1. Click Chemistry
  2. PROTAC Synthesis

PROTAC Synthesis

PROTAC molecules are generally composed of three parts: ligand for target protein, linker and ligand for E3 ligase. “Click chemistry” reactions provide an accessible and tunable strategy for the selection of synthetic linkers and lay a solid foundation for the development of a diverse library of PROTACs in biomedical research. The copper-catalyzed reaction is typically high yielding, requiring stoichiometric quantities of each component and boasts excellent functional group compatibility under mild reaction conditions. This approach would allow for the parallel synthesis of libraries of PROTACs provided the necessary azides and alkynes could be prepared. For example, click chemistry was utilized to prepare a library of PROTACs based on entinostat a class I histone deacetylase (HDAC) inhibitor in clinical trials. Recently, an advanced PROTAC technology was developed, namely CLIPTAC (in-cell click-formed proteolysis-targeting chimeras), with two precursor components combined by bioorthogonal “click” reaction.

PROTAC Synthesis (765):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-118411
    5-Ethynyl-2'-deoxyuridine 61135-33-9 99.77%
    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
    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-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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    L-Azidohomoalanine hydrochloride
  • 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    Biotin-PEG3-azide
  • 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    Amino-PEG3-C2-Azido
  • 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-138749
    Biotin alkyne 773888-45-2 98.03%
    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-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-W016735
    Azido-PEG3-alcohol 86520-52-7 98.17%
    Azido-PEG3-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Azido-PEG3-alcohol 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    Azido-PEG3-alcohol
  • HY-140922
    Biotin-PEG4-alkyne 1458576-00-5 98.88%
    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
  • HY-126885
    DBCO-PEG5-NHS ester 2144395-59-3
    DBCO-PEG5-NHS ester is a PEG/Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs. DBCO-PEG5-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG5-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-PEG5-NHS ester
  • HY-108374
    4-Azidobutylamine 88192-20-5 ≥98.0%
    4-Azidobutylamine is a PROTAC linker, which refers to the alkyl chain composition. 4-Azidobutylamine can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins. 4-Azidobutylamine 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    4-Azidobutylamine
  • HY-138461
    Azido-PEG1 1517-05-1 99.95%
    Azido-PEG1 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG1 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    Azido-PEG1
  • HY-140459
    2-((Azido-PEG8-carbamoyl)methoxy)acetic acid 846549-37-9 ≥98.0%
    2-((Azido-PEG8-carbamoyl)methoxy)acetic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. 2-((Azido-PEG8-carbamoyl)methoxy)acetic acid 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    2-((Azido-PEG8-carbamoyl)methoxy)acetic acid
  • HY-69220
    7-Octynoic acid 10297-09-3 ≥98.0%
    7-Octynoic acid (compound 42) is a PROTAC linker and can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins. 7-Octynoic 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.
    7-Octynoic acid
  • HY-140910
    Biotin-PEG4-azide 1309649-57-7 99.75%
    Biotin-PEG4-azide is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Biotin-PEG4-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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    Biotin-PEG4-azide
  • HY-140452
    Azido-PEG2-C2-acid 1312309-63-9
    Azido-PEG2-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG2-C2-acid 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    Azido-PEG2-C2-acid
  • HY-108368
    Azido-PEG2-CH2COOH 882518-90-3
    Azido-PEG2-CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Azido-PEG2-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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    Azido-PEG2-CH2COOH
  • HY-128834
    N3-PEG4-C2-NH2 951671-92-4 ≥98.0%
    N3-PEG4-C2-NH2 (PROTAC Linker 20) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. N3-PEG4-C2-NH2 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    N3-PEG4-C2-NH2
  • HY-130653
    Azido-PEG4-C2-acid 1257063-35-6 ≥98.0%
    Azido-PEG4-C2-acid a PEG-based PROTAC linker can be used in the synthesis of vRucaparib-TP4. Azido-PEG4-C2-acid is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG4-C2-acid 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    Azido-PEG4-C2-acid