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 (360):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-130992
    Androgen receptor antagonist 1 1338812-36-4 99.71%
    Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
    Androgen receptor antagonist 1
  • HY-147091
    Tazemetostat de(methyl morpholine)-COOH 2685873-44-1 98.15%
    Tazemetostat de(methyl morpholine)-COOH (compound 7) is a ligand for the PROTAC target protein EZH2, which can be used to synthesis of EZH2 degraders (PROTACs). EZH2 degraders have potent cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphoma.
    Tazemetostat de(methyl morpholine)-COOH
  • 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-163926
    SMARCA2/4-IN-2 1339378-93-6 99.27%
    SMARCA2/4-IN-2 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). SMARCA2/4-IN-2 can be used for synthesis PROTAC SMARCA2/4-degrader-5 (HY-159456).
    SMARCA2/4-IN-2
  • HY-126351
    PROTAC ERRα ligand 2 2306388-57-6 99.36%
    PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).
    PROTAC ERRα ligand 2
  • HY-131388
    ABM-14 1973408-76-2 98.17%
    ABM-14 is a ligand for targeting androgen receptor (AR) for PROTAC. ABM-14 binds to a ligand for VHL via linker to form ARCC-4 (HY-130492) to degrade AR.
    ABM-14
  • 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-150879
    BMS-37 1675202-20-6 98.01%
    BMS-37 is a PD-1/PD-L1 immune checkpoint inhibitor with an IC50 towards the PD-L1/PD-1 complex in the range of 18 to 200 nM. BMS-37 shows unspecific toxicity against modified Jurkat T cells with an EC50 between 3 and 6 µM. BMS-37 can be used for the study of the PD-L1-induced exhaustion of T-cells or as PD-L1 ligand to synthesize PROTAC molecules.
    BMS-37
  • 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-107445A
    PROTAC BRD9-binding moiety 1 hydrochloride 2448414-41-1 98.13%
    PROTAC BRD9-binding moiety 1 hydrochloride is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
    PROTAC BRD9-binding moiety 1 hydrochloride
  • 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-168683
    CDK8 ligand 1 2924557-38-8 ≥98.0%
    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-44012B
    SMARCA-BD ligand 1 for PROTAC hydrochloride 2380272-56-8 99.24%
    SMARCA-BD ligand 1 hydrochloride 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 hydrochloride
  • HY-169396
    TAE648 2769753-10-6 99.50%
    TAE648 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). TAE648 can be used for synthesis PROTAC SK-3-91 (HY-137341).
    TAE648
  • 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-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-164278
    diABZI-V/C-Mal 3035557-55-9 99.28%
    diABZI-V/C-Mal is a STING agonist.
    diABZI-V/C-Mal
  • HY-130850
    CDK9-IN-10 3542-63-0 98.09%
    CDK9-IN-10 is a potent CDK9 inhibitor. CDK9-IN-10 is the ligand for the PROTAC CDK9 degrader-2 (HY-112811).
    CDK9-IN-10
  • 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-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