2. PROTAC
  3. Target Protein Ligand-Linker Conjugates

Target Protein Ligand-Linker Conjugates

Target Protein Ligand-Linker Conjugate incorporates a ligand for the target protein and a linker. When binding to an E3 ligase ligand, the conjugate will be a PROTAC with ability to induce ubiquitylation and subsequent degradation the protein of interest.

Target proteins are usually proteins whose overexpression or accumulation may play important roles in the progress of diseases. Numbers of PROTACs have been developed to degrade kinases, transcription factors, epigenetic tools and E3 ligase themselves.

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.

Target Protein Ligand-Linker Conjugates Related Products (36):

Cat. No. Product Name Effect Purity
  • HY-130499
    ERRα Ligand-Linker Conjugates 1 98.78%
    ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα), and a PROTAC linker, which recruit E3 ligases MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader[1].
  • HY-131230
    Desmorpholinyl Quizartinib-PEG2-COOH
    Desmorpholinyl Quizartinib-PEG2-COOH incorporates a ligand for FLT-3, and a PEG-based PROTAC linker. Desmorpholinyl Quizartinib-PEG2-COOH can be used in the synthesis of PROTAC FLT-3 degrader 1 (HY-114323). PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM[1].
  • HY-147090
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH 99.06%
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) incorporates a ligand for EZH2, and a PROTAC linker, which recruit E3 ligases. Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) can be used for the research of lymphoma[1].
  • HY-49382
    Fluocinolone acetonide 3-benzylaniline
    Fluocinolone acetonide 3-benzylaniline (Precursor Example 1) is a glucocorticoid receptor agonist-linker conjugate, which can be used for the synthesis of anti-CD40 antibody-drug conjugates (ADCs)[1].
  • HY-130991
    K-Ras ligand-Linker Conjugate 6
    K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells[1].
  • HY-172266
    FKBP12 Ligand-Linker Conjugate 2
    FKBP12 Ligand-Linker Conjugate 2 is a conjugate of the FKBP12 target protein ligand and a linker, and it can be used for the synthesis of FKBP12 PROTAC FM4 (HY-172265)[1].
  • HY-173137
    KDM4 Ligand-Linker Conjugate 1
    KDM4 Ligand-Linker Conjugate 1 is a conjugate of a KDM4 target protein ligand and a linker, and can be used for the synthesis of PROTAC KDM4 degrader-1 (HY-173135)[1].
  • HY-176038
    MS1262-C3-amide-C10-amine
    MS1262-C3-amide-C10-amine is a E3 Ligase Ligand-Linker Conjugates. MS1262-C3-amide-C10-amine incorporates a GLP ligand for the E3 ligase SPOP (HY-176036), and a PROTAC linker (HY-176037). MS1262-C3-amide-C10-amine can be used to design PROTACs such as MS479 (HY-176035)[1].
  • HY-171159
    MC-Val-Cit-PAB-Sunitinib
    MC-Val-Cit-PAB-Sunitinib is the conjugate of a payload Sunitinib (HY-10255A) and a linker. MC-Val-Cit-PAB-Sunitinib can be used for synthesis of HR97-Sunitinib[1].
  • HY-169490
    Target Protein Ligand-Linker Conjugates 4
    Target Protein Ligand-Linker Conjugates 4 is a conjugate generated by linking a target protein ligand (HY-44824) to a linker (HY-169489). Target Protein Ligand-Linker Conjugates 4 can be used in the synthesis of PROTACs (e.g. PROTAC SMARCA2 degrader-21 (HY-169272))[1].
  • HY-170987
    FKBP12 Ligand-Linker Conjugate 1
    FKBP12 Ligand-Linker Conjugate 1 is the conjugate composed of a target protein ligand for FKBP12 and a linker. FKBP12 Ligand-Linker Conjugate 1 can be used for synthesis of PROTAC degrader MC-25B (HY-170983)[1].
  • HY-44148
    FAK ligand-Linker Conjugate 1 98.91%
    FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation[1].
  • HY-147050
    Ahx-DM1
    Ahx-DM1 (compound 2A) is a conjugate of protein/peptide which can be combined with a therapeutic, diagnostic or labelling agent[1].
  • HY-172067
    ER ligand-9
    ER ligand-9 is a conjugate of an estrogen receptor (Estrogen Receptor/ERR) and a linker, which can be used to synthesize PROTAC ERD-1233 (HY-169367)[1].
  • HY-131386A
    BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride
    BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1?(HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM[1].
  • HY-170854
    RET Ligand-Linker Conjugate-1
    RET Ligand-Linker Conjugate-1 is the conjugate composed of a RET ligand and a linker. RET Ligand-Linker Conjugate-1 can be used for synthesis of QZ2135 (HY-170852)[1].
  • HY-163019
    EN884
    EN884 is a BRD4 degrader via a SKP1- and proteasome-dependent manner. EN884 can be used in synthetic proteolysis targeting chimeras (PROTACs)[1].
  • HY-168458
    RNA recruiter-linker 1
    RNA recruiter-linker 1 is the RNA ligand-linker part of RNAse L RIBOTAC (HY-168455), an RNA-degrading chimera which binds to a four-way RNA helix called SL5 in the 5’ UTR of the SARS-CoV-2 RNA genome and inhibits the virus replication in lung epithelial carcinoma cells. RNA recruiter-linker 1 can be utilized in the synthesis of RIBOTAC[1].
  • HY-141486
    (Rac)-PROTAC PARP/EGFR ligand 1
    (Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP[1].
  • HY-168682
    Adamantane-Butyl alcohol
    Adamantane-Butyl alcohol is a selective and persistent degrader targeting the CDK8-cyclin C complex. Adamantane-Butyl alcohol is the linker for LL-K8-22 (PROTAC CDK8-cyclin C, HY-149209) and HyT[1].