现货大促销,价格低至8折起,量大更优惠,详细咨询客服
全部分类
全部分类
  • SGC707
SGC707的可视化放大

SGC707

A potent allosteric inhibitor of PRMT3

原价
¥525-2437
价格
420-1950
SGC707的二维码

所有产品仅用于科学研究,我们不为任何个人用途提供产品和服务

询价有惊喜,量大更优惠 点击这里给我发消息

  • 库存: 现货
可选包装 >>>
首页
  • 货号: ajci9990
  • CAS: 1687736-54-4
  • 别名:
  • 分子式: C16H18N4O2
  • 分子量: 298.34
  • 纯度: >98%
  • 溶解度: ≥ 29.8mg/mL in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

SGC707 is a selective, potent, low molecular weight (MW = 298) and cell-active allosteric inhibitor of protein arginine N-methyltransferase 3 (PRMT3). PRMT3, one of the four type I protein arginine N-methyltransferases, has been implicated in ribosomal biosynthesis via catalyzing the formation of asymmetric (type I) mono- and dimethylarginine. PRMT3 has also been involved in cancer via interaction with the DAL-1 tumor suppressor protein [1]. SGC707 inhibits the activity of PRMT3 by targeting the dimerization interface of PRMT3[2].


In vitro: The IC50 and KD value of SGC707 against PRMT3was 31 ± 2 nM and 53 ± 2 nM respectively. SGC707 showed an outstanding selectivity for PRMT3 against 31 other methyltransferases and a broad range of 250 non-epigenetic targets, G protein-coupled receptors (GPCRs), ion channels, and transporters. The residence time of SGC707 was 9.7 min. In both HEK293 and A549 cells, SGC707 stabilized PRMT3 with EC50 values of 1.3 μM and 1.6 μM, respectively. SGC707 treatment at high concentrations 50 and 100 mM for 72 h lead to some toxicity [1].


In vivo: In CD-1 male mice, intraperitoneal injection of SGC707 at 30 mg/kg for over 6 h showed good plasma exposure with the peak plasma level of 38 μM. After injection 6 h, the plasma level of SGC707 decreased to 208 nM. The half-life of SGC707 was about 1 h. The 30 mg/kg dose was well tolerated in the tested mouse model [1].

参考文献:
[1].Kaniskan H, Szewczyk M M, Yu Z, et al.? A Potent, Selective and Cell‐Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)[J]. Angewandte Chemie International Edition, 2015, 54(17): 5166-5170.
[2].Luo M.? Inhibitors of protein methyltransferases as chemical tools[J]. Epigenomics, 2015, 7(8): 1327-1338.

动态评分

0.0

没有评分数据
没有评价数据
一键回到顶部
展开 收缩
安捷凯在线客服