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Merck
모든 사진(1)

Key Documents

920762

Sigma-Aldrich

(S,R,S)-AHPC-benzyl-piperazine hydrochloride

동의어(들):

(2S,4R)-1-((S)-3,3-dimethyl-2-(4-(piperazin-1-ylmethyl)benzamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader, VH032 conjugate

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About This Item

실험식(Hill 표기법):
C34H44N6O4S · xHCl
Molecular Weight:
632.82 (free base basis)
NACRES:
NA.22

ligand

VH032

Quality Level

형태

solid

반응 적합성

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

작용기

amine

저장 온도

2-8°C

SMILES string

CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(C4=CC=C(CN5CC[ClH](CC5)=N)C=C4)=O)C(C)(C)C)=O)=O)C=C2

애플리케이션

Protein degrader building block (S,R,S)-AHPC-benzyl-piperazine hydrochloride 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, 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 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.

법적 정보

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

관련 제품

제품 번호
설명
가격

Storage Class Code

11 - Combustible Solids

WGK

WGK 3


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시험 성적서(COA)

Lot/Batch Number

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문서 라이브러리 방문

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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