1. Signaling Pathways
  2. PROTAC
  3. PROTAC Linkers

PROTAC Linkers

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.

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-130426
    Maleimido-tri(ethylene glycol)-propionic acid 518044-40-1 98.0%
    Maleimido-tri(ethylene glycol)-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Maleimido-tri(ethylene glycol)-propionic acid is used for the preparation of neolymphostin-based ADC precursors for site-specific cysteine mutant trastuzumab-A114C conjugation. Maleimido-tri(ethylene glycol)-propionic acid also can be used as a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Maleimido-tri(ethylene glycol)-propionic acid
  • HY-135927
    H2N-PEG2-CH2COOtBu 1122484-77-8
    H2N-PEG2-CH2COOtBu is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    H2N-PEG2-CH2COOtBu
  • HY-130175
    Fmoc-NH-PEG4-CH2COOH 437655-95-3 99.11%
    Fmoc-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.
    Fmoc-NH-PEG4-CH2COOH
  • HY-W040257
    NH2-PEG6-CH2CH2COOH 905954-28-1
    NH2-PEG6-CH2CH2COOH is a cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). NH2-PEG6-CH2CH2COOH is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    NH2-PEG6-CH2CH2COOH
  • HY-126963
    Mal-PEG6-acid 518044-42-3 ≥98.0%
    Mal-PEG6-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
    Mal-PEG6-acid
  • HY-140056
    Aminooxy-PEG1-propargyl 1895922-69-6
    Aminooxy-PEG1-propargyl is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Aminooxy-PEG1-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Aminooxy-PEG1-propargyl
  • HY-133292
    Thiol-PEG4-alcohol 90952-27-5 99.39%
    Thiol-PEG4-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Thiol-PEG4-alcohol
  • HY-W001958
    Monomethyl octanoate 3946-32-5 99.08%
    Monomethyl octanoate (Suberic acid monomethyl ester) is an ester product. Monomethyl octanoate is a PROTAC linker that can be used in the synthesis of PROTACs, DDD2 (HY-176261).
    Monomethyl octanoate
  • HY-W009030
    N-Fmoc-8-aminooctanoic acid 126631-93-4
    N-Fmoc-8-aminooctanoic acid can be used as a PROTAC linker in the synthesis of PROTACs. N-Fmoc-8-aminooctanoic acid is an alkane chain with terminal Fmoc-protected amine and carboxylic acid groups. The Fmoc group can be deprotected under basic condition to obtain the free amine which can be used for further conjugations. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond.
    N-Fmoc-8-aminooctanoic acid
  • HY-W105727
    9-Aminononanoic acid 1120-12-3
    9-Aminononanoic acid can be used as a PROTAC linker and other conjugation in the synthesis of PROTACs. 9-Aminononanoic acid is an alkane chain with terminal carboxlic acid and amine groups. The amino group (NH2) is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. The terminal carboxylic acid can react with primary amine groups of activated NHS ester to form a stable amide bond.
    9-Aminononanoic acid
  • HY-150910
    Brigatinib C 1197958-75-0 99.72%
    Brigatinib C is a linker, as a part of PROTAC Linker to target HJM-561 (HY-156698).
    Brigatinib C
  • HY-40144
    Azetidin-3-ol hydrochloride 18621-18-6 99.74%
    Azetidin-3-ol hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azetidin-3-ol hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthes PROTAC.
    Azetidin-3-ol hydrochloride
  • 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-130425
    Bromo-PEG1-acid 1393330-33-0 98.0%
    Bromo-PEG1-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
    Bromo-PEG1-acid
  • HY-130541
    Propargyl-PEG2-OH 7218-43-1 99.66%
    Propargyl-PEG2-OH is a PEG-based PROTAC linker can be used in the synthesis of Thalidomide-O-PEG2-propargyl (HY-126458). Propargyl-PEG2-OH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Propargyl-PEG2-OH
  • HY-130161
    m-PEG4-Br 110429-45-3 98.81%
    m-PEG4-Br is a cleavable ADC linker used in the synthesis of antibody-drug conjugate (ADC) for Trastuzumab (HY-P9907). m-PEG4-Br is placed distally from the monomethyl auristatin E (MMAE) payload to yield an ADC with altered hydrophilicity, antigen binding, and in vitro potency. m-PEG4-Br also can be used as a PROTAC linker that can be used in the synthesis of PROTACs.
    m-PEG4-Br
  • HY-128801
    NH2-PEG3-C1-Boc 189808-70-6 ≥98.0%
    NH2-PEG3-C1-Boc (PROTAC Linker 5) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
    NH2-PEG3-C1-Boc
  • HY-W022232
    Boc-NH-PEG5-CH2CH2COOH 1347750-78-0
    Boc-NH-PEG5-CH2CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.
    Boc-NH-PEG5-CH2CH2COOH
  • HY-126949
    Aminooxy-PEG3-azide 1306615-51-9
    Aminooxy-PEG3-azide is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Aminooxy-C2-PEG3-azide is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Aminooxy-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.
    Aminooxy-PEG3-azide
  • HY-140617
    DNP-PEG3-azide 951671-87-7 99.18%
    DNP-PEG3-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. DNP-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.
    DNP-PEG3-azide

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