217531
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
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
相关类别
一般描述
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
PRMT4
可逆性：是
次要靶标
SET7
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
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
免责声明
毒性：标准处理（A）
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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