibitor II|
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