Ligand for Target Protein for PROTAC

Ligands for target proteins in PROTAC design bind the protein that a degrader is meant to remove. A proteolysis-targeting chimera (PROTAC) joins such a ligand to an E3 ubiquitin ligase ligand through a linker, so that the ligase ubiquitinates the bound target. Most entries are known inhibitors or receptor ligands modified with an attachment point, such as an aldehyde, amine, carboxylic acid or alkyne group. Dasatinib carbaldehyde and Imatinib carbaldehyde are aldehyde-bearing analogs of two kinase inhibitors. BI-4464 binds protein tyrosine kinase 2 (PTK2), also called focal adhesion kinase (FAK), and SirReal1-O-propargyl carries a propargyl handle on a sirtuin 2 (SIRT2) ligand. Receptor ligands in the list include Estrone-N-O-C1-amido and AP1867-2-(carboxymethoxy), which binds FK506-binding proteins.

Items 76-100 of 156

  • 7α,25-Dihydroxycholesterol intermediate-1
    Cat. No.
    A60236

    7α,25-Dihydroxycholesterol intermediate-1

    7α,25-Dihydroxycholesterol intermediate-1 is a crucial synthetic intermediate in the production of 7α,25-Dihydroxycholesterol. This compound functions as a ligand for the orphan G protein-coupled receptor EBI2 (GPR183), playing a significant role in immune system regulation and cellular signaling pathways. Its applications extend to the development of PROTACs, enabling targeted protein degradation in research and therapeutic contexts.

    Out of stock

    All 3 sizes
  • STING ligand-3
    Cat. No.
    A65578

    STING ligand-3

    STING ligand-3 functions as a ligand for the target protein, enabling the control of PROTAC activity. This compound plays a critical role in the synthesis of anti-inflammatory agents, specifically Anti-inflammatory agent 70. Its application in chemical research can facilitate advancements in understanding inflammatory pathways and developing therapeutic strategies.

    5 mg
    $170.00
    10 mg
    $290.00
    All 5 sizes
  • HPK1 ligand-Linker Conjugate 1
    Cat. No.
    A65763

    HPK1 ligand-Linker Conjugate 1

    HPK1 ligand-Linker Conjugate 1 is a synthesized ligand-linker conjugate designed for the development of PROTACs targeting HPK1. This compound serves as a critical component in the synthesis of PROTAC HPK1 Degrader-5, which exhibits significant anti-tumor activity and is characterized by its potency and oral bioavailability. Its applications extend to cell signaling research and targeted protein degradation strategies in cancer therapy studies.

    Out of stock

    All 3 sizes
  • PD0325901-O-C2-dioxolane
    Cat. No.
    A65809

    PD0325901-O-C2-dioxolane

    PD0325901-O-C2-dioxolane is a derivative of the MEK inhibitor PD0325901, designed as a ligand for targeted protein degradation in conjunction with VHL or CRBN E3 ligases. This compound facilitates the synthesis of MEK1/2 degraders, enabling the selective degradation of MEK proteins in experimental studies. Its application in research provides critical insights into MEK-related signaling pathways and their role in various diseases, particularly in cancer biology.

    1 mg
    $80.00
    5 mg
    $180.00
    All 6 sizes
  • MEK ligand-2
    Cat. No.
    A65824

    MEK ligand-2

    MEK ligand-2 is a ligand specifically designed for PROTAC applications targeting MEK1 and MEK2 proteins. This compound serves as a vital component for the development of the MS934 PROTAC, facilitating the degradation of MEK1 and MEK2 via a VHL-recruiting mechanism. It plays a crucial role in research aimed at understanding the regulation of MAPK signaling pathways and potential therapeutic strategies in cancer biology.

    Out of stock

    All 3 sizes
  • PROTAC SOS1 ligand 1
    Cat. No.
    A65864

    PROTAC SOS1 ligand 1

    PROTAC SOS1 ligand 1 is a high-affinity ligand for the SOS1 protein, facilitating targeted protein degradation through PROTAC technology. This compound is instrumental in the development of therapeutic strategies by enabling the selective modulation of SOS1, which plays a pivotal role in various oncogenic signaling pathways. Researchers can utilize this reagent in studies focused on cancer biology and drug discovery, particularly in exploring novel approaches to target and degrade specific proteins associated with tumor progression.

    Out of stock

    All 3 sizes
  • IDO1 ligand-1
    Cat. No.
    A75757

    IDO1 ligand-1

    IDO1 ligand-1 is a specific ligand that interacts with the IDO1 protein, facilitating targeted protein degradation through the PROTAC mechanism. This compound is instrumental in research focused on IDO1 modulation, which has implications in oncology and immunology. By effectively promoting the degradation of IDO1, IDO1 ligand-1 serves as a valuable tool for investigating the therapeutic potential of PROTACs in various biological contexts.

