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SGI-1027 DNA Methyltransferase inhibitor

Name: SGI-1027
Brand: Selleck Chemicals
SKU: S7276
Availability: InStock
Rating: 5 (15 reviews)

Cat.No.S7276

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. This compound induces apoptosis.

Chemical Structure

Molecular Weight: 461.52

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.58%

99.58

Related Targets	Epigenetic Reader Domain HDAC JAK Histone Methyltransferase AMPK PKC PARP HIF Histone Acetyltransferase Aurora Kinase Sirtuin PRMT Histone Demethylase EZH1/2 Pim LSD1 MLL JMJD G9a/GLP NSD FTO MicroRNA PAD SETD SMYD DOT1 COMT WDR5 HNMT SAM MTase
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
human U937 cells	Cytotoxicity assay	48 h	Cytotoxicity against human U937 cells after 48 hrs by trypan blue exclusion assay, IC50=1.7 μM
human KARPAS299 cells	Proliferation assay	2-4 days	Antiproliferative activity against human KARPAS299 cells after 2 to 4 days by ATPlite 1step luminescence assay, EC50=1.8 μM
human KG1 cells	Proliferation assay	2-4 days	Antiproliferative activity against human KG1 cells after 2 to 4 days by ATPlite 1step luminescence assay, EC50=4.4 μM
human MDA-MB-231 cells	Cytotoxicity assay	48 h	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by trypan blue exclusion assay, IC50=4.8 μM
human PC3 cells	Cytotoxicity assay	48 h	Cytotoxicity against human PC3 cells after 48 hrs by trypan blue exclusion assay, IC50=6.5 μM
human Raji cells	Cytotoxicity assay	48 h	Cytotoxicity against human Raji cells after 48 hrs by trypan blue exclusion assay, IC50=9.1 μM
human PBMC	Cytotoxicity assay	48 h	Cytotoxicity against human PBMC after 48 hrs by trypan blue exclusion assay, IC50=23.8 μM
human HCT116 cells	Cytotoxicity assay		Cytotoxicity against human HCT116 cells assessed as viability, TD50=25 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	461.52	Formula	C₂₇H₂₃N₇O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1020149-73-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Solubility

In vitro
Batch:

DMSO : 68 mg/mL (147.33 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 30%PEG300 2 2%Tween80 3 66%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (4.33mM)	Taking the 1 mL working solution as an example, add 20 μL of 100 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Potential for use in epigenetic cancer therapy.
Targets/IC₅₀/Ki	DNMT1 ^[1] (Cell-free assay) 6 μM DNMT3B ^[1] (Cell-free assay) 7.5 μM DNMT3A ^[1] (Cell-free assay) 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. This compound exhibits minimal or no cytotoxic effect in rat hepatoma H4IIE cells. ^[1] This chemical (0-100 μM) exhibits a moderate pro-apoptotic effect on U937 human leukemia cell line with no relevant changes on the cell cycle. ^[2]
Kinase Assay	DNA methyltransferase (CpG methyltransferase) assay
Kinase 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. 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 this compound, DNMT1 enzyme activityis measured in presence of a fixed concentration of this chemical (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 vivo	SGI-1027 (DNA Methyltransferase Inhibitor II) is a DNMT inhibitor .
References	[1] https://pubmed.ncbi.nlm.nih.gov/19417133/ [2] https://pubmed.ncbi.nlm.nih.gov/23402879/ [3] https://pubmed.ncbi.nlm.nih.gov/34461189/

Applications

Methods	Biomarkers	Images	PMID
Growth inhibition assay	Cell viability		30344731
Western blot	Bcl-2 / Bax DNMT1 / TIMP3 / P16		30344731

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