919357
(S,R,S)-AHPC-PEG1-piperazine hydrochloride
≥95%
동의어(들):
(2S,4R)-1-((S)-3,3-dimethyl-2-(3-(2-(piperazin-1-yl)ethoxy)propanamido)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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크기 선택
보기 변경
ligand
VH032
assay
≥95%
form
powder or crystals
reaction suitability
reagent type: ligand-linker conjugate
storage temp.
2-8°C
SMILES string
O=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)CCOCCN4CCNCC4.Cl
Application
Protein degrader building block (S,R,S)-AHPC-PEG1-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 semi-flexible linkers, and pendant amine for reactivity with an acid on the target warhead. Because even slight alterations in ligands, warheads, 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.
Other Notes
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
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
Legal Information
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
문서
Protein Degrader Building Blocks are a collection of crosslinker-E3 ligand conjugates with a pendant functional group for covalent linkage to a target ligand.
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
국제 무역 품목 번호
| SKU | GTIN |
|---|---|
| 919357-50MG | 04065265082716 |