Boc-Gly-Lys-Arg-AMC | 109358-48-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Boc-Gly-Lys-Arg-AMC
• 英文别名: Boc-GKR-AMC；Boc-Gly-Lys-Arg-Mca；tert-butyl N-[2-[[(2S)-6-amino-1-[[(2S)-5-(diaminomethylideneamino)-1-[(4-methyl-2-oxochromen-7-yl)amino]-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]carbamate
• CAS: 109358-48-7
• 化学式: C₂₉H₄₄N₈O₇
• 分子量: 616.718
• InChiKey: GCCXTNKNTDPTJQ-SFTDATJTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  44
• 可旋转键数：
  17
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.517
• 拓扑面积：
  242
• 氢给体数：
  7
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  Boc-Gly-Lys-Arg-AMC 在 West Nile virus protease NS₂B(H)/NS₃-pro domains 、 水 、 二甲基亚砜 、 甘油 、 三羟甲基氨基甲烷 、 Triton X-100 作用下， 生成 7-氨基-4-甲基香豆素
  参考文献：
  名称：

  Effects of detergents on the West Nile virus protease activity

  摘要：

  Detergents such as Triton X-100 are often used in drug discovery research to weed out small molecule promiscuous and non-specific inhibitors which act by aggregation in solution and undesirable precipitation in aqueous assay buffers. We evaluated the effects of commonly used detergents, Triton X-100, Tween-20, Nonidet-40 (NP-40), Brij-35, and CHAPS, on the enzymatic activity of West Nile virus (WNV) protease. Unexpectedly, Triton X-100, Tween-20, and NP-40 showed an enhancement of in vitro WNV protease activity from 2 to 2.5-fold depending on the detergent and its concentration. On the other hand, Brij-35, at >= 0.001% enhanced the protease activity by 1.5-fold and CHAPS had the least enhancing effect. The kinetic analysis showed that the increase in protease activity by Triton X-100 was dose-dependent. Furthermore, at Triton X-100 and Tween-20 concentrations higher than 0.001%, the inhibition of compound B, one of the lead compounds against WNV protease identified in a high throughput screen (IC50 value of 5.7 +/- 2.5 mu M), was reversed. However, in the presence of CHAPS, compound B still showed good inhibition of WNV protease. Our results, taken together, indicate that nonionic detergents, Triton X-100, Tween, and NP-40 are unsuitable for the purpose of discrimination of true versus promiscuous inhibitors of WNV protease in high throughput assays. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2009.03.050

文献信息

• Novel class of metacaspases
  申请人：Inze G. Dirk

  公开号：US20060029995A1

  公开（公告）日：2006-02-09

  The invention relates to a novel class of metacaspases. More particularly, the present invention relates to the use of metacaspases, preferably plant metacaspases to process a protein at a cleavage site comprising an arginine or a lysine at the P1 position, and to the use of such metacaspases to modulate cell death.

  本发明涉及一类新型元天冬酶。更具体地说，本发明涉及利用元天冬酶（最好是植物元天冬酶）在包含 P1 位精氨酸或赖氨酸的裂解位点上处理蛋白质，以及利用这类元天冬酶调节细胞死亡。
• PROTEIN EXPRESSION SYSTEM
  申请人：Technologene Inc.

  公开号：EP0910658A1

  公开（公告）日：1999-04-28
• EP0910658A4
  申请人：——

  公开号：EP0910658A4

  公开（公告）日：2003-02-12
• A CLASS OF METACASPASES
  申请人：VIB, vzw

  公开号：EP1601764B1

  公开（公告）日：2010-04-28
• US5935824A
  申请人：——

  公开号：US5935824A

  公开（公告）日：1999-08-10