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SGI-1027

SGI-1027 (DNA Methyltransferase Inhibitor II) 是一种 DNA 甲基转移酶(DNMT)抑制剂，对以 poly(dI-dC) 为底物的 DNMT3B，DNMT3A 和 DNMT1 的IC50值分别为 7.5 μM，8 μM 和 12.5 μM。

CAS号

1020149-73-8

分子式

C27H23N7O

主要靶点

Apoptosis|DNA Methyltransferase

仅限科研使用

Cat No : CM03700

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Synonyms

SGI1027|DNA Methyltransferase Inhibitor II

验证数据展示

  • CAS No.: 1020149-73-8

    SGI-1027
    CAS#: 1020149-73-8

产品信息

SGI-1027 (DNA Methyltransferase Inhibitor II) is an effective and selective inhibitor of DNA methyltransferase (DNMT). The IC50 of SGI-1027(SGI1027) against DNMT1, DNMT3A, and DNMT3B are 6, 8, 7.5 μM, respectively.

CAS号 1020149-73-8
分子式 C27H23N7O
主要靶点 Apoptosis|DNA Methyltransferase
主要通路 表观遗传|凋亡
分子量 461.52
纯度 99.18%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 SGI1027|DNA Methyltransferase Inhibitor II

靶点活性

DNMT3B:7.5 μM|DNMT3a:8 μM|DNMT1:6 μM

体内活性

在U937人白血病细胞系中,SGI-1027（0-100 μM）显示出适度的促凋亡作用,单不影响细胞周期。SGI-1027可直接抑制DNMTs使DNA甲基化受到抑制,并使各种人癌细胞系中的DNMT1选择性降解。在大鼠肝癌H4IIE细胞中,SGI-1027毒性很小或没有。

溶解度

DMSO:23.1 mg/mL (50 mM)

细胞实验

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)

参考文献

1.Datta J, et al. Cancer Res. 2009, 69(10), 4277-4285.
2.García-Domínguez P, et al. Bioorg Med Chem Lett. 2013, 23(6):1631-5.

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