920894
(S,R,S)-VL285 Phenol-PEG2-NH2 hydrochloride
동의어(들):
(2R,4S)-N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)-4-(4-methylthiazol-5-yl)benzyl)-4-hydroxy-1-((R)-3-methyl-2-(1-oxoisoindolin-2-yl)butanoyl)pyrrolidine-2-carboxamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, VHL protein degrader building block for PROTAC® research
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C35H45N5O7S · xHCl
Molecular Weight:
679.83 (free base basis)
NACRES:
NA.22
추천 제품
ligand
VL285 phenol
Quality Level
형태
solid
반응 적합성
reactivity: carboxyl reactive
reagent type: ligand-linker conjugate
작용기
amine
저장 온도
2-8°C
SMILES string
O=C([C@H]1C[C@H](O)CN1C([C@@H](C(C)C)N2CC(C=CC=C3)=C3C2=O)=O)NCC4=CC=C(C5=C(C)N=CS5)C=C4OCCOCCOCCN.Cl
애플리케이션
Protein degrader building block (S,R,S)-VL285 Phenol-PEG2-NH2 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 with alternative exit vector from the widely used VH032 (901490), a PEG 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 terminal amine, 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)
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
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
Portal: Building PROTAC® Degraders for Targeted Protein Degradation
Targeted Protein Degradation by Small Molecules
Targeted Protein Degradation: from Chemical Biology to Drug Discovery
HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
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.
Dennis L Buckley et al.
ACS chemical biology, 10(8), 1831-1837 (2015-06-13)
Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes. One method for inducing targeted protein degradation involves the use of PROTACs, heterobifunctional molecules that can recruit specific E3 ligases to a desired protein of interest.
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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