PROTAC Degrader

PROTAC degraders recruit an E3 ubiquitin ligase to a target protein so that the proteasome degrades it. Each proteolysis-targeting chimera (PROTAC) links a target-binding ligand to an E3 ligase ligand through a chemical linker. The approach was first described in 2001, and later work showed that small-molecule PROTACs can act catalytically, removing several target copies per molecule. Examples include the bromodomain and extra-terminal (BET) degraders dBET1, MZ1 and ARV-771, and the estrogen receptor degrader ERD-308. Degraders of anti-apoptotic proteins, such as PROTAC Mcl1 degrader-1, are also listed.

9 Items

  • PROTAC ERα Degrader-1
    Cat. No.
    A24001

    PROTAC ERα Degrader-1

    PROTAC ERα Degrader-1 is a bifunctional molecule composed of an estrogen receptor-alpha (ERα) ligand, a linker, and an E3 ubiquitin ligase-recruiting moiety. Derived from compound P1 in patent WO2017201449A1, it functions as a targeted protein degrader that promotes ubiquitination and subsequent proteasomal degradation of ERα. PROTAC ERα Degrader-1 represents a novel approach for modulating estrogen receptor signaling in hormone-dependent cancers.

    1 mg
    $288.00
    5 mg
    $864.00
    All 4 sizes
  • PROTAC FKBP Degrader-3
    Cat. No.
    A24845

    PROTAC FKBP Degrader-3

    PROTAC FKBP Degrader-3 is a proteolysis-targeting chimera that utilizes a FKBP ligand binding group and a von Hippel-Lindau (VHL) E3 ligase recruiting moiety linked by a flexible linker. This compound effectively induces the degradation of FKBP12, demonstrating potent biological activity in targeted protein degradation. It is primarily used in research applications related to protein homeostasis, cellular signaling mechanisms, and therapeutic development strategies for modulating protein levels.

    1 mg
    $395.00
    5 mg
    $815.00
    All 6 sizes
  • Thalidomide-5-CH2-NH2 hydrochloride
    Cat. No.
    A30815

    Thalidomide-5-CH2-NH2 hydrochloride

    Thalidomide-5-CH2-NH2 hydrochloride serves as an E3 ligase ligand targeting cereblon (CRBN) for the development of PROTACs (Proteolysis Targeting Chimeras). This compound facilitates the selective recruitment of CRBN to ubiquitin-proteasome pathways, promoting the degradation of specific target proteins. Its application is pivotal in targeted protein degradation studies and drug discovery processes aimed at modulating protein levels in various biological contexts.

    25 mg
    $75.00
    50 mg
    $115.00
    All 3 sizes
  • PROTAC BRD4 Degrader-3
    Cat. No.
    A40542

    PROTAC BRD4 Degrader-3

    PROTAC BRD4 Degrader-3 is a targeted protein degradation compound that operates through the recruitment of von Hippel-Lindau (VHL) ligands to promote the ubiquitination and subsequent proteasomal degradation of the BRD4 protein. This compound demonstrates significant efficacy in downregulating BRD4, a key regulator in various cancers and inflammatory diseases. Research applications for PROTAC BRD4 Degrader-3 include the investigation of therapeutic strategies for cancer treatment and exploring the role of BRD4 in gene expression and signaling pathways.

    Out of stock

    All 3 sizes
  • EZH2 ligand-3
    Cat. No.
    A57758

    EZH2 ligand-3

    EZH2 ligand-3 functions as a ligand targeting the Enhancer of Zeste Homolog 2 (EZH2) protein. This compound plays a crucial role in the synthesis of PROTAC EZH2 Degrader-35, facilitating the selective degradation of EZH2 in cellular models. It is valuable for research applications focused on epigenetic regulation and targeted protein degradation strategies.

    Out of stock

    All 3 sizes
  • KRAS ligand 5
    Cat. No.
    A63665

    KRAS ligand 5

    KRAS ligand 5 is a target protein ligand utilized in the development of PROTAC K-Ras Degrader-3. This compound specifically facilitates the degradation of KRAS mutated proteins, making it a vital tool for research focused on targeted protein degradation. It is particularly relevant in studies addressing KRAS-related oncogenesis and potential therapeutic applications in cancer treatment.

    25 mg
    $2,000.00
    50 mg
    $2,630.00
    All 3 sizes
  • HPK1-IN-47
    Cat. No.
    A65774

    HPK1-IN-47

    HPK1-IN-47 is a selective HPK1 ligand designed for the synthesis of PROTACs, specifically serving as a precursor for PROTAC HPK1 Degrader-2. It exhibits potential in targeting HPK1, which plays a significant role in various HPK1-mediated diseases, particularly cancer. This compound is valuable for research applications focused on elucidating the therapeutic potential of HPK1 degradation in cancer treatment.

    Out of stock

    All 3 sizes
  • tri-GalNAc biotin
    Cat. No.
    A81374

    tri-GalNAc biotin

    tri-GalNAc biotin is a biotinylated ligand that targets the asialoglycoprotein receptor (ASGPR). It facilitates the cellular uptake of neutravidin, directing it to lysosomes for degradation. This compound is valuable for research related to lysosome-targeting chimeras (LYTAC), enhancing the understanding of lysosomal pathways and targeted delivery systems in therapeutic applications.

    1 mg
    $480.00
    5 mg
    $1,230.00
    All 3 sizes
  • F1-RIBOTAC
    Cat. No.
    A84580

    F1-RIBOTAC

    F1-RIBOTAC is a ribonuclease-targeting chimera (RIBOTAC) that functions by enhancing the activity of RNase L to selectively degrade QSOX1-a mRNA. This targeted approach results in a significant reduction in QSOX1-a expression, making F1-RIBOTAC a valuable tool for cancer research. Its design integrates RNA ligands and RNase L ligands, providing a novel modality for studying RNA degradation pathways in malignant cells.

    Out of stock

    All 3 sizes

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