    Out of stock

    All 3 sizes
  • TBK1 ligand 2-C-O-C4-O-C3-O-C-amide
    Cat. No.
    A79473

    TBK1 ligand 2-C-O-C4-O-C3-O-C-amide

    TBK1 ligand 2-C-O-C4-O-C3-O-C-amide is a protein ligand-linker conjugate specifically designed to facilitate the development of targeted protein degraders. This compound serves as a crucial component in the synthesis of the PROTAC TBK1 degrader-2, enabling selective degradation of the TBK1 protein. Its application in chemical biology research allows for the investigation of TBK1's role in various cellular processes and the potential modulation of its activity.

    Out of stock

    All 3 sizes
  • Nrf2 activator-22
    Cat. No.
    A79524

    Nrf2 activator-22

    Nrf2 activator-22 is a ligand specifically targeting the Nrf2 protein, playing a crucial role in the development of PROTAC-based therapeutics. This compound facilitates the synthesis of PROTAC K-Ras Degrader-7, highlighting its potential in targeted protein degradation research. Nrf2 activator-22 is valuable for studies aimed at manipulating oxidative stress responses and related signaling pathways.

    Out of stock

    All 3 sizes
  • PI3Kγ ligand 1
    Cat. No.
    A79856

    PI3Kγ ligand 1

    PI3Kγ ligand 1 is a selective ligand for phosphoinositide 3-kinase gamma (PI3Kγ), utilized in the development of proteolysis-targeting chimeras (PROTACs). This compound effectively engages with PI3Kγ, facilitating targeted protein degradation. Its biological activity makes it valuable for research applications in cancer therapeutics and immunology, particularly in elucidating PI3K signaling pathways.

    Out of stock

    All 3 sizes
  • Thalidomide-5-piperazine
    Cat. No.
    A81258

    Thalidomide-5-piperazine

    Thalidomide-5-piperazine is a ligand designed for protein-targeted degradation utilizing the PROTAC technology. This compound facilitates the recruitment of E3 ubiquitin ligases to specific target proteins, promoting their ubiquitination and subsequent proteasomal degradation. It is primarily used in research applications focused on studying protein function and modulation within cellular pathways.

    Out of stock

    All 3 sizes
  • CBP/p300 ligand 2
    Cat. No.
    A81267

    CBP/p300 ligand 2

    CBP/p300 ligand 2 is a selective ligand targeting the dCBP-1 protein, facilitating its role as a heterobifunctional degrader of the p300/CBP proteins. This compound is essential for research applications focused on targeted protein degradation, enabling the study of p300/CBP's involvement in various biological processes and diseases. Its utility in PROTAC development makes it a valuable tool for investigating therapeutic strategies in cancer and other disorders linked to aberrant p300/CBP activity.

    1 mg
    $130.00
    5 mg
    $340.00
    All 6 sizes
  • EED226-COOH
    Cat. No.
    A81269

    EED226-COOH

    EED226-COOH is an EED226-derived ligand that targets the EED protein, facilitating the formation of PROTACs. This compound effectively binds to a VHL ligand through a linker, leading to the degradation of the PRC2 complex. EED226-COOH is valuable for research applications focused on targeted protein degradation and studying the roles of PRC2 in various biological processes.

    5 mg
    $110.00
    10 mg
    $180.00
    All 5 sizes
  • Ipatasertib-NH2
    Cat. No.
    A81270

    Ipatasertib-NH2

    Synonyms: GDC-0068-NH2; RG7440-NH2

    Ipatasertib-NH2 is a targeted ligand for the protein AKT, functioning as a key component in PROTAC-mediated degradation systems, specifically in INY-03-041. This compound is structured with a ten-hydrocarbon linker and the CRBN ligand Lenalidomide, enabling selective recruitment of E3 ubiquitin ligase for targeted protein degradation. Its utility in research includes elucidating AKT's role in cellular signaling and developing novel therapeutic strategies.

    5 mg
    $370.00
    10 mg
    $590.00
    All 5 sizes
  • TAE648
    Cat. No.
    A81271

    TAE648

    TAE648 is a ligand specifically designed for target proteins involved in PROTAC (Proteolysis Targeting Chimeras) research. This compound plays a crucial role in the synthesis of PROTAC SK-3-91, facilitating targeted degradation of specific proteins. Its applications span various areas of chemical biology and drug discovery, advancing studies in protein modulation and therapeutic development.

    5 mg
    $185.00
    10 mg
    $300.00
    All 5 sizes
  • Palbociclib-propargyl
    Cat. No.
    A81274

    Palbociclib-propargyl

    Synonyms: PROTAC CDK6 ligand 1

    Palbociclib-propargyl is a selective ligand for CDK6, designed for use in PROTAC applications. This compound functions through a PEG linker to effectively bind to the CRBN ligand, forming the PROTAC CP-10, which exhibits a DC50 of 2.1 nM for CDK6. Additionally, Palbociclib-propargyl features an alkyne group making it suitable for click chemistry, specifically allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-bearing molecules. This reagent is valuable for advancing research in targeted protein degradation and cancer therapeutics.

    2 mg
    $70.00
    5 mg
    $90.00
    All 6 sizes
  • (S)-SKBG-1
    Cat. No.
    A81275

    (S)-SKBG-1

    (S)-SKBG-1 is a covalent ligand designed for targeting specific proteins in the context of PROTAC applications. Though classified as inactive, it serves an essential role as an assay control to help validate experimental conditions and results. This compound is valuable for researchers investigating the mechanisms of protein degradation and the development of targeted therapeutic strategies.

