920886
(S,R,S)-VL285 Phenol-PEG4-NH2 hydrochloride
别名:
(2S,4R)-N-(2-((14-Amino-3,6,9,12-tetraoxatetradecyl)oxy)-4-(4-methylthiazol-5-yl)benzyl)-4-hydroxy-1-((S)-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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所有图片(1)
About This Item
经验公式（希尔记法）:
C39H53N5O9S · xHCl
分子量:
767.93 (free base basis)
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.22
ligand
VL285 phenol
质量水平
表单
solid
反应适用性
reactivity: carboxyl reactive
reagent type: ligand-linker conjugate
官能团
amine
储存温度
2-8°C
SMILES字符串
O=C1N([C@H](C(N(C2)[C@H](C(NCC3=CC=C(C=C3OCCOCCOCCOCCOCCN)C(SC=N4)=C4C)=O)C[C@H]2O)=O)C(C)C)CC5=C1C=CC=C5.Cl
InChI key
WAOFVRRJKKKFIU-GJMJWEODSA-N
应用
Protein degrader building block (S,R,S)-VL285 Phenol-PEG4-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)
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
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
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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