PROTAC Linkers

PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules composed of two ligands; an “anchor” that binds to an E3 ubiquitin ligase and a “warhead” that binds to a protein of interest, connected by a chemical linker.

Figure 1: Schematic of typical PROTAC structure and an example (ARV-110).
Figure 1: Schematic of typical PROTAC structure and an example (ARV-110).

PROTAC linker plays a vital role in efficient ubiquitination of the target protein and its ultimate degradation. To date, several kinds of linkers have been reported and applied in PROTAC ternary complexes formation, such as PEG linker, Alkyl linker, alkyne linkers, and click chemistry linker, etc. 

PEG linkers are the most common motifs incorporated into PROTAC linker structures. According to statistics, 54% of the reported PROTAC molecules used PEG as a linker.
▶ The introduction of PEG can increase the water solubility of PROTAC molecules and affect cell permeability, thus affecting oral absorption.
▶ Systematic changes in linker length can be easily achieved by using PEGs of different chain lengths, affecting the degradation efficiency of PROTAC molecules.
​▶ The use of various bifunctionalized PEG linkers enables the simple and rapid assembly of molecules with different linker groups and accelerates the screening of efficient degradation structures.

Biopharma PEG is dedicated to the R&D of PROTAC Linker, providing high purity PEG linkers with various reactive groups to continuously assist your project development.

[1] Sun X, Gao H, Yang Y, et al. PROTACs: great opportunities for academia and industry.Signal Transduct Target Ther. 2019;4:64.
​[2]Troup RI, Fallan C, Baud MGJ. Current strategies for the design of PROTAC linkers: a critical review. Explor Target Antitumor Ther. 2020;1:273-312.

Catalog No. Name Structure M.W. Purity
MD005002 NH2-PEG3-OH NH2-PEG3-OH 149.18 ≥95%
MD005002 NH2-PEG4-OH NH2-PEG4-OH 193.2 ≥95%
MD005005 NH2-PEG2-NH2 NH2-PEG2-NH2 148.2 ≥95%
MD005016 NH2-PEG2-COOH NH2-PEG2-COOH 177.2 ≥95%
MD005016 NH2-PEG3-COOH NH2-PEG3-COOH 221.25 ≥95%
MD005016 NH2-PEG4-COOH NH2-PEG4-COOH 265.3 ≥95%
MD001002 mPEG5-OH mPEG5-OH 252.3 ≥95%
MD001005 mPEG3-NH2 mPEG3-NH2 163.2 ≥95%
MD001212 mPEG8-CH2CH2CHO mPEG8-CH2CH2CHO 396.5 ≥95%
MD002038 OH-PEG3-Tos OH-PEG3-Tos 304.359 ≥95%
MD005121 NH2-PEG2-CH2COOH NH2-PEG2-CH2COOH 163.2 ≥95%
MD005121 NH2-PEG3-CH2COOH NH2-PEG3-CH2COOH 207.22 ≥95%