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-W013381
    10-Bromodecanoic acid 50530-12-6 ≥98.0%
    10-Bromodecanoic acid (Decanoic acid, 10-bromo-) is a linker that can be used in the synthesis of PROTACs, such as PROTAC KDM4 degrader-1 (HY-173135).
    10-Bromodecanoic acid
  • HY-W089232
    Boc-10-Aminodecanoic acid 173606-50-3
    Boc-10-Aminodecanoic acid can be used as a PROTAC linker in the synthesis of PROTACs and other conjugation applications. Boc-10-Aminodecanoic acid is an alkane chain with terminal carboxlic acid and Boc-protected amino groups. 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. The Boc group can be deprotected under mild acidic conditions to form the free amine.
    Boc-10-Aminodecanoic acid
  • HY-130856
    Mal-amido-PEG9-acid 2112731-43-6 99.54%
    Mal-amido-PEG9-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Mal-amido-PEG9-acid
  • HY-133407
    β-Estradiol-6-one 6-(O-carboxymethyloxime) 35048-47-6 99.67%
    β-Estradiol-6-one 6-(O-carboxymethyloxime) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
    β-Estradiol-6-one 6-(O-carboxymethyloxime)
  • HY-140894
    Biotin-PEG8-alcohol 2182601-20-1 99.30%
    Biotin-PEG8-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Biotin-PEG8-alcohol
  • HY-W459522
    7-Bromohept-1-yne 81216-14-0 99.71%
    7-Bromohept-1-yne is a PROTAC linker that can be used to synthesize AK-1690 (HY-169179).
    7-Bromohept-1-yne
  • HY-47373
    Folate-PEG3-C2-acid
    Folate-PEG3-C2-acid is the acid fragment of Folate-PEG3-NHS ester (HY-133493), which belongs to the PEG-type PROTAC linker and is used to synthesize PROTAC molecules.
    Folate-PEG3-C2-acid
  • HY-140646
    PEG-bis-amine (MW 2000) 24991-53-5 99.39%
    PEG-bis-amine (Poly(ethylene glycol)-bis-amine) (MW 2000) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    PEG-bis-amine (MW 2000)
  • HY-156383
    SCO-PEG3-NHS 2141976-25-0
    SCO-PEG3-NHS is a PEG linker with a terminal imine(NH) group. SCO-PEG3-NHS is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
    SCO-PEG3-NHS
  • HY-A0102
    AMCA 701-54-2 98.0%
    AMCA (4-(Aminomethyl)-1-cyclohexanecarboxylic acid) is a PROTAC linker. AMCA can be used to synthesize the PROTAC molecule YB-3–17 (HY-170405).
    AMCA
  • HY-135923
    Cbz-NH-PEG2-CH2COOH 165454-06-8 99.70%
    Cbz-NH-PEG2-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Cbz-NH-PEG2-CH2COOH
  • HY-W131541
    N-Boc-undecane-1,11-diamine 937367-26-5
    tert-Butyl (11-aminoundecyl)carbamate is an alkane chain with terminal amine and Boc-protected amino groups. tert-Butyl (11-aminoundecyl)carbamate can be used as a PROTAC linker in the synthesis of PROTACs and other conjugation applications. Amine group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. The Boc group can be deprotected under mild acidic conditions to form the free amine.
    N-Boc-undecane-1,11-diamine
  • HY-43538
    5-Bromopentanoyl chloride 4509-90-4 98.63%
    5-Bromopentanoyl chloride is a PROTAC linker in PROTAC ATR degrader-2 (HY-161615), and can be used for synthesis of PROTACs.
    5-Bromopentanoyl chloride
  • HY-130985
    9-Decyn-1-ol 17643-36-6
    9-Decyn-1-ol is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. 9-Decyn-1-ol can be used to conjugate GDC-0068 with Lenalidomide to generate INY-03-041. INY-03-041 is a potent, highly selective and PROTAC-based pan-Akt degrader. INY-03-041 inhibits Akt1, Akt2 and Akt3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively. 9-Decyn-1-ol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    9-Decyn-1-ol
  • HY-120430
    HO-PEG14-OH 1189112-05-7 98.0%
    HO-PEG14-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    HO-PEG14-OH
  • HY-130524
    Amino-PEG4-CH2COOH 195071-49-9 ≥98.0%
    Amino-PEG4-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Amino-PEG4-CH2COOH is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    Amino-PEG4-CH2COOH
  • HY-133493
    Folate-PEG3-NHS ester
    Folate-PEG3-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Folate-PEG3-NHS ester
  • HY-138380
    Mal-PEG4-C2-NH2 TFA 2512227-13-1 98.60%
    Mal-PEG4-C2-NH2 TFA is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Mal-PEG4-C2-NH2 TFA
  • HY-126958
    Biotin-PEG2-acid 1365655-89-5
    Biotin-PEG2-acid is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Biotin-PEG2-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
    Biotin-PEG2-acid
  • HY-140408
    Bis-aminooxy-PEG2 98627-71-5
    Bis-aminooxy-PEG2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Bis-aminooxy-PEG2
PROTAC Linkers Isoform Comparison

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