PEG Linkers
PEG linkers provide covalent spacing and hydrophilicity in drug conjugates, rather than receptor-level agonism or inhibition[1]. Mechanistically, PEGylation links one or more polyethylene glycol chains to protein, peptide, or non-peptide molecules and improves delivery-relevant physicochemical behavior[1]. Releasable PEGylation uses customized linkers that reversibly tether therapeutic moieties to polyethylene glycol polymers, enabling regeneration of authentic and fully active drug[2]. In antibody-drug conjugates, hydrophilic PEG-containing linkers mask or reduce payload hydrophobicity and improve physical stability and in vivo performance[3]. Disease-model studies in cancer ADC research show that hydrophilic linker design supports antibody-maytansinoid conjugates and PEGylated glucuronide-MMAE conjugates[4][5]. Compared with alkyl linkers in PROTACs, ethylene glycol linkers can reduce cell permeability, showing that linker polarity and folding must be optimized for intracellular degrader design[6]. Compared with other hydrophilic linker classes, PEG linkers act as monodisperse hydrophilicity reservoirs for highly loaded lysine-conjugated ADCs[3]. For experimental applications, PEG linker selection should prioritize spacer length, cleavable release chemistry, hydrophilicity, aggregation control, and payload exposure in ADC, PEGylation, and PROTAC projects[2][3][6][7].
References:
- [1]. Veronese FM, et al. PEGylation, successful approach to drug delivery. Drug Discov Today. 2005 Nov 1;10(21):1451-8. [Content Brief]
- [2]. Filpula D, et al. Releasable PEGylation of proteins with customized linkers. Adv Drug Deliv Rev. 2008 Jan 3;60(1):29-49. [Content Brief]
- [3]. Tedeschini T, et al. Polyethylene glycol-based linkers as hydrophilicity reservoir for antibody-drug conjugates. J Control Release. 2021 Sep 10;337:431-447. [Content Brief]
- [4]. Zhao RY, et al. Synthesis and evaluation of hydrophilic linkers for antibody-maytansinoid conjugates. J Med Chem. 2011 May 26;54(10):3606-23. [Content Brief]
- [5]. Burke PJ, et al. Optimization of a PEGylated Glucuronide-Monomethylauristatin E Linker for Antibody-Drug Conjugates. Mol Cancer Ther. 2017 Jan;16(1):116-123. [Content Brief]
- [6]. Poongavanam V, et al. Linker-Dependent Folding Rationalizes PROTAC Cell Permeability. J Med Chem. 2022 Oct 13;65(19):13029-13040. [Content Brief]
- [7]. Su Z, et al. Antibody-drug conjugates: Recent advances in linker chemistry. Acta Pharm Sin B. 2021 Dec;11(12):3889-3907. [Content Brief]
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PEG Linkers Related Products (2334)
Related Products (2334)
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Fmoc-NH-PEG4-CH2COOH
0 ImagesFmoc-NH-PEG4-CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-NH-PEG4-CH2COOH is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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Propargyl-PEG2-amine
0 ImagesPropargyl-PEG2-amine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG2-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG2-amine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Methyltetrazine-PEG4-maleimide
0 ImagesMethyltetrazine-PEG4-maleimide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Methyltetrazine-PEG4-maleimide is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.
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N-Boc-PEG2-bromide
0 ImagesN-Boc-PEG2-bromide is a PEG/Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs. N-Boc-PEG2-bromide is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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Azido-PEG10-amine
0 ImagesCat. No.: HY-140217CAS No.: 912849-73-1Azido-PEG10-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG10-amine 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.
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Fmoc-NH-PEG3-CH2CH2COOH
0 ImagesFmoc-NH-PEG3-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-NH-PEG3-CH2CH2COOH is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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Azido-PEG4-hydrazide
0 ImagesAzido-PEG4-hydrazide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG4-hydrazide 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.
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DBCO-S-S-PEG3-biotin
0 ImagesCat. No.: HY-140128CAS No.: 1430408-09-5
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Azido-PEG3-Val-Cit-PAB-PNP
0 ImagesAzido-PEG3-Val-Cit-PAB-PNP is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG3-Val-Cit-PAB-PNP is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG3-Val-Cit-PAB-PNP 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.
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NH2-PEG2-C2-Boc
0 ImagesNH2-PEG2-C2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. NH2-PEG2-C2-Boc is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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Propargyl-PEG1-acid
0 ImagesCat. No.: HY-130504CAS No.: 55683-37-9Propargyl-PEG1-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-CRBN PROTACs Ibrutinib(HY-10997)-based PROTAC 4 and PROTAC 5. PROTAC 5 causes the degradation of BTK and induces the degradation of CSK, LYN, and LAT2 at 10 μM. Propargyl-PEG1-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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NH2-PEG5-C2-NH-Boc
0 ImagesCat. No.: HY-W022240CAS No.: 189209-27-6Synonyms: PROTAC Linker 17
