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SGI-1027

別名：DNA Methyltransferase Inhibitor II

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化学構造

CAS No. 1020149-73-8

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 145500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
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SGI-1027関連製品

シグナル伝達経路

DNA Methyltransferase Signaling Pathways

DNA Methyltransferaseシグナル伝達経路

DNA Methyltransferase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
human PBMC Cytotoxicity assay 48 h Cytotoxicity against human PBMC after 48 hrs by trypan blue exclusion assay, IC50=23.8 μM 24387159
human Raji cells Cytotoxicity assay 48 h Cytotoxicity against human Raji cells after 48 hrs by trypan blue exclusion assay, IC50=9.1 μM 24387159
human PC3 cells Cytotoxicity assay 48 h Cytotoxicity against human PC3 cells after 48 hrs by trypan blue exclusion assay, IC50=6.5 μM 24387159
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 24387159
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 26220519
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 26220519
human U937 cells Cytotoxicity assay 48 h Cytotoxicity against human U937 cells after 48 hrs by trypan blue exclusion assay, IC50=1.7 μM 24387159
human HCT116 cells Cytotoxicity assay Cytotoxicity against human HCT116 cells assessed as viability, TD50=25 μM 23639684
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生物活性

製品説明 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.
特性 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
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]
Kinase Assay 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. 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.
細胞実験 細胞株 Rat hepatoma H4IIE cells
濃度 ~300 μM
反応時間 48 hours
実験の流れ

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.
実験結果図 Methods Biomarkers 結果図 PMID
Growth inhibition assay Cell viability 30344731
Western blot Bcl-2 / Bax DNMT1 / TIMP3 / P16 30344731
In Vivo
In Vivo

SGI-1027 (DNA Methyltransferase Inhibitor II) is a DNMT inhibitor .
動物実験 動物モデル Male Sprague-Dawley rats
投与量 11.2 mg/kg
投与経路 i.p.

化学情報

分子量 461.52 化学式

C27H23N7O
CAS No. 1020149-73-8 SDF Download SGI-1027 SDFをダウンロードする
Smiles CC1=CC(=NC(=N1)N)NC2=CC=C(C=C2)NC(=O)C3=CC=C(C=C3)NC4=CC=NC5=CC=CC=C54
保管

In vitro
Batch:

DMSO : 68 mg/mL ( (147.33 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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