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

Ligands for Target Protein for PROTAC

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 (293):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-44103
    Desmethyl-QCA276 2126819-55-2
    Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM. Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Desmethyl-QCA276
  • HY-130815
    MAK683-CH2CH2COOH 2639882-68-9
    MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 (HY-130614) and PROTAC EED degrader-2 (HY-130615).
    MAK683-CH2CH2COOH
  • HY-107445
    PROTAC BRD9-binding moiety 1 2097512-23-5
    PROTAC BRD9-binding moiety 1 is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
    PROTAC BRD9-binding moiety 1
  • HY-115729
    PROTAC CDK9 ligand-1 3031327-95-1 99.75%
    PROTAC CDK9 ligand-1 is a CDK9 ligand that can be used in the synthesis of PROTACs.
    PROTAC CDK9 ligand-1
  • HY-168683
    CDK8 ligand 1 2924557-38-8
    CDK8 ligand 1 is the ligand of CDK8. CDK8 ligand 1 can be used to synthesize LL-K8-22 (HY-149209).
    CDK8 ligand 1
  • HY-201580
    ER ligand-8 2229713-97-5
    ER ligand-8 is an ER (Estrogen Receptor/ERR) ligand that can be used to synthesize the PROTAC molecule ERD-1233 (HY-169367).
    ER ligand-8
  • 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-163563
    JYQ-173
    JYQ-173 is a selective inhibitor for human Parkinson disease protein 7 (PARK7), with an IC50 of 19 nM. JYQ-173 exhibits good cell permeability. JYQ-173 is the ligand for target protein PARK7, which can be utilized for synthesis of PROTAC Degrader JYQ-194 (HY-163564).
    JYQ-173
  • 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-169182
    AK-068 2982851-09-0
    AK-068 is a STAT6 ligand, with a Ki of 6 nM and at least >85-fold binding selectivity over STAT5. AK-068 is a ligand for target protein (STAT6) for PROTAC (HY-169179).
    AK-068
  • 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 98.01%
    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-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-131178
    HG-7-85-01-NH2 1258391-29-5 98.05%
    HG-7-85-01-NH2 is the HG-7-85-01 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.
    HG-7-85-01-NH2
  • 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