929301
FBnG-C3-PEG3-C3-NH2 hydrochloride
≥95%
別名:
(R)-2-Acetamido-3-((2-amino-9-(4-fluorobenzyl)-6-oxo-6,9-dihydro-1H-purin-8-yl)thio)-N-(3-(2-(2-(3-aminopropoxy)ethoxy)ethoxy)propyl)propanamide hydrochloride
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About This Item
実験式（ヒル表記法）:
C27H39FN8O6S · xHCl
分子量:
622.71 (free base basis)
UNSPSCコード:
12352101
NACRES:
NA.21
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品質水準
アッセイ
≥95%
形状
powder
官能基
amine
保管温度
2-8°C
SMILES記法
O=C1NC(N)=NC2=C1N=C(SC[C@@H](C(NCCCOCCOCCOCCCN)=O)NC(C)=O)N2CC3=CC=C(C=C3)F.Cl
アプリケーション
Protein degrader building block FBnG-C3-PEG3-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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その他情報
法的情報
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
929301-BULK:
929301-VAR:
929301-50MG:
最新バージョンのいずれかを選択してください：
試験成績書（COA）
Lot/Batch Number
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
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
Philipp M Cromm et al.
Cell chemical biology, 24(9), 1181-1190 (2017-06-27)
Traditional pharmaceutical drug discovery is almost exclusively focused on directly controlling protein activity to cure diseases. Modulators of protein activity, especially inhibitors, are developed and applied at high concentration to achieve maximal effects. Thereby, reduced bioavailability and off-target effects can
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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