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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-双-（3-溴-4-羟基亚苄基）哌啶-4-酮，3,5-双（3-溴-4-羟基亚苄基）-1-苯基哌啶-4-酮，PRMT抑制剂V

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About This Item

经验公式（希尔记法）:
C26H21Br2NO3
CAS号:
1020399-49-8
分子量:
555.26
MDL號碼:
MFCD23115307
分類程式碼代碼:
12352200
NACRES:
NA.28

品質等級

100

化驗

≥95% (HPLC)

形狀

solid

製造商／商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

orange

溶解度

DMSO: 50 mg/mL

運輸包裝

ambient

儲存溫度

2-8°C

SMILES 字串

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

一般說明

一种细胞可渗透的（双亚苄基）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，

包裝

用惰性气体包装

警告

毒性：标准处理（A）

其他說明

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

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 2

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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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

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