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920835

Sigma-Aldrich

(S,R,S)-VL285 Phenol-piperazine-pyridine-alkyne-NH2 hydrochloride

Sinônimo(s):

(2S,4R)-N-{[2-(3-{4-[5-(3-Aminoprop-1-yn-1-yl)pyridin-2-yl]piperazin-1-yl}propoxy)-4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}-4-hydroxy-1-[(2S)-3-methyl-2-(1-oxo-2,3-dihydro-1H-isoindol-2-yl)butanoyl]pyrrolidine-2-carboxamide hydrochloride, Crosslinker−E3 Ligase ligand conjugate, VHL protein degrader building block for PROTAC® research

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About This Item

Fórmula empírica (Notação de Hill):
C44H52N8O5S · xHCl
Peso molecular:
805.00 (free base basis)
Código UNSPSC:
12352101
NACRES:
NA.22

ligand

VL285 phenol

Nível de qualidade

100

adequação da reação

reactivity: carboxyl reactive
reagent type: ligand-linker conjugate

grupo funcional

amine

temperatura de armazenamento

2-8°C

Categorias relacionadas

Aplicação

Protein degrader building block (S,R,S)-VL285 Phenol-piperazine-pyridine-alkyne-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 rigid inker, 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.

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC® Degraders for Targeted Protein Degradation

Outras notas

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

Informações legais

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

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Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

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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

Global Trade Item Number

SKUGTIN
920835-50MG4065266438789

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