For research use only.

Catalog No.S7276 Synonyms: DNA Methyltransferase Inhibitor II

9 publications

SGI-1027 Chemical Structure

CAS No. 1020149-73-8

SGI-1027 (DNA Methyltransferase Inhibitor II) is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B in cell-free assays, respectively. SGI‑1027 induces apoptosis.

Selleck's SGI-1027 has been cited by 9 publications

2 Customer Reviews

  • 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.

    Effect of SGI-1027 on the apoptosis of Huh7 cells. Flow cytometric analysis for apoptosis with Annexin V-FITC and propidium iodide staining on Huh7 cells following treatment with (A) 0.1% DMSO as a control, (B) 10 µmol/l, (C) 20 µmol/l and (D) 30 µmol/l of SGI-1027 for 24 h. Annexin V-FITC was used to identify the early apoptotic cells and the late apoptotic cells were assessed by PI staining.

    Oncol Lett, 2018, 16(5):5799-5806. SGI-1027 purchased from Selleck.

Purity & Quality Control

Choose Selective DNA Methyltransferase Inhibitors

Biological Activity

Description SGI-1027 (DNA Methyltransferase Inhibitor II) is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B in cell-free assays, respectively. SGI‑1027 induces apoptosis.
Features Potential for use in epigenetic cancer therapy.
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 M1vmfmN6fG:2b4jpZ4l1gSCjc4PhfS=> NGfBem41QCCq M1THWmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHU6OzdiY3XscJMh[W[2ZYKgOFghcHK|IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCjc4PhfUwhUUN3ME2xMlch|ryP MmjZNlQ{QDdzNUm=
human KARPAS299 cells MmPuVJJwdGmoZYLheIlwdiCjc4PhfS=> MXyyMVQh\GG7cx?= NF\rNVJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjZoTldkAzKHSxIESg[IF6eyCkeTDBWHBtcXSnIEHzeIVxKGy3bXnu[ZNk\W6lZTDhd5NigSxiRVO1NF0yNjhizszN MV[yOlIzODVzOR?=
human KG1 cells MXzQdo9tcW[ncnH0bY9vKGG|c3H5 NX61ZmZlOi12IHThfZM> NYXEOXVWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLS|Eh[2WubIOgZYZ1\XJiMjD0c{A1KGSjeYOgZpkhSVSSbHn0[UAye3SncDDseY1qdmW|Y3XuZ4Uh[XO|YYmsJGVEPTB;ND60JO69VQ>? M4G3dFI3OjJyNUG5
human MDA-MB-231 cells NVn3NFRYS3m2b4TvfIlkcXS7IHHzd4F6 NYDGN|NXPDhiaB?= MoT1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB2ODDodpMh[nlidIL5dIFvKGKudXWg[ZhkdHW|aX;uJIF{e2G7LDDJR|UxRTRwODFOwG0> M1rEflI1Ozh5MUW5
human PC3 cells MYjDfZRwfG:6aXPpeJkh[XO|YYm= MYe0PEBp NFvxPYtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgOFghcHK|IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCjc4PhfUwhUUN3ME22MlUh|ryP NILNVGMzPDN6N{G1PS=>
human Raji cells Mn3VR5l1d3SxeHnjbZR6KGG|c3H5 MVW0PEBp M1nUfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJicmliY3XscJMh[W[2ZYKgOFghcHK|IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCjc4PhfUwhUUN3ME25MlEh|ryP MnzGNlQ{QDdzNUm=
human PBMC NGP2RlFEgXSxdH;4bYNqfHliYYPzZZk> NF;zZ3Q1QCCq M2rLeGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBDVUNiYX\0[ZIhPDhiaILzJIJ6KHS{eYDhckBjdHWnIHX4Z4x2e2mxbjDhd5NigSxiSVO1NF0zOy56IN88US=> M3GzeFI1Ozh5MUW5
human HCT116 cells NXqxOVBpS3m2b4TvfIlkcXS7IHHzd4F6 MoK2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|II\pZYJqdGm2eTygWGQ2OD1{NTFOwG0> NFjPVpEzOzZ|OU[4OC=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 30344731     

Effect of SGI-1027 on the viability of Huh7 cells treated with SGI-1027 for 24 h. Cell viability was determined by using an MTS assay. ***P<0.01 and ****P<0.0001, compared with the control group. DMSO, dimethyl sulfoxide.

Western blot
Bcl-2 / Bax ; 

PubMed: 30344731     

Bcl-2 and BAX protein expression levels were evaluated by western blotting in Huh7 cells treated with different concentrations (0.1% DMSO as control, 10, 20, 30 µmol/l) of SGI-1027 for 24 h. β-actin was used as a loading control. 

DNMT1 / TIMP3 / P16 ; 

PubMed: 19417133     

Cells were treated with varying concentrations of decitabine and SGI-1027 continuously for 12 d. Whole-cell extracts were prepared and separated on a SDS-polyacrylamide gel and immunoblotted against antibodies specific for human DNMT1, TIMP3, P16, and Ku-70.

30344731 19417133


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
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

* 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


CAS No. 1020149-73-8
Storage powder
in solvent
Synonyms DNA Methyltransferase Inhibitor II
Smiles CC1=CC(=NC(=N1)N)NC2=CC=C(C=C2)NC(=O)C3=CC=C(C=C3)NC4=CC=NC5=CC=CC=C54

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DNA Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID