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品質水準
アッセイ
≥95%
フォーム
powder or chunks
反応適合性
reagent type: ligand
保管温度
2-8°C
SMILES記法
O=C1NC(N)=NC2=C1N=C(SC[C@@H](C(O)=O)NC(C)=O)N2CC3=CC=C(C=C3)F
アプリケーション
N-acetyl-S-(2-amino-9-(4-fluorobenzyl)-6-oxo-6,9-dihydro-1H-purin-8-yl)-L-cysteine is a p-fluorobenzylguanine (FBnG) based ligand used to initiate selective autophagy as a strategy for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology.
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Related Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation
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その他情報
AUTACs: Cargo-Specific Degraders Using Selective Autophagy
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs
Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs
Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders
法的情報
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
関連製品
製品番号
詳細
価格
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
929476-VAR:
929476-250MG:
929476-50MG:
929476-BULK:
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
William Farnaby et al.
Nature chemical biology, 15(7), 672-680 (2019-06-11)
Targeting subunits of BAF/PBAF chromatin remodeling complexes has been proposed as an approach to exploit cancer vulnerabilities. Here, we develop proteolysis targeting chimera (PROTAC) degraders of the BAF ATPase subunits SMARCA2 and SMARCA4 using a bromodomain ligand and recruitment of
Christian Steinebach et al.
Chemical science, 11(13), 3474-3486 (2020-11-03)
Cyclin-dependent kinase 6 (CDK6) is an important regulator of the cell cycle. Together with CDK4, it phosphorylates and inactivates retinoblastoma (Rb) protein. In tumour cells, CDK6 is frequently upregulated and CDK4/6 kinase inhibitors like palbociclib possess high activity in breast
Miriam Girardini et al.
Bioorganic & medicinal chemistry, 27(12), 2466-2479 (2019-03-04)
The von Hippel-Lindau (VHL) and cereblon (CRBN) proteins are substrate recognition subunits of two ubiquitously expressed and biologically important Cullin RING E3 ubiquitin ligase complexes. VHL and CRBN are also the two most popular E3 ligases being recruited by bifunctional
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
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