E3 ligase Ligand-Linker Conjugates 4

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E3 ligase Ligand-Linker Conjugates 4 manufacturers

E3 ligase Ligand-Linker Conjugates 4 Basic information
Product Name:E3 ligase Ligand-Linker Conjugates 4
Synonyms:E3 ligase Ligand-Linker Conjugates 4;VHL Ligand-Linker Conjugates 5;VH032-PEG4-N3;(2S,4R)-1-((S)-17-azido-2-(tert-butyl)-4-oxo-6,9,12,15-tetraoxa-3-azaheptadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;L-Prolinamide, N-(14-azido-1-oxo-3,6,9,12-tetraoxatetradec-1-yl)-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-
CAS:1797406-81-5
MF:C32H47N7O8S
MW:689.83
EINECS:
Product Categories:
Mol File:1797406-81-5.mol
E3 ligase Ligand-Linker Conjugates 4 Structure
E3 ligase Ligand-Linker Conjugates 4 Chemical Properties
storage temp. Storage temp. 2-8°C
form Liquid
color Colorless to off-white
Safety Information
MSDS Information
E3 ligase Ligand-Linker Conjugates 4 Usage And Synthesis
DescriptionUUN06815, also known as (S,R,S)-AHPC-PEG4-Azide, is a ProTAC building block. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant azide for click chemistry with an alkyne on the target ligand. When used with other protein degrader building blocks with a pendant azide group, parallel synthesis can be used to more quickly generate ProTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand. This product has no formal name at the moment.
Uses(S,R,S)-AHPC-PEG4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
IC 50VHL
References[1] Zengerle M, et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chemical Biology (2015), 10(8), 1770-1777. DOI:10.1021/acschembio.5b00216
E3 ligase Ligand-Linker Conjugates 4 Preparation Products And Raw materials
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