모든 사진(1)

문서

918350

C5 Lenalidomide-alkyne-piperidine hydrochloride

Name: C5 Lenalidomide-alkyne-piperidine hydrochloride
Brand: ALDRICH

≥95%

동의어(들):

N-(2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)-3-(piperidin-4-yl)propiolamide hydrochloride, Crosslinker-E3 Ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader

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모든 사진(1)

About This Item

실험식(Hill 표기법):

C₂₁H₂₂N₄O₄ · xHCl

Molecular Weight:

394.42 (free base basis)

추천 제품

Slide 1 of 10

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Sigma-Aldrich

921300

C5 Lenalidomide-pyrimidine-piperazine-PEG₁-NH₂ hydrochloride

Sigma-Aldrich

911755

C5 Lenalidomide-PEG₅-NH₂ hydrochloride

Sigma-Aldrich

911704

C5 Lenalidomine-C₃-NH₂ hydrochloride

Sigma-Aldrich

922153

(S,R,S)-VL285 Phenol-C₃-piperazine hydrochloride

Sigma-Aldrich

919454

CCW16-PEG₃-BocNH

Sigma-Aldrich

919969

C5 Lenalidomide-PEG₂-Butyl NH₂ hydrochloride

Sigma-Aldrich

921327

C5 Lenalidomide-PEG₆-Butyl NH₂ hydrochloride

Sigma-Aldrich

919896

C5 Lenalidomide-dipiperazine-NH₂ hydrochloride

Sigma-Aldrich

923885

Pomalidomide-piperazine-piperidine-4-carboxamide hydrochloride

Sigma-Aldrich

901504

Pomalidomide-PEG₃-CO₂H

ligand

C5 Lenalidomide

분석

≥95%

형태

powder or crystals

반응 적합성

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

작용기

amine

저장 온도

2-8°C

SMILES string

O=C1N(C2CCC(NC2=O)=O)CC3=CC(NC(C#CC4CCNCC4)=O)=CC=C31.Cl

애플리케이션

Protein degrader building block C5 Lenalidomide-alkyne-piperidine hydrochloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a Cereblon (CRBN)-recruiting ligand with alternative exit vector, a linker with added rigidity, 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 PROTAC, 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 PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

기타 정보

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC^® Degraders for Targeted Protein Degradation

Targeted Protein Degradation by Small Molecules

Small-Molecule PROTACS: New Approaches to Protein Degradation

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Impact of linker length on the activity of PROTACs

법적 정보

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

시험 성적서(COA)

제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.

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문서 라이브러리에서 최근에 구매한 제품에 대한 문서를 찾아보세요.

문서 라이브러리 방문

Targeted Protein Degradation by Small Molecules.

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

Impact of linker length on the activity of PROTACs.

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

Targeted Protein Degradation: from Chemical Biology to Drug Discovery.

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

Small-Molecule PROTACS: New Approaches to Protein Degradation.

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

문서

Degrader Building Blocks for Targeted Protein Degradation

Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.

자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..

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문서

C5 Lenalidomide-alkyne-piperidine hydrochloride

≥95%

About This Item

추천 제품

속성

ligand

분석

형태

반응 적합성

작용기

저장 온도

SMILES string

설명

애플리케이션

기타 정보

법적 정보

관련 제품

관련 제품

안전성 정보

Storage Class Code

WGK

Flash Point (°F)

Flash Point (°C)

문서

시험 성적서(COA)

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