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Target Protein Ligand-Linker Conjugates

Target protein ligand-linker conjugates join a target-binding ligand to a linker for degrader synthesis. In a proteolysis-targeting chimera (PROTAC), this half binds the protein of interest, while the other half recruits an E3 ubiquitin ligase. The free linker end, often an amine, carboxylic acid or piperazine, is coupled to a ligase ligand in the final step. One conjugate can thus be paired with cereblon or von Hippel-Lindau (VHL) ligands to compare degraders for the same target. Kinase examples include FLT3 Ligand-Linker Conjugate 1 for FMS-like tyrosine kinase 3 (FLT3) and Desmorpholinyl Quizartinib-PEG2-COOH, which carries a polyethylene glycol (PEG) spacer. Others address the GTPase Kirsten rat sarcoma viral oncogene homolog (KRAS), as in K-Ras ligand-Linker Conjugate 6.

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  • BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride
    Cat. No.
    A84634
    CAS No.
    2691796-83-3

    BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride

    BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride is a compound designed for the synthesis of Protein Targeting Chimeras (PROTACs) targeting the PD-1/PD-L1 immune checkpoint. It features a ligand that facilitates binding to PD-1/PD-L1 and includes a PROTAC linker for degradation of target proteins. This compound can be utilized in the development of PROTAC PD-1/PD-L1 degrader-1, which effectively inhibits PD-1/PD-L1 interactions with an IC50 of 39.2 nM, making it a valuable tool for cancer immunotherapy research.

    In stock View Details
    1 mg
    $90.00
    5 mg
    $235.00
    All 6 sizes

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