SGI-1027

Catalog No.S7276 Synonyms: DNA Methyltransferase Inhibitor II

For research use only.

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.

SGI-1027 Chemical Structure

CAS No. 1020149-73-8

Selleck's SGI-1027 has been cited by 12 Publications

2 Customer Reviews

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.
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 NGXnNJpEgXSxdH;4bYNqfHliYYPzZZk> MYO0PEBp MoTlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWVk{PyClZXzsd{Bi\nSncjC0PEBpenNiYomgeJJ6eGGwIHLseYUh\XilbIXzbY9vKGG|c3H5MEBKSzVyPUGuO{DPxE1? M3nRdFI1Ozh5MUW5
human KARPAS299 cells M1XzNXBzd2yrZnXyZZRqd25iYYPzZZk> NEO4OJQzNTRiZHH5dy=> NXL3O3JuSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLRXJRSVN{OUmgZ4VtdHNiYX\0[ZIhOiC2bzC0JIRigXNiYomgRXRRdGm2ZTCxd5RmeCCudX3pcoV{[2WwY3WgZZN{[XluIFXDOVA:OS56IN88US=> NUXkRVkyOjZ{MkC1NVk>
human KG1 cells MoPXVJJwdGmoZYLheIlwdiCjc4PhfS=> M{XBclIuPCCmYYnz NFnOdW1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvHNUBk\WyuczDh[pRmeiB{IITvJFQh\GG7czDifUBCXFCuaYTlJFF{fGWyIHz1cYlv\XOlZX7j[UBie3OjeTygSWM2OD12LkSg{txO NXnyUHZ4OjZ{MkC1NVk>
human MDA-MB-231 cells NF60b5JEgXSxdH;4bYNqfHliYYPzZZk> MX:0PEBp NXTmRpY{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjC0PEBpenNiYomgeJJ6eGGwIHLseYUh\XilbIXzbY9vKGG|c3H5MEBKSzVyPUSuPEDPxE1? NXK1SJFMOjR|OEexOVk>
human PC3 cells NIDUfmFEgXSxdH;4bYNqfHliYYPzZZk> M3j3blQ5KGh? MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IITyfZBidiCkbIXlJIV5[2y3c3nvckBie3OjeTygTWM2OD14LkWg{txO M{ixRlI1Ozh5MUW5
human Raji cells MnvIR5l1d3SxeHnjbZR6KGG|c3H5 NWe1O3pRPDhiaB?= M3HJbmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJicmliY3XscJMh[W[2ZYKgOFghcHK|IHL5JJRzgXCjbjDicJVmKGW6Y3z1d4lwdiCjc4PhfUwhUUN3ME25MlEh|ryP NGW1cI0zPDN6N{G1PS=>
human PBMC MoTpR5l1d3SxeHnjbZR6KGG|c3H5 MYS0PEBp M4\OSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBDVUNiYX\0[ZIhPDhiaILzJIJ6KHS{eYDhckBjdHWnIHX4Z4x2e2mxbjDhd5NigSxiSVO1NF0zOy56IN88US=> M{K5VFI1Ozh5MUW5
human HCT116 cells M4\veGN6fG:2b4jpZ4l1gSCjc4PhfS=> Mkn4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|II\pZYJqdGm2eTygWGQ2OD1{NTFOwG0> NVX0ZZVEOjN4M{m2PFQ>
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 30344731
Western blot Bcl-2 / Bax ; DNMT1 / TIMP3 / P16 30344731 19417133

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • 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.

Solubility (25°C)

In vitro

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.

2mg/mL

Chemical Information

Molecular Weight 461.52
Formula

C27H23N7O

CAS No. 1020149-73-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=NC(=N1)N)NC2=CC=C(C=C2)NC(=O)C3=CC=C(C=C3)NC4=CC=NC5=CC=CC=C54

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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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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