2. Signaling Pathways
  3. PROTAC
  4. PROTAC Linkers

PROTAC Linkers

PROTAC Linkers

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PROTACs (Proteolysis Targeting Chimeric Molecules) are heterobifunctional protein degraders and promising targeted therapeutics candidates for cancer. The PROTAC linker connects two functional motifs of a PROTAC, a target protein binder and an E3 ligase recruiter.

The linker plays an important role in a PROTAC. The features of the linker (type, length, attachment position) can affect the formation of ligase:PROTAC:target ternary complex, resulting in influencing the efficient ubiquitination of the target protein and its ultimate degradation. The optimal lengths of the PROTAC linkers are reported varying from 12-carbon to over 20-carbon, and the commonly used linkers in the development of PROTACs are PEGs, Alkyl-Chain and Alkyl/ether.

PROTAC Linkers Isoform Specific Products:

PROTAC Linkers Isoform Comparison
Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-118411
    5-Ethynyl-2'-deoxyuridine 61135-33-9 99.78%
    5-Ethynyl-2'-deoxyuridine (EdU), a thymidine analogue, is incorporated into cellular DNA during DNA replication and the subsequent reaction of EdU with a fluorescent azide in a “Click” reaction. EdU staining is a fast, sensitive and reproducible method to study cell proliferation. 5-Ethynyl-2'-deoxyuridine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. 5-Ethynyl-2'-deoxyuridine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    5-Ethynyl-2'-deoxyuridine
  • HY-140272
    DBCO-PEG4-NHS ester 1427004-19-0 98.66%
    DBCO-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. DBCO-PEG4-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.
    DBCO-PEG4-NHS ester
  • HY-W008574
    TGN-020 51987-99-6 99.52%
    TGN-020 is a selective Aquaporin 4 (AQP4) inhibitor with an IC50 of 3.1 μM. TGN-020 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.TGN-020 alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats.
    TGN-020
  • HY-40171
    NH2-C2-NH-Boc 57260-73-8 99.97%
    NH2-C2-NH-Boc (PROTAC Linker 22) is a alkyl chain-based PROTAC linker can be used in the synthesis of PROTACs.
    NH2-C2-NH-Boc
  • HY-140346A
    L-Azidohomoalanine hydrochloride 942518-29-8 99.76%
    L-Azidohomoalanine hydrochloride is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. L-Azidohomoalanine (hydrochloride) 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.
    L-Azidohomoalanine hydrochloride
  • HY-69260
    tert-Butyl 4-formylpiperidine-1-carboxylate 137076-22-3 99.54%
    tert-Butyl 4-formylpiperidine-1-carboxylate is the linker of PROTAC BRM/BRG1 degrader-3 (HY-168251).
    tert-Butyl 4-formylpiperidine-1-carboxylate
  • HY-43048
    2-(2-((6-Chlorohexyl)oxy)ethoxy)acetic acid 2231744-57-1
    2-(2-((6-Chlorohexyl)oxy)ethoxy)acetic acid is a PROTACT linker in PROTAC SMARCA2/4-degrader-34 (HY-169279).
    2-(2-((6-Chlorohexyl)oxy)ethoxy)acetic acid
  • HY-W248248
    tert-Butyl 9-aminononanoate 134857-22-0 ≥98.0%
    tert-Butyl 9-aminononanoate is a PROTAC linker. tert-Butyl 9-aminononanoate can be used in synthesis PROTAC sEH-degrader-1 (HY-159494).
    tert-Butyl 9-aminononanoate
  • HY-W021401
    Amino-PEG3-C2-Azido 134179-38-7 99.67%
    Amino-PEG3-C2-Azido is a PEG-based PROTAC linker can be used in the synthesis of the PARP1 degrader iRucaparib-TP3 (HY-130645). Amino-PEG3-C2-Azido 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.
    Amino-PEG3-C2-Azido
  • HY-130143
    Biotin-PEG3-azide 875770-34-6
    Biotin-PEG3-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Biotin-PEG3-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.
    Biotin-PEG3-azide
  • HY-W040304
    Alkynyl Palmitic Acid 99208-90-9
    Alkynyl Palmitic Acid (Alk-C16) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. Alkynyl Palmitic 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.
    Alkynyl Palmitic Acid
  • HY-140345
    L-Homopropargylglycine 98891-36-2 ≥98.0%
    L-Homopropargylglycine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. L-homopropargylglycine is an amino acid analog of methionine containing an alkyne moiety that can undergo a classic click chemical reaction with azide containing Alexa Fluor.
    L-Homopropargylglycine
  • HY-130458
    EGNHS 70539-42-3
    EGNHS is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
    EGNHS
  • HY-140213
    Azido-PEG2-C2-amine 166388-57-4 99.85%
    Azido-PEG2-C2-amine (N3-PEG2-CH2CH2NH2) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG2-C2-amine is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG2-C2-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.
    Azido-PEG2-C2-amine
  • HY-W000434
    Fmoc-NH-PEG4-CH2CH2COOH 557756-85-1 99.92%
    Fmoc-NH-PEG4-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-NH-PEG4-CH2CH2COOH is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Fmoc-NH-PEG4-CH2CH2COOH
  • HY-136159
    3-Mercaptopropionic acid NHS ester 117235-10-6
    3-Mercaptopropanyl-N-hydroxysuccinimide ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
    3-Mercaptopropionic acid NHS ester
  • HY-141128
    Ac4GalNAz 653600-56-7 99.71%
    Ac4GalNAz is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. Ac4GalNAz 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.
    Ac4GalNAz
  • HY-30105
    N-Boc-piperazine 57260-71-6 99.97%
    N-Boc-piperazine is a Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183).
    N-Boc-piperazine
  • HY-138749
    Biotin alkyne 773888-45-2 98.60%
    Biotin alkyne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Biotin alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Biotin alkyne
  • HY-140922
    Biotin-PEG4-alkyne 1458576-00-5 99.09%
    Biotin-PEG4-alkyne is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Biotin-PEG4-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Biotin-PEG4-alkyne
PROTAC Linkers Isoform Comparison

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