跳转至内容
Merck
CN

917214

Sigma-Aldrich

BocA1V2PF1-NHPEG3-NH2

≥85%

别名:

tert-Butyl ((S)-1-(((S)-2-((S)-2-(((S)-1-amino-13-oxo-15-phenyl-3,6,9-trioxa-12-azapentadecan-14-yl)carbamoyl)pyrrolidin-1-yl)-1-cyclohexyl-2-oxoethyl)amino)-1-oxopropan-2-yl)carbamate, AVP conjugate for IAP-mediated protein degrader development, Protein degrader building block for PROTAC® research

登录查看公司和协议定价


About This Item

经验公式(希尔记法):
C38H62N6O9
分子量:
746.93
UNSPSC代码:
41116105
NACRES:
NA.22

ligand

BocA1V2PF1

质量水平

检测方案

≥85%

形式

powder

反应适用性

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

官能团

amine

储存温度

2-8°C

SMILES字符串

C[C@H](NC(OC(C)(C)C)=O)C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(NCCOCCOCCOCCN)=O)CC2=CC=CC=C2)=O)=O)C3CCCCC3)=O

应用

Protein degrader building block BocA1V2PF1-NHPEG3-NH2 enables the synthesis of molecules for targeted protein degradation and SNIPER (specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein erasers) technology. Developed in partnership with ComInnex, this conjugate contains an in silico-derived IAP-recruiting ligand, an alkyl-chain crosslinker, and a pendant amine for reactivity with an acid on a target warhead. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and protein degrader, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a terminal amine, including CRBN and VHL targeted, parallel synthesis can be used to more quickly generate SNIPER and PROTAC® degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand. Learn more about the novel IAP ligands generated through virtual screening of AVP mimetics in our Technology Spotlight.

Building blocks in this series:
916978 BocA1V2PF1
917966 BocA1V2PF1-NHC6-NH2
916706 BocA1V2PF1-NHC10-NH2
916951 BocA1V2PF1-NHPEG1-NH2
917214 BocA1V2PF1-NHPEG3-NH2

Technology Spotlight: Degrader Building Blocks with Inhibitor of Apoptosis Protein (IAP) In Silico-Derived Ligands

法律信息

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

相关产品

产品编号
说明
价格

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

新产品

分析证书(COA)

输入产品批号来搜索 分析证书(COA) 。批号可以在产品标签上"批“ (Lot或Batch)字后找到。

已有该产品?

在文件库中查找您最近购买产品的文档。

访问文档库

Junjie Liu et al.
Minimally invasive therapy & allied technologies : MITAT : official journal of the Society for Minimally Invasive Therapy, 31(3), 332-341 (2020-11-05)
This paper evaluates the efficacy and safety of repeat hepatic resection and radiofrequency ablation in the treatment of recurrent hepatocellular carcinoma. We retrieved and collected all relevant articles from the inception to 8 March 2020. After data extraction, we conducted
Mikihiko Naito et al.
Drug discovery today. Technologies, 31, 35-42 (2019-06-16)
The induction of protein degradation by chimeric small molecules represented by proteolysis-targeting chimeras (PROTACs) is an emerging approach for novel drug development. We have developed a series of chimeric molecules termed specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein
Nobumichi Ohoka et al.
The Journal of biological chemistry, 292(11), 4556-4570 (2017-02-06)
Many diseases, especially cancers, result from aberrant or overexpression of pathogenic proteins. Specific inhibitors against these proteins have shown remarkable therapeutic effects, but these are limited mainly to enzymes. An alternative approach that may have utility in drug development relies

商品

Targeted protein degradation reduces disease-relevant proteins in cells using small molecules, hijacking endogenous proteolysis systems.

Plate of 80 ligands against E3 ligase IAP designed by ComInnex; allows creation of bifunctional targeted protein degraders or molecular glues.

Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

我们的科学家团队拥有各种研究领域经验,包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.

联系技术服务部门