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Merck

911003

Sigma-Aldrich

Pomalidomide-PEG2-butyl amine hydrochloride

≥95%

別名:

2-(2-((6-Aminohexyl)oxy)ethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)acetamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, Pomalidomide conjugate, Pomalidomide-2-2-6-NH2 HCl salt, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader

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About This Item

実験式(ヒル表記法):
C23H30N4O7
分子量:
474.51
UNSPSCコード:
12352101

ligand

pomalidomide

アッセイ

≥95%

形状

solid

反応適合性

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

官能基

amine

保管温度

2-8°C

SMILES記法

O=C(C(CC1)N(C2=O)C(C3=C2C=CC=C3NC(COCCOCCCCCCN)=O)=O)NC1=O.Cl

アプリケーション

Protein degrader builiding block Pomalidomide-PEG2-butyl amine hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant amine acid 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 PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

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

911003-BULK:
911003-VAR:
911003-50MG:


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文書ライブラリにアクセスする

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
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

資料

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

Partial PROTACs are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

関連コンテンツ

Targeted protein degradation (TPD) is an emerging drug discovery strategy that uses small-molecules, such as proteolysis-targeting chimeras (PROTACs), to eradicate targeted proteins linked to disease from cells.

ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.

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