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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Bis-PEG13-NHS ester
0 ImagesBis-PEG13-NHS ester is a PEG/Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs. Bis-PEG13-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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N3-PEG3-CH2COOH
0 ImagesSynonyms: PROTAC Linker 14N3-PEG3-CH2COOH (PROTAC Linker 14) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. N3-PEG3-CH2COOH 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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Biotin-PEG4-amino-t-Bu-DADPS-C3-alykne
0 ImagesCat. No.: HY-140928CAS No.: 2241685-22-1Biotin-PEG4-amino-t-Bu-DADPS-C3-alykne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Biotin-PEG4-amino-t-Bu-DADPS-C3-alykne 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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Mal-PEG4-acid
0 ImagesCat. No.: HY-126961CAS No.: 518044-41-2
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Boc-NH-PEG6-CH2CH2COOH
0 ImagesCat. No.: HY-W040244CAS No.: 882847-13-4Boc-NH-PEG6-CH2CH2COOH is a cleavable ADC linker used as a linker for antibody-drug conjugates (ADC). Boc-NH-PEG6-CH2CH2COOH is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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Azido-PEG5-azide
0 ImagesAzido-PEG5-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG5-azide 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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Propargyl-PEG2-acid
0 ImagesPropargyl-PEG2-acid is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG2-acid is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Propargyl-PEG2-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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Bromo-PEG5-Boc
0 ImagesCat. No.: HY-141366CAS No.: 1415800-38-2
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N-DBCO-N-bis(PEG2-C2-NHS ester)
0 ImagesCat. No.: HY-140585CAS No.: 2128735-29-3N-DBCO-N-bis(PEG2-C2-NHS ester) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. N-DBCO-N-bis(PEG2-C2-NHS ester) is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
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Mal-PEG24-NHS ester
0 ImagesCat. No.: HY-135819CAS No.: 2226733-37-3
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Propargyl-PEG4-acid
0 ImagesPropargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC50 of 200 nM in THP-1 cells. Propargyl-PEG4-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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Biotin-PEG3-SH
0 ImagesCat. No.: HY-132115CAS No.: 1244028-52-1
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Br-PEG4-C2-Boc
0 ImagesBr-PEG4-C2-Boc is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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NH2-PEG2-CH2-Boc
0 ImagesCat. No.: HY-42427CAS No.: 1948273-09-3
