E3 ligase Ligand-Linker Conjugates 4 Chemical Properties

storage temp. 

Storage temp. 2-8°C

form 

Liquid

color 

Colorless to off-white

E3 ligase Ligand-Linker Conjugates 4 Usage And Synthesis

Description

UUN06815, 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 50

VHL

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

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