2. Signaling Pathways
  3. PROTAC
  4. Ligands for Target Protein for PROTAC

Ligands for Target Protein for PROTAC

Target Protein-binding Moiety

Ligands for Target Protein for PROTAC

Related Products

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The PROTAC molecule consists of a target protein ligand and an E3 ubiquitin ligase ligand, with a linker binds them together. The ligand for target protein will lead to attachment of a PROTAC to the proteins of interest for ubiquitin and subsequent degradation.

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 (such as MEK, KRAS, CDK and Bcr/Abl), transcription factors (such as p53, STAT, RAR, ER and AR), epigenetic tools (such as HDAC and BET bromodomain) and E3 ligase themselves (such as MDM2).

Ligands for Target Protein for PROTAC Related Products (252):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-126534S
    Abemaciclib metabolite M18-d8 98.47%
    Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1][2].
    Abemaciclib metabolite M18-d<sub>8</sub>
  • HY-131187
    BMS-1166-N-piperidine-COOH 2447066-00-2
    BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
    BMS-1166-N-piperidine-COOH
  • HY-141798
    OICR-9429-N-C2-NH2 2407457-55-8
    OICR-9429-N-C2-NH2 is a ligand for Wd40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1, intermediate 2. OICR-9429-N-C2-NH2 can be used in the synthesis of PROTACs.
    OICR-9429-N-C2-NH2
  • HY-132942A
    PROTAC BRD4 ligand-2 hydrochloride 99.65%
    PROTAC BRD4 ligand-2 hydrochloride is a ligand for target BRD4 protein for PROTAC CFT-2718.
    PROTAC BRD4 ligand-2 hydrochloride
  • HY-49421
    BTK ligand 12 1791402-91-9
    BTK ligand 12 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). BTK ligand 12 can serve as an active control for the target protein ligand of NRX-0492 (HY-153357).
    BTK ligand 12
  • HY-107443A
    (R)-I-BET762 carboxylic acid 1786401-70-4 99.50%
    (R)-I-BET762 carboxylic acid, the R-enantiomer of I-BET762 carboxylic acid (HY-107443). I-BET762 carboxylic acid is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid is a BRD4 inhibitor with a pIC50 value of 5.1.
    (R)-I-BET762 carboxylic acid
  • HY-164278
    diABZI-V/C-Mal 3035557-55-9
    diABZI-V/C-Mal is a STING agonist.
    diABZI-V/C-Mal
  • HY-139660
    PROTAC PTK6 ligand-1 2408341-98-8
    PROTAC PTK6 ligand-1 is an intermediate for BTK kinase inhibitor preparation. PROTAC PTK6 ligand-1 can be used in the synthesis of ARD-61 (HY-139659).
    PROTAC PTK6 ligand-1
  • HY-126534
    Abemaciclib metabolite M18 2704316-81-2
    Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.
    Abemaciclib metabolite M18
  • HY-44146
    Defactinib analogue-1 2296719-34-9
    Defactinib analogue-1 (Compound 7) is a ligand for target protein Fak, that can be used for synthesis of PROTAC FAK degrader 1 (HY-119932).
    Defactinib analogue-1
  • HY-107453
    SirReal1-O-propargyl 1862237-99-7
    SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2. SirReal1-O-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SirReal1-O-propargyl
  • HY-12863B
    CPI-0610 carboxylic acid 1380089-81-5
    CPI-0610 carboxylic acid is a ligand for target protein for PROTACT. CPI-0610 carboxylic acid is a potent bromodomain and extra-terminal (BET) protein inhibitor. CPI-0610 carboxylic acid has the potential in the therapy of multiple myeloma.
    CPI-0610 carboxylic acid
  • HY-44012
    SMARCA-BD ligand 1 for PROTAC 1997319-92-2 99.07%
    SMARCA-BD ligand 1 for PROTAC is a compound that binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC.
    SMARCA-BD ligand 1 for PROTAC
  • HY-130813
    BET-IN-6 2570470-39-0
    BET-IN-6 is a potent and high affnity BRD2/BRD4 inhibitor. BET-IN-6 is the ligand for target protein BRD2/4, and is used for the systhesis of PROTAC BRD2/BRD4 degrader-1 (HY-130612).
    BET-IN-6
  • HY-125908
    A-1210477-piperazinyl 2351218-72-7
    A-1210477-piperazinyl is a compound binds to protein myeloid cell leukemia 1 (MCL1) used for PROTAC technology.
    A-1210477-piperazinyl
  • HY-130988A
    Ipatasertib-NH2 dihydrochloride 1001264-73-8
    Ipatasertib-NH2 dihydrochloride is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase.
    Ipatasertib-NH2 dihydrochloride
  • HY-134592
    Piperidine-GNE-049-N-Boc 1936431-36-5 98.82%
    Piperidine-GNE-049-N-Boc is a ligand for target protein for PROTAC of dCBP-1 (HY-134582). dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.
    Piperidine-GNE-049-N-Boc
  • HY-130981
    FN-1501-propionic acid 2408642-48-6
    FN-1501-propionic acid is a CDK2/9 ligand for PROTAC. FN-1501-propionic acid and a CRBN ligand have been used to design PROTAC CDK2/9 degrader (HY-130709).
    FN-1501-propionic acid
  • HY-107447S
    N-Deshydroxyethyl Dasatinib-d8 1189998-96-6
    N-Deshydroxyethyl Dasatinib-d8 is the deuterium labeled N-Deshydroxyethyl Dasatinib. N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825), the Dasatinib-based moiety, binds to IAP ligand via a linker to form SNIPER to degrade ABL[1].
    N-Deshydroxyethyl Dasatinib-d<sub>8</sub>
  • HY-169280
    PXR Ligand 2
    PXR Ligand 2 (Compound 55) is the target protein ligand for PROTAC SMARCA2/4-degrader-34 (HY-169279).
    PXR Ligand 2