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 (329):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-130852
    CDK9-IN-11 2748368-15-0
    CDK9-IN-11 is a potent CDK9 inhibitor. CDK9-IN-11 is the ligand for the PROTAC CDK