1. Signaling Pathways
  2. PROTAC
  3. Target Protein Ligand-Linker Conjugate

Target Protein Ligand-Linker Conjugate

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 Conjugate Related Products (8):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-44148
    FAK ligand-Linker Conjugate 1 2307461-45-4 98.28%
    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.
    FAK ligand-Linker Conjugate 1
  • HY-130499
    ERRα Ligand-Linker Conjugates 1
    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.
    ERRα Ligand-Linker Conjugates 1
  • HY-130822
    K-Ras ligand-Linker Conjugate 4 2378261-83-5
    K-Ras ligand-Linker Conjugate 4 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 4 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.
    K-Ras ligand-Linker Conjugate 4
  • HY-131230
    Desmorpholinyl Quizartinib-PEG2-COOH 2292116-14-2
    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 .
    Desmorpholinyl Quizartinib-PEG2-COOH
  • HY-130823
    K-Ras ligand-Linker Conjugate 5 2378261-85-7
    K-Ras ligand-Linker Conjugate 5 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 5 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.
    K-Ras ligand-Linker Conjugate 5
  • HY-130991
    K-Ras ligand-Linker Conjugate 6 2378261-89-1
    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.
    K-Ras ligand-Linker Conjugate 6
  • HY-129775
    K-Ras ligand-Linker Conjugate 1
    K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 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.
    K-Ras ligand-Linker Conjugate 1
  • HY-130707
    K-Ras ligand-Linker Conjugate 3 2378261-87-9
    K-Ras ligand-Linker Conjugate 3 (Compound 001371) 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 3 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.
    K-Ras ligand-Linker Conjugate 3
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