E3 Ligase Ligand-Linker Conjugate

E3 ligase ligand-linker conjugates combine a ligase ligand and a linker in one ready-to-couple PROTAC building block. Attaching such a conjugate to a target-protein ligand completes a proteolysis-targeting chimera (PROTAC) in a final coupling step. Many conjugates in this category carry a cereblon ligand derived from pomalidomide, lenalidomide or thalidomide, for example Pomalidomide-PEG4-C2-NH2 and Lenalidomide-C5-NH2. Others are built on von Hippel-Lindau (VHL) ligands, such as (S,R,S)-AHPC-C3-NH2 and VH032-thiol-C6-NH2. Terminal amines, acids and azides allow attachment by amide coupling or click chemistry.

5 Items

  • Pomalidomide 5'-pip-acid
    Cat. No.
    A79941

    Pomalidomide 5'-pip-acid

    Pomalidomide 5'-pip-acid is a molecular glue that functions as a dual-target PROTAC degrader, specifically targeting CBP/p300 and BRD4. It exhibits significant antiproliferative activity against cancer cells, with an IC50 value of 2.73 nM. This compound is particularly relevant for research in prostate and colorectal cancer, offering a valuable tool for investigating targeted degradation pathways in oncogenesis.

    5 mg
    $25.00
    10 mg
    $45.00
    All 5 sizes
  • (E)-JP-2-196 TFA
    Cat. No.
    A79962

    (E)-JP-2-196 TFA

    (E)-JP-2-196 TFA is a molecular glue handle that specifically interacts with E3-ubiquitin ligases, including RNF126, LRSAM1, RNF40, MID2, and RNF14, in vitro. This compound facilitates the synthesis of molecular glue degraders, making it a valuable tool for studying targeted protein degradation and investigating ubiquitin-proteasome system pathways. Its unique binding capabilities lend themselves to various research applications in protein modulation and therapeutic development.

    5 mg
    $65.00
    10 mg
    $110.00
    All 5 sizes
  • Azido-PEG2-VHL
    Cat. No.
    A80104

    Azido-PEG2-VHL

    Azido-PEG2-VHL is a multikinase degrader that serves as a versatile building block for the synthesis of PROTACs (proteolysis-targeting chimeras). This compound features an azide functionality, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) and strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with alkyne-functionalized molecules, such as those containing DBCO or BCN groups. Its application in targeted protein degradation makes it a valuable tool in chemical biology research.

    Out of stock

    All 3 sizes
  • Lenalidomide 4'-alkyl-C3-azide
    Cat. No.
    A80123

    Lenalidomide 4'-alkyl-C3-azide

    Lenalidomide 4'-alkyl-C3-azide is a click chemical reagent that incorporates an azide group into lenalidomide, facilitating the synthesis of PROTACs. As an orally active immunomodulator, lenalidomide acts as a ligand for the ubiquitin E3 ligase cereblon (CRBN). This compound is capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) reactions with alkyne-containing molecules, as well as strain-promoted azide-alkyne cycloaddition (SPAAC) with DBCO or BCN groups, thereby enabling versatile modifications in chemical biology research.

    Out of stock

    All 3 sizes
  • E3 Ligase Ligand-linker Conjugate 122
    Cat. No.
    A80355

    E3 Ligase Ligand-linker Conjugate 122

    E3 Ligase Ligand-linker Conjugate 122 is a specialized reagent designed for the synthesis of PROTAC degraders, specifically NR-11c. It combines an E3 ligase ligand with a linker, facilitating targeted protein degradation through the ubiquitin-proteasome system. This compound is essential for studies focused on E3 ligase-mediated degradation pathways and therapeutic applications in targeted cancer therapies.

    Out of stock

    All 3 sizes

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