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 (366):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-111857
    Dasatinib carbaldehyde 2112837-79-1 99.74%
    Dasatinib carbaldehyde (BMS-354825 carbaldehyde), the Dasatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .
    Dasatinib carbaldehyde
  • 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.
    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-125001
    JH-VIII-49 2209084-73-9
    JH-VIII-49 (compound 10) is a potent and selective CDK8 inhibitor (IC50=16 nM) with excellent biological activity. JH-VIII-49 promotes CDK8 inhibition through its steroid backbone design. JH-VIII-49 can be used in the synthesis of PROTAC as a target protein ligand of JH-XI-10-02 (HY-111518).
    JH-VIII-49
  • 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-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-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-169049
    Smurf1 ligand 1 99.31%
    Smurf1 ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). Smurf1 ligand 1 can be used for synthesis SMART1 (HY-W998345).
    Smurf1 ligand 1
  • HY-173012
    CypA ligand-2
    CypA ligand-2 is the target protein ligand of PROTAC RJS308 (HY-173011). RJS308 is a PROTAC targeting CypA and exhibits antiviral activity.
    CypA ligand-2
  • HY-130297
    PROTAC BCR-ABL1 ligand 1 2489876-34-6 99.17%
    PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.
    PROTAC BCR-ABL1 ligand 1
  • 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-114872A
    SLF TFA 2378802-47-0 99.58%
    SLF TFA is a synthetic ligand for FK506-binding protein (FKBP) with an affinity of 3.1 μM for FKBP51 and an IC50 of 2.6 μM for FKBP12. SLF TFA can be used in the synthesis of PROTAC.
    SLF TFA
  • 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-47709
    STING ligand-3 2762552-73-6 99.21%
    STING ligand-3 is a Ligand for Target Protein for PROTAC activity control. STING ligand-3 can be used to synthesize Anti-inflammatory agent 70 (HY-157570).
    STING ligand-3
  • 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-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-13001S
    Quizartinib-d8 1300734-19-3
    Quizartinib-d8 (AC220-d8) is deuterium labeled Quizartinib. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis.
    Quizartinib-d<sub>8</sub>