929484
FBnG-C3-PEG1-C3-NH2 hydrochloride
≥95%
别名:
(R)-2-acetamido-3-((2-amino-9-(4-fluorobenzyl)-6-oxo-6,9-dihydro-1H-purin-8-yl)thio)-N-(3-(3-aminopropoxy)propyl)propanamide hydrochloride
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所有图片(1)
About This Item
经验公式（希尔记法）:
C23H31FN8O4S · xHCl
分子量:
534.61 (free base basis)
UNSPSC代码:
12352101
NACRES:
NA.21
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质量水平
方案
≥95%
表单
powder
官能团
amine
储存温度
2-8°C
SMILES字符串
O=C1NC(N)=NC2=C1N=C(SC[C@@H](C(NCCCOCCCN)=O)NC(C)=O)N2CC3=CC=C(C=C3)F.Cl
应用
Protein degrader building block FBnG-C3-PEG1-C3-NH2 hydrochloride enables the synthesis of molecules for degradation of proteins and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a p-fluorobenzylguanine (FBnG) ligand, a PEG linker, and a pendant amine for reactivity with a carboxylic acid on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and degrader, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a terminal amine, parallel synthesis can be used to more quickly generate degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.
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其他说明
法律信息
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Vittoria Zoppi et al.
Journal of medicinal chemistry, 62(2), 699-726 (2018-12-13)
Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently degrade a target protein within cells can be a lengthy and unpredictable process, and it remains unclear whether any combination of E3 and target might be productive for
Daiki Takahashi et al.
Molecular cell, 76(5), 797-810 (2019-10-14)
Protein silencing represents an essential tool in biomedical research. Targeted protein degradation (TPD) strategies exemplified by PROTACs are rapidly emerging as modalities in drug discovery. However, the scope of current TPD techniques is limited because many intracellular materials are not
Daniel P Bondeson et al.
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of
Kedra Cyrus et al.
Molecular bioSystems, 7(2), 359-364 (2010-10-06)
Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations
Momar Toure et al.
Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is
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