SGI-1027

Catalog No.S7276 Synonyms: DNA Methyltransferase Inhibitor II

SGI-1027 Chemical Structure

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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1 Customer Review

  • 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.

Purity & Quality Control

Choose Selective DNA Methyltransferase Inhibitors

Biological Activity

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.
Targets
DNMT1 [1]
(Cell-free assay)
DNMT3B [1]
(Cell-free assay)
DNMT3A [1]
(Cell-free assay)
6 μM 7.5 μM 8 μM
In vitro

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. [1] 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. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human U937 cells NF\nU2xEgXSxdH;4bYNqfHliYYPzZZk> NVHLWpN4PDhiaB?= MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVPVM4KGOnbHzzJIFnfGW{IES4JIhzeyCkeTD0dplx[W5iYnz1[UBmgGOudYPpc44h[XO|YYmsJGlEPTB;MT63JO69VQ>? MVGyOFM5PzF3OR?=
human KARPAS299 cells NIfuRmZRem:uaX\ldoF1cW:wIHHzd4F6 NYnke3M6Oi12IHThfZM> NH7ndJRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjZoTldkAzKHSxIESg[IF6eyCkeTDBWHBtcXSnIEHzeIVxKGy3bXnu[ZNk\W6lZTDhd5NigSxiRVO1NF0yNjhizszN MViyOlIzODVzOR?=
human KG1 cells NIHXVldRem:uaX\ldoF1cW:wIHHzd4F6 MV6yMVQh\GG7cx?= MlLDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNR{GgZ4VtdHNiYX\0[ZIhOiC2bzC0JIRigXNiYomgRXRRdGm2ZTCxd5RmeCCudX3pcoV{[2WwY3WgZZN{[XluIFXDOVA:PC52IN88US=> NV:wS3A4OjZ{MkC1NVk>
human MDA-MB-231 cells MYrDfZRwfG:6aXPpeJkh[XO|YYm= NULZd2hiPDhiaB?= MmrvR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB2ODDodpMh[nlidIL5dIFvKGKudXWg[ZhkdHW|aX;uJIF{e2G7LDDJR|UxRTRwODFOwG0> MoPwNlQ{QDdzNUm=
human PC3 cells NIf4PFhEgXSxdH;4bYNqfHliYYPzZZk> MVG0PEBp NVjFbWFGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGGodHXyJFQ5KGi{czDifUB1enmyYX6gZox2\SCneHPseZNqd25iYYPzZZktKEmFNUC9Ok42KM7:TR?= MUWyOFM5PzF3OR?=
human Raji cells NXvXe4oxS3m2b4TvfIlkcXS7IHHzd4F6 Ml\iOFghcA>? NWSzU4VrS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWmGsaTDj[YxteyCjZoTldkA1QCCqcoOgZpkhfHK7cHHuJIJtfWViZYjjcJV{cW:wIHHzd4F6NCCLQ{WwQVkvOSEQvF2= MVmyOFM5PzF3OR?=
human PBMC M{SwSGN6fG:2b4jpZ4l1gSCjc4PhfS=> MUS0PEBp MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQRm1EKGGodHXyJFQ5KGi{czDifUB1enmyYX6gZox2\SCneHPseZNqd25iYYPzZZktKEmFNUC9NlMvQCEQvF2= NITNdIYzPDN6N{G1PS=>
human HCT116 cells M{HWZmN6fG:2b4jpZ4l1gSCjc4PhfS=> M1fEWmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczD2bYFjcWyrdImsJHRFPTB;MkWg{txO Ml;kNlM3Ozl4OES=

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: Rat hepatoma H4IIE cells
  • Concentrations: ~300 μM
  • Incubation Time: 48 hours
  • Method: Rat hepatoma H4IIE cells are used as the test system. These cells are grown in DMEM supplemented with fetal bovine serum (10%) and calf serum (10%). Cells are seeded into 96-well plates and after 48 h exposed to SGI-1027 at concentrations ranging from 0 to 300 µmol/L. The solubility is determined by Nephalometry techniques immediately after dosing and before harvesting the cells at 24 h. Following the exposure period, the cells or their supernatant (culture medium) are analyzed for changes in cell proliferation (propidium iodide), membrane leakage (α-GST), mitochondrial function [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and cellular ATP], oxidative stress (intracellular GSH and 8-isoprostane), and apoptosis. The half-maximal toxic concentration (TC50) is determined from the dose-response curves.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (199.34 mM)
Water Insoluble
Ethanol Insoluble

* 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.

Chemical Information

Molecular Weight 461.52
Formula

C27H23N7O

CAS No. 1020149-73-8
Storage powder
Synonyms DNA Methyltransferase Inhibitor II

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Related Antibodies

DNA Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID