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N-酞酰-L-色氨酸

N-酞酰-L-色氨酸用途

RG108 是一种非核苷的 DNA 甲基转移酶 (DNA methyltransferase) 抑制剂,IC50 值为 115 nM。

N-酞酰-L-色氨酸名称

[ CAS 号 ]:
48208-26-0

[ 中文名 ]:
N-酞酰-L-色氨酸

[ 英文名 ]:
RG108

[英文别名 ]:

DNA Methyltransferase Inhibitor
N-phthalimide l-tryptophane
N-Phthalyl-L-tryptophan
N-Phth-Trp-OH
RG108

N-酞酰-L-色氨酸生物活性

[ 描述 ]:

RG108 是一种非核苷的 DNA 甲基转移酶 (DNA methyltransferase) 抑制剂,IC50 值为 115 nM。

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> DNA甲基转移酶

研究领域 >> 癌症

[ 靶点 ]

CpG methylase M.SssI:115 nM (IC50)

[体外研究]

RG108在体外有效阻断DNA甲基转移酶,并且不会在人细胞系中引起共价酶捕获。用低微摩尔浓度的RG108孵育细胞导致基因组DNA的显着去甲基化而没有任何可检测的毒性。有趣的是,RG108引起肿瘤抑制基因的去甲基化和再激活,但它不影响着丝粒卫星序列的甲基化[1]。在另一项研究中,研究了生物素化RG108结合物的合成和体外分析,以评估与DNA甲基转移酶的相互作用[2]。在最近的一项研究中,显示与天然SM相比,RG108可以显着降低SM衍生的iPS细胞中的DNA甲基转移酶活性[3]。

[激酶实验]

用于体外甲基化测定的底物DNA是来自人p16Ink4a基因的启动子区的798bp片段（相对于起始密码子为-423 / + 375）。甲基化反应含有350至400ng底物DNA和4单位M.SssI甲基化酶（0.5μM），终体积为50μL。加入抑制剂至终浓度分别为10,100,200和500μM。反应在37℃下进行2小时。完成后，将反应在65℃下灭活15分钟，并使用PCR纯化试剂盒纯化DNA。将300纳克纯化的DNA在60℃下用30单位BstUI消化3小时，并在2％Tris-硼酸盐EDTA琼脂糖凝胶上分析。

[参考文献]

[1]. Brueckner B, et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res. 2005 Jul 15;65(14):6305-11.

[2]. Schirrmacher E, et al. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug Chem. 2006 Mar-Apr;17(2):261-6.

[3]. Pasha Z, et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitor cells. PLoS One. 2011;6(8):e23667.

[相关活性小分子]

阿扎胞苷 | SGI-1027 | 泽布拉林 | 罗米鲁曲 | 桧木醇 | 谷维素 | DC_517 | DC-05 | 葡萄糖缀合的MGMT抑制剂

N-酞酰-L-色氨酸物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
606.0±50.0 °C at 760 mmHg

[ 熔点 ]:
192-194℃

[ 分子式 ]:
C₁₉H₁₄N₂O₄

[ 分子量 ]:
334.326

[ 闪点 ]:
320.3±30.1 °C

[ 精确质量 ]:
334.095367

[ PSA ]:
90.47000

[ LogP ]:
3.33

[ 外观性状 ]:
yellow

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.741

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
DMSO: >10mg/mL

N-酞酰-L-色氨酸MSDS

详细MSDS(安全技术说明书)

N-酞酰-L-色氨酸安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

N-酞酰-L-色氨酸文献

Inhibition of DNA methyltransferase as a novel therapeutic strategy to overcome acquired resistance to dual PI3K/mTOR inhibitors.

Oncotarget 6(7) , 5134-46, (2015)

Dual PI3K/mTOR(phosphatidylinositol 3-kinase/mammalian target of rapamycin) inhibitors are being evaluated clinically for the treatment of tumors with a hyperactivated PI3K/mTOR pathway. However, unex...

c-ETS transcription factors play an essential role in the licensing of human MCM4 origin of replication.

Biochim. Biophys. Acta 1849 , 1319-28, (2015)

In metazoans, DNA replication is a highly regulated and ordered process that occurs during the S phase of cell cycle. It begins with the licensing of origins of replication usually found in close prox...

DNA methyltransferase DNMT3A associates with viral proteins and impacts HSV-1 infection.

Proteomics 15 , 1968-82, (2015)

Viral infections can alter the cellular epigenetic landscape, through modulation of either DNA methylation profiles or chromatin remodeling enzymes and histone modifications. These changes can act to ...

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