539214
PRMT Inhibitor VI
别名:
PRMT Inhibitor VI, 1-(1,2,3-Benzothiadiazol-6-yl)-3-[2-(1-cyclohexen-1-yl)ethyl]urea, Protein Arginine Methyltransferase Inhibitor VI, 1-(Benzo[d][1,2,3]thiadiazol-6-yl)-3-(2-cyclohexenylethyl)urea
方案
≥99% (HPLC)
质量水平
表单
solid
效能
1.6 μM IC50
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
off-white
溶解性
DMSO: 100 mg/mL
运输
ambient
储存温度
2-8°C
一般描述
A benzothiadiazolyl-cyclohexenylethylurea compound that binds to protein arginine methyltransferase 3 at the dimer interface and selectively inhibits PRMT3 activity in an allosteric manner (IC50 = 1.6 µM), while being non-competitive with respect to AdoMet (S-adenosyl-L-methionine; SAM) or peptide substrates (Ki = 2.9 and 4.2 mM, respectively). Exhibits little or no inhibitory activity against PRMT1/4/5/8 or protein lysine methyltransferases, EHMT1, SUV39H2, SETD7, and SETD8, even at concentrations above 100 µM. Although cell-permeable, it is metabolically unstable and therefore not recommended for cell cultures or in vivo applications.
生化/生理作用
Cell permeable: yes
Primary Target
PRMT3
PRMT3
Reversible: yes
包装
Packaged under inert gas
制备说明
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Siarheyeva, A., et al. 2012. Structure20, 1425.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Alena Siarheyeva et al.
Structure (London, England : 1993), 20(8), 1425-1435 (2012-07-17)
PRMT3, a protein arginine methyltransferase, has been shown to influence ribosomal biosynthesis by catalyzing the dimethylation of the 40S ribosomal protein S2. Although PRMT3 has been reported to be a cytosolic protein, it has been shown to methylate histone H4
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