    5 mg
    $245.00
    10 mg
    $405.00
    All 3 sizes
  • Tazemetostat de(methyl morpholine)-COOH
    Cat. No.
    A81276

    Tazemetostat de(methyl morpholine)-COOH

    Tazemetostat de(methyl morpholine)-COOH is a ligand specifically designed for the target protein EZH2, facilitating the synthesis of EZH2 degraders for the PROTAC approach. This compound exhibits significant biological activity by effectively inhibiting cell viability in diffuse large B-cell lymphoma (DLBCL) and various lymphoma subtypes. It serves as a valuable tool for researchers investigating targeted protein degradation and its therapeutic potential in oncology.

    5 mg
    $330.00
    10 mg
    $505.00
    All 5 sizes
  • SMARCA2/4-IN-2
    Cat. No.
    A81277

    SMARCA2/4-IN-2

    SMARCA2/4-IN-2 is a ligand specifically designed for the SMARCA2 and SMARCA4 proteins, facilitating the development of proteolysis-targeting chimeras (PROTACs). This compound serves as a critical component in the synthesis of PROTAC SMARCA2/4-degrader-5, enabling targeted degradation of these chromatin remodelers. SMARCA2/4-IN-2 is valuable for research applications in cancer biology and therapeutic development focused on modulation of epigenetic regulators.

    5 mg
    $135.00
    10 mg
    $225.00
    All 5 sizes
  • PROTAC ERRα ligand 1
    Cat. No.
    A81279

    PROTAC ERRα ligand 1

    PROTAC ERRα ligand 1 is an orally active inverse agonist targeting ERRα with an IC50 of 0.6 μM. This compound demonstrates selective inhibition, as it exhibits minimal activity against a range of other nuclear receptors, including ERαc, ERRγ, ERβ, PPARα, PPARγ, PPARδ, and RXRα. PROTAC ERRα ligand 1 is valuable for research in metabolic diseases, such as type 2 diabetes and obesity, and has shown potential in enhancing insulin sensitivity in vivo.

    1 mg
    $25.00
    2 mg
    $30.00
    All 8 sizes
  • PROTAC BRD9-binding moiety 1 hydrochloride
    Cat. No.
    A81280

    PROTAC BRD9-binding moiety 1 hydrochloride

    PROTAC BRD9-binding moiety 1 hydrochloride is a ligand that selectively binds to the bromodomain protein BRD9, facilitating its targeted degradation through the PROTAC (Proteolysis Targeting Chimeras) mechanism. This compound is instrumental in research focusing on protein degradation pathways and the modulation of BRD9-associated functions in various biological contexts, such as cancer and inflammation. It serves as a valuable tool for studying the therapeutic potential of targeting BRD9 in disease models.

    5 mg
    $370.00
    10 mg
    $630.00
    All 5 sizes
  • BRD9 ligand-6
    Cat. No.
    A81282

    BRD9 ligand-6

    BRD9 ligand-6 serves as a ligand for the BRD9 target protein, facilitating the development of PROTAC (Proteolysis Targeting Chimeras) compounds. This reagent exhibits specific binding properties that enable the selective degradation of target proteins in cellular models. It is particularly valuable in research applications focused on targeted protein degradation and therapeutic intervention strategies.

    5 mg
    $45.00
    10 mg
    $70.00
    All 6 sizes
  • Piperidine-GNE-049-N-Boc
    Cat. No.
    A81283

    Piperidine-GNE-049-N-Boc

    Piperidine-GNE-049-N-Boc is a ligand that targets the dCBP-1 protein, facilitating the development of proteolysis-targeting chimeras (PROTACs). This compound serves as a potent and selective heterobifunctional degrader for the transcriptional co-activators p300 and CBP. It is applicable in research aimed at understanding protein degradation mechanisms and the modulation of gene expression.

    5 mg
    $180.00
    10 mg
    $295.00
    All 5 sizes
  • Demethyl-RSL3
    Cat. No.
    A81284

    Demethyl-RSL3

    Demethyl-RSL3 functions as a ligand for targeted protein degradation through the proteolysis targeting chimera (PROTAC) mechanism. This compound effectively modulates cellular pathways by inducing degradation of specific proteins. Its applications lie primarily in cancer research and the development of novel therapeutic strategies aimed at improving targeted protein degradation efficacy.

    5 mg
    $100.00
    10 mg
    $165.00
    All 5 sizes
  • PROTAC Her3-binding moiety 1
    Cat. No.
    A81285

    PROTAC Her3-binding moiety 1

    PROTAC Her3-binding moiety 1 is a ligand designed to selectively target the HER3 protein, facilitating its degradation via the PROTAC (PROteolysis TArgeting Chimeras) technology. This compound plays a critical role in modulating HER3 activity, which is implicated in various cancer pathways. Its application in research includes studying HER3 signaling and developing targeted therapies for HER3-expressing malignancies.

    5 mg
    $335.00
    10 mg
    $550.00
    All 4 sizes

Items 76-100 of 156

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