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

Ligands for Target Protein for PROTAC

Target Protein-binding Moiety

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 (512):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-161575
    NSD2 ligand 1 99.76%
    NSD2 ligand 1 is a NSD2 ligand. NSD2 ligand 1 can be used for synthesis of LLC0424 (HY-161574) (a PROTAC NSD2 degrader).
    NSD2 ligand 1
  • HY-129363
    AP1867-3-(aminoethoxy) 2127390-15-0 98.60%
    AP1867-3-(aminoethoxy), the AP1867 (HY-114434) based moiety, is a synthetic ligand for FKBP. AP1867-3-(aminoethoxy) can be used in the synthesis of PROTAC FKBP12 F36V degrader.
    AP1867-3-(aminoethoxy)
  • HY-130845A
    AR antagonist 1 hydrochloride 1818885-55-0 99.53%
    AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
    AR antagonist 1 hydrochloride
  • HY-161830
    CDK7 ligand 2 2603381-71-9 99.92%
    CDK7 ligand 2 (Compound A6) is a CDK7 ligand. CDK7 ligand 2 can be used in the synthesis of PROTACs.
    CDK7 ligand 2
  • HY-126351
    PROTAC ERRα ligand 2 2306388-57-6 99.36%
    PROTAC ERRα ligand 2 is a ERRα ligand with a target IC50 of 5.67 nM. PROTAC ERRα ligand 2 blocks the protein-protein interaction between ERRα and PGC-1α. PROTAC ERRα ligand 2 can be used for synthesis of PROTACs.
    PROTAC ERRα ligand 2
  • HY-134592
    Piperidine-GNE-049-N-Boc 1936431-36-5 98.48%
    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-173562
    PRMT5 ligand 2 1616391-79-7 98.03%
    PRMT5 ligand 2 (Compound 38) is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PRMT5 ligand 2 can be used for synthesis MS115 (HY-173561).
    PRMT5 ligand 2
  • HY-168542
    TTK ligand 2 99.43%
    TTK ligand 2 is a monopolar spindle 1 (TTK) ligand that can be used in the synthesis of PROTACT (HY-168540).
    TTK ligand 2
  • HY-162946
    Alkyne-P60 99.96%
    Alkyne-P60 is a potent 15-mer peptide inhibitor of Foxp3. Alkyne-P60 can bind with Foxp3, hinder its nuclear translocation, and diminish Foxp3-mediated inhibition of NFKB and NFAT functions. Alkyne-P60 is a ligand for target protein for PROTAC (HY-162943).
    Alkyne-P60
  • HY-150859
    HDAC ligand-1 34840-28-3
    HDAC ligand-1 is a HDAC ligand that can be used to synthesize PROTAC HDAC degraders, such as compounds 21a and 21b in references.
    HDAC ligand-1
  • HY-107442
    PROTAC BRD4-binding moiety 1 2101200-10-4 99.10%
    PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136). PROTAC BRD4-binding moiety 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC BRD4-binding moiety 1
  • HY-43723
    PROTAC BET-binding moiety 2 916493-82-8 99.77%
    PROTAC BET-binding moiety 2 is an inhibitor of BET bromodomain.
    PROTAC BET-binding moiety 2
  • HY-W453397
    Aberrant tau ligand 1 1892461-96-9 99.33%
    Aberrant tau ligand 1 is a tau protein ligand. Aberrant tau ligand 1 engages tau and CRBN to trigger proteasomal degradation. Aberrant tau ligand 1 can be used for synthesis PROTACs, such as QC-01–175 (HY-134850).
    Aberrant tau ligand 1
  • HY-163526
    STAT3-IN-26 3033746-27-6
    STAT3-IN-26 is the ligand for the target protein STAT3 in PROTAC STAT3 degrader-3 (HY-163502), which can be used for the synthesis of PROTACs.
    STAT3-IN-26
  • HY-49393
    BRD9 ligand-6 2460248-49-9
    BRD9 ligand-6 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). BRD9 ligand-6 can be utilized for the synthesis of FHD-609 (HY-153367).
    BRD9 ligand-6
  • HY-150407
    TSPO ligand-1 4560-08-1 98.0%
    TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration.
    TSPO ligand-1
  • HY-171141
    HDAC6 ligand-2 98.70%
    HDAC6 ligand-2 (Compound 15) is the ligand for HDAC6 that can be used for synthesis of PROTAC HDAC6 degrader 2 (HY-171139).
    HDAC6 ligand-2
  • HY-44103
    Desmethyl-QCA276 2126819-55-2 99.16%
    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-44012A
    SMARCA-BD ligand 1 for PROTAC dihydrochloride 2369053-68-7 98.08%
    SMARCA-BD ligand 1 for PROTAC dihydrochloride 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 dihydrochloride
  • HY-110167
    TFC 007 927878-49-7 98.01%
    TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon).
    TFC 007