跳转至内容
Merck
CN
所有图片(2)

主要文件

217531

Sigma-Aldrich

CARM1抑制剂

The CARM1 Inhibitor controls the biological activity of CARM1. This small molecule/inhibitor is primarily used for Cell Structure applications.

别名:

CARM1抑制剂, 共激活剂相关的精氨酸甲基转移酶1抑制剂,1-苄基-3,5--(3-溴-4-羟基亚苄基)哌啶-4-酮,3,5-(3-溴-4-羟基亚苄基)-1-苯基哌啶-4-酮,PRMT抑制剂V

登录查看公司和协议定价


About This Item

经验公式(希尔记法):
C26H21Br2NO3
分子量:
555.26
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.28

质量水平

方案

≥95% (HPLC)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

orange

溶解性

DMSO: 50 mg/mL

运输

ambient

储存温度

2-8°C

SMILES字符串

O=C(/C(CN(CC1=CC=CC=C1)C/2)=C/C3=CC=C(O)C(Br)=C3)C2=C\C4=CC(Br)=C(O)C=C4

InChI key

KNMFTTWVELIVCC-CLVAPQHMSA-N

一般描述

一种细胞可渗透的(亚苄基)哌啶酮化合物,可作为CARM1/PRMT4精氨酸甲基转移酶活性的选择性抑制剂(IC50 = 7.1 µM,以PABP1为底物)。它仅在更高的浓度下抑制PRMT3(分别使用NPL3或rpS2作为底物的100 µM抑制剂分别抑制70%和62%),对PRMT1,PRMT5,PRMT6(IC50 >100 µM)或四个HKMT(<20%抑制,针对用100 µM抑制剂的DOTL1,G9a,SET7或Suv39H1)几乎没有活性。显示以剂量依赖性方式抑制LNCaP细胞中PSA启动子介导的报告基因转录(用4和6 µM抑制剂分别抑制74%和97%)。

生化/生理作用

主要靶标
PRMT4
可逆性:是
次要靶标
SET7
细胞可渗透性:是
靶标IC50:CARM1介导的PRMT1和SET7甲基化(IC₅₀=7.1、63和943 µM,

包装

用惰性气体包装

警告

毒性:标准处理(A)

其他说明

Cheng, D., et al. 2011.J. Med. Chem.54, 4928.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

储存分类代码

11 - Combustible Solids

WGK

WGK 2

闪点(°F)

Not applicable

闪点(°C)

Not applicable


分析证书(COA)

输入产品批号来搜索 分析证书(COA) 。批号可以在产品标签上"批“ (Lot或Batch)字后找到。

已有该产品?

在文件库中查找您最近购买产品的文档。

访问文档库

Ricardo de Matos Simoes et al.
Nature cancer, 4(5), 754-773 (2023-05-27)
Clinical progress in multiple myeloma (MM), an incurable plasma cell (PC) neoplasia, has been driven by therapies that have limited applications beyond MM/PC neoplasias and do not target specific oncogenic mutations in MM. Instead, these agents target pathways critical for
Macheng Lu et al.
Oncology reports, 51(1) (2023-11-24)
Ribosome production factor 2 homolog (RPF2) plays an important role in the life processes of ribosomal biogenesis; however, the function and mechanism of RPF2 in tumors are unclear. The present study demonstrated that RPF2 expression is involved in chemoresistance in
Yugo Ishino et al.
Developmental neurobiology, 82(3), 245-260 (2022-02-28)
Protein arginine methylation has been recognized as one of key posttranslational modifications for refined protein functions, mediated by protein arginine methyltransferases (Prmts). Coactivator-associated arginine methyltransferase (Carm1, also known as Prmt4) participates in various cellular events, such as cell survival, proliferation
Yiming Cheng et al.
Molecular therapy. Nucleic acids, 34, 102063-102063 (2023-11-29)
Ferroptosis is an iron-catalyzed form of regulated cell death that results from the accumulation of lipid peroxidation products and reactive oxygen species to a lethal content. However, the transcriptional regulation of ferroptosis is not well understood. Sorafenib, a standard drug

我们的科学家团队拥有各种研究领域经验,包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.

联系技术服务部门