모든 사진(3)

문서

901855

(S,R,S)-AHPC-PEG₅-Alkyne

Name: (S,R,S)-AHPC-PEG5-Alkyne
Brand: ALDRICH

동의어(들):

(2S,4R)-1-((S)-2-(tert-Butyl)-4-oxo-7,10,13,16,19-pentaoxa-3-azadocos-21-ynoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC^® research, Template for synthesis of targeted protein degrader

로그인조직 및 계약 가격 보기

모든 사진(3)

About This Item

실험식(Hill 표기법):

C₃₆H₅₂N₄O₉S

Molecular Weight:

716.88

UNSPSC 코드:

51171641

NACRES:

NA.22

추천 제품

Slide 1 of 10

1 of 10

Sigma-Aldrich

903434

Pomalidomide-PEG₆-butyl azide

Sigma-Aldrich

764205

Alkyne-PEG4-maleimide

Sigma-Aldrich

904651

(S,R,S)-AHPC-PEG₃-azide

Sigma-Aldrich

88539

Ethyl azidoacetate solution

Sigma-Aldrich

901534

(S,R,S)-AHPC-C₆-CO₂H hydrochloride

Sigma-Aldrich

930644

VH 032 amide-PEG₂-acid

Sigma-Aldrich

901517

(S,R,S)-AHPC-PEG₂-Alkyne

Sigma-Aldrich

764191

Alkyne-PEG5-N-hydroxysuccinimidyl ester

Sigma-Aldrich

SML1556

AEM1

Sigma-Aldrich

918687

(S,R,S)-AHPC-alkyne-piperidine hydrochloride

형태

solid

반응 적합성

reaction type: click chemistry
reagent type: ligand-linker conjugate

작용기

alkyne

저장 온도

2-8°C

SMILES string

O=C(CCOCCOCCOCCOCCOCC#C)N[C@H](C(N1[C@H](C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)C(C)(C)C

애플리케이션

Protein degrader builiding block (S,R,S)-AHPC-PEG₅-Alkyne enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand and a PEGylated crosslinker with pendant alkyne for click chemistry with an azide 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 alkyne group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Automate your VHL-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)

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

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

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

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

문서

Partial PROTACs for Targeted Protein Degradation

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

Degrader Building Blocks for Targeted Protein Degradation

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

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고객지원팀으로 연락바랍니다.

문서

(S,R,S)-AHPC-PEG5-Alkyne

About This Item

추천 제품

속성

형태

반응 적합성

작용기

저장 온도

SMILES string

관련 카테고리

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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(S,R,S)-AHPC-PEG₅-Alkyne