Description

JenKem Technology provides high-purity PROTAC PEG linkers with various active groups and a range of E3 ligase ligands and E3 ligase ligand-linker conjugates to assist with your PROTAC-related projects. PROTAC (Proteolysis Targeting Chimera) is a novel technology that induces the targeted protein degradation by the ubiquitin–proteasome system. A PROTAC molecule consists of a ligand binding to the target protein, a ligand for recruiting an E3 ligase, and a linker.

The linker plays an important role in a PROTAC. The most common motifs incorporated into PROTAC linker structures are PEGs of different lengths [1]. Employing a PEG spacer in the linker influences the properties of the PROTAC:

– PEG linker increases the PROTAC water solubility, affecting the cell permeability, thereby improving oral absorption
– Linker length contributes to degradation efficiency and PEG molecules can be constructed with various lengths
– Bifunctional PEG linkers enable the rapid and facile assembly of structures containing different attachment sites

E3 Ligase Ligands

(S,R,S)-AHPC hydrochloride
4-Hydroxy-thalidomide
Pomalidomide

E3 Ligase Ligand-Linker Conjugates

(S,R,S)-AHPC-PEG2-acid
(S,R,S)-AHPC-PEG4-acid
(S,R,S)-AHPC-PEG6-acid
(S,R,S)-AHPC-PEG2-NH2 hydrochloride
(S,R,S)-AHPC-PEG4-NH2 hydrochloride
(S,R,S)-AHPC-PEG4-azide
(S,R,S)-AHPC-PEG6-alkyne
Thalidomide-O-PEG4-acid
Thalidomide-O-PEG4-NHS ester
Thalidomide-O-PEG4-t-butyl ester
Thalidomide-O-PEG4-amine
Thalidomide-O-PEG4-azide
Thalidomide-O-amido-PEG4-azide
Thalidomide-O-PEG4-propargyl
Thalidomide-O-amido-PEG4-propargyl
Pomalidomide-PEG3-acid
Pomalidomide-PEG4-Ph-NH2
Pomalidomide-PEG4-azide

Please contact us at sales@jenkemusa.com for more information about our E3 ligase ligands for PROTAC applications.

References:

1. Zhou X, et al., PROTAC: A promising technology for cancer treatment. Eur J Med Chem. 2020; 203:112539.
2. Troup RI, et al., Current strategies for the design of PROTAC linkers: a critical review. Explor Target Antitumor Ther. 2020; 1:273-312.

Founded in 2001 by experts in PEG synthesis and PEGylation, JenKem Technology specializes exclusively in the development and manufacturing of high quality polyethylene glycol (PEG) products and derivatives, and related custom synthesis and PEGylation services. JenKem Technology is ISO 9001 and ISO 13485 certified, and adheres to ICH Q7 guidelines for GMP manufacture. The production of JenKem® PEGs is back-integrated to in-house polymerization from ethylene oxide, enabling facile traceability for regulated customers. JenKem Technology caters to the PEGylation needs of the pharmaceutical, biotechnology, medical device and diagnostics, and emerging chemical specialty markets, from laboratory scale through large commercial scale.