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Key Documents

923907

Sigma-Aldrich

6F,C5-Pomalidomide-piperazine-piperidine-4-carbothioamide hydrochloride

同義詞:

2-(2,6-Dioxopiperidin-3-yl)-5-fluoro-6-(4-(piperidine-4-carbonothioyl)piperazin-1-yl)isoindoline-1,3-dione hydrochloride, Crosslinker–E3 ligase ligand conjugate, Protein degrader building block

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About This Item

經驗公式(希爾表示法):
C23H26FN5O4S · xHCl
分子量::
487.55 (free base basis)
分類程式碼代碼:
12352101
NACRES:
NA.21

ligand

6F,C5-Pomalidomide

品質等級

反應適用性

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

官能基

amine

儲存溫度

2-8°C

SMILES 字串

O=C1C(N2C(C(C=C(F)C(N3CCN(C(C4CCNCC4)=S)CC3)=C5)=C5C2=O)=O)CCC(N1)=O.Cl

應用

Protein degrader building block 6F,C5-Pomalidomide-piperazine-piperidine-4-carbothioamide hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC® (proteolysis-targeting chimeras) research. This conjugate contains a Cereblon (CRBN) recruiting ligand, a rigid 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.

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Protein Degrader Building Blocks

法律資訊

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

相關產品

產品號碼
描述
訂價

象形圖

Health hazard

訊號詞

Danger

危險聲明

危險分類

Repr. 1B

儲存類別代碼

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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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

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