PROTAC PEG LINKERS

Please contact us at sales@jenkemusa.com for a quotation for our high-purity PROTAC PEG linkers with various active groups, E3 ligase ligands, and E3 ligase ligand-linker conjugates

 

Description

Newsletter PROTAC PEG LinkersJenKem 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

PROTAC PEG Linkers

Product Name CAS No.
Amino PEG2 Propionic Acid 791028-27-8
Amino PEG3 Propionic Acid 784105-33-5
Amino PEG4 Propionic Acid 663921-15-1
Amino PEG2 Acetic Acid 134978-97-5
Amino PEG3 Acetic Acid 134978-99-7
Amino PEG4 Acetic Acid 195071-49-9
Hydroxyl PEG4 Amine, HCl Salt 86770-74-3
Hydroxyl PEG3 Azide 86520-52-7
Azido-PEG3-Acetic Acid 172531-37-2
Azido-PEG4-Propionic Acid 1257063-35-6
Alkyne PEG5 Propionic Acid 1951438-84-8
Alkyne PEG6 Amine, HCl Salt 1589522-46-2
Propionic Acid PEG5 Propionic Acid 119189-70-7

Ligands for E3 Ligase

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

E3 Ligase Ligand – PEG Linker Conjugates

Product Name CAS No.
(S,R,S)-AHPC PEG2 Propionic Acid 2172820-09-4
(S,R,S)-AHPC PEG4 Propionic Acid 2172820-12-9
(S,R,S)-AHPC PEG6 Propionic Acid
(S,R,S)-AHPC PEG2 Amine, HCl Salt 2010159-60-9
(S,R,S)-AHPC PEG4 Amine, HCl Salt 2010159-57-4
(S,R,S)-AHPC PEG4 Azide
(S,R,S)-AHPC PEG5 Alkyne
Thalidomide-O PEG4 Propionic Acid 2353563-50-3
Thalidomide-O PEG4 Succinimidyl Propionate 2411681-88-2
Thalidomide-O PEG4 tert-Butyl Propionate 2411681-87-1
Thalidomide-O PEG5 Amine, HCl Salt 2401832-00-4
Thalidomide-O PEG5 Azide 2380318-57-8
Thalidomide-O Amido PEG5 Azide 2411681-89-3
Thalidomide-O PEG4 Alkyne 2098799-77-8
Thalidomide-O Amido PEG4 Alkyne 2411681-90-6
Pomalidomide PEG3 Propionic Acid
Pomalidomide PEG4 Phenyl Amine 1818885-63-0
Pomalidomide PEG5 Azide 2271036-47-4

Please contact us at sales@jenkemusa.com for more information about our linkers 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.

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