(S,R,S)-VL285 Phenol-C3-piperazine hydrochloride

产品名称：

(S,R,S)-VL285 Phenol-C₃-piperazine hydrochloride
Crosslinker-E3 Ligase ligand conjugate
(2S,4R)-4-Hydroxy-1-((S)-3-methyl-2-(1-oxoisoindolin-2-yl)butanoyl)-N-(4-(4-methylthiazol-5-yl)-2-((6-(3-(piperazin-1-yl)propoxy)pyridin-3-yl)methoxy)benzyl)pyrrolidine-2-carboxamide
VHL protein degrader building block for PROTAC research

产品介绍：

产品说明

应用

Protein degrader building block (S,R,S)-VL285 Phenol-C₃-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 with alternative exit vector from the widely used VH032 (901490), a linker with added rigidity, 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.

其他说明

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

法律信息

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

基本信息

经验(实验)分子式	C₄₂H₅₁N₇O₆S · xHCl
分子量	781.96 (free base basis)

产品性质

质量水平	100
储存温度	2-8℃
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=C4OCC6=CC=C(OCCCN7CCNCC7)C=N6.Cl 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=C4OCC6=CC=C(OCCCN7CCNCC7)C=N6.Cl

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable