产品说明
一般描述
A cell-permeable (bis-benzylidene)piperidinone compound that acts as a selective inhibitor against CARM1/PRMT4 arginine methyltransferase activity (IC50 = 7.1 µM with PABP1 as substrate). It inhibits PRMT3 only at much higher concentrations (by 70% and 62% with 100 µM inhibitor using NPL3 or rpS2 as substrate, respectively), exhibiting little activity against PRMT1, PRMT5, PRMT6 (IC50 >100 µM), or four HKMTs (<20% inhibition against DOTL1, G9a, SET7, or Suv39H1 with 100 µM inhibitor). Shown to inhibit PSA promoter-mediated reporter transcription in LNCaP cells in a dose-dependent manner (by 74% and 97%, respectively, with 4 and 6 µM inhibitor).
包装
10 mg in Glass bottle
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Secondary Target
SET7
Primary Target
PRMT4
Target IC50: CARM1-mediated methylation over PRMT1 and SET7 (IC₅₀ = 7.1, 63 and 943 µM,
Reversible: yes
警告
Toxicity: Standard Handling (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
基本信息
| 经验(实验)分子式 | C26H21Br2NO3 |
| 分子量 | 555.26 |
| MDL编号 | MFCD23115307 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥95% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | 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℃ |
| SMILES string | 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 |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 2 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
