PROTAC Linkers, PEG Linkers Supply

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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).

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.

References:
[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. https://doi.org/10.37349/etat.2020.00018

Catalog No.	Name	Structure	M.W.	Purity	Buy
MD006002	N3-PEG3-OH		175.186	≥95%

MD006002	N3-PEG7-OH		351.4	≥95%

MD006005	N3-PEG2-NH2		174.2	≥95%

MD006005	N3-PEG4-NH2		262.31	≥95%

MD006016	N3-PEG3-COOH		247.3	≥95%

MD006016	N3-PEG4-COOH		291.301	≥95%

MD006016	N3-PEG5-COOH		335.35	≥95%

MD006016	N3-PEG6-COOH		379.41	≥95%

MD006016	N3-PEG8-COOH		467.51	≥95%

MD006016	N3-PEG9-COOH		511.56	≥95%

MD002038	OH-PEG3-Tos		304.359	≥95%

MD001002	mPEG5-OH		252.3	≥95%

MD001002	mPEG12-OH		560.67	≥95%

MD005002	NH2-PEG3-OH		149.18	≥95%

MD005016	NH2-PEG2-COOH		177.2	≥95%

MD005016	NH2-PEG3-COOH		221.25	≥95%

MD005016	NH2-PEG4-COOH		265.3	≥95%

MD005016	NH2-PEG6-COOH		353.4	≥95%

MD005067	NH2-PEG4-CH2CH2COOtBu		321.4	≥95%

MD005067	NH2-PEG6-CH2CH2COOtBu		409.5	≥95%

MD068006	Boc-NH-PEG11-N3		670.79	≥89%

MD068038	Boc-NH-PEG2-Tos		403.49	≥95%

MD068038	Boc-NH-PEG3-Tos		447.54	≥95%

MD141025	Mal-PEG1-SPA		310.26	≥95%

MD000121	Bis-PEG1-C-PEG1-CH2COOH		350.4	≥95%

MD002067	OH-PEG4-CH2CH2COOtBu		322.39	≥95%

MD002121	OH-PEG3-CH2COOH		208.21	≥95%

MD005005	NH2-PEG2-NH2		148.2	≥95%

MD005121	NH2-PEG2-CH2COOH		163.2	≥95%

MD005121	NH2-PEG3-CH2COOH		207.22	≥95%

MD005121	NH2-PEG4-CH2COOH		251.3	≥95%

MD005128	NH2-PEG3-CH2COOtBu		263.33	≥95%

MD006121	N3-PEG3-CH2COOH		233.22	≥95%

MD006121	N3-PEG4-CH2COOH		277.27	≥95%

MD016016	COOH-PEG3-COOH		294.298	≥95%

MD016016	COOH-PEG5-COOH		382.403	≥95%

MD038005	Tos-PEG2-NH2		259.32	≥95%

MD038038	Tos-PEG4-Tos		502.6	≥95%

MD038330	Tos-PEG3-O-C1-CH3COO		376.42	≥95%

MD007005	Alkyne-PEG2-NH2		143.2	≥95%

MD007005	Alkyne-PEG5-NH2		275.3	≥95%

MD007016	Alkyne-PEG3-COOH		216.2	≥95%

MD056006	Br-PEG2-N3		238.08	≥95%

MD056006	Br-PEG3-N3		282.1	≥95%

MD056068	Br-PEG4-NH-Boc		400.31	≥95%

MD068002	Boc-NH-PEG2-OH		205.252	≥95%

MD068002	Boc-NH-PEG3-OH		249.3	≥95%

MD068002	Boc-NH-PEG4-OH		293.4	≥95%

MD068002	Boc-NH-PEG6-OH		381.5	≥95%

MD068005	BOC-NH-PEG3-NH2		292.4	≥95%

MD068005	BOC-NH-PEG5-NH2		380.5	≥95%

MD068121	Boc-NH-PEG2-CH2COOH		263.3	≥95%

MD068325	Boc-NH-PEG2-C2-amido-C4-acid		376.45	≥95%

MD005286	Thalidomide-O-amido-PEG3-NH2		506.509	≥95%

MD128324	Boc-C1-PEG2-C4-Cl		294.81	≥95%

MD170170	Bis-NH2-C1-PEG3		220.31	≥95%

MD288005	Pomalidomide-PEG4-NH2		492.52	≥95%

MD288007	Pomalidomide-PEG2-Propargyl		399.4	≥95%

MD288016	Pomalidomide-PEG1-COOH		389.36	≥95%

MD288016	Pomalidomide-PEG2-COOH		433.41	≥95%

MD288016	Pomalidomide-PEG3-COOH		477.46	≥95%

MD288016	Pomalidomide-PEG4-COOH		521.52	≥95%

MD288016	Pomalidomide-PEG5-COOH		565.57	≥95%

MD121288	Pomalidomide-PEG4-CH2COOH		507.493	≥95%

MD288050	Pomalidomide-PEG3-NH2.HCl		484.93	≥95%

MD288065	Pomalidomide-PEG4-Ph-NH2		540.57	≥95%

MD324121	Cl-C6-PEG4-O-CH2COOH		370.87	≥95%

MD326304	Dox-Ph-PEG1-Cl		228.67	≥95%

MD327006	Pomalidomide-NH-CO-PEG1-N3		400.35	≥95%

MD327328	Pomalidomide-PEG2-butyl iodide		585.39	≥95%

MD327328	Pomalidomide-PEG6-butyl iodide		761.6	≥95%

MD286050	Thalidomide-O-amido-PEG1-NH2.HCl		454.86	≥95%

MD286050	Thalidomide-O-amido-PEG2-NH2.HCl		498.92	≥95%

MD286123	Thalidomide-O-amido-PEG2-NH2.TFA		576.48	≥95%

MD329005	Thalidomide-O-PEG4-NH2		493.51	≥95%

MD329006	Thalidomide-O-PEG4-N3		519.51	≥95%

MD329007	Thalidomide-O-PEG2-Propargyl		400.38	≥95%

MD329007	Thalidomide-O-PEG4-Propargyl		488.49	≥95%

MD329025	Thalidomide-O-PEG2-SPA		531.47	≥95%

MD329025	Thalidomide-O-PEG4-SPA		619.57	≥95%

MD329038	Thalidomide-O-PEG5-Tosyl		648.68	≥95%

MD329050	Thalidomide-O-PEG5-NH2.HCl		574.02	≥95%

MD329067	Thalidomide-O-PEG4-t-butyl ester		578.61	≥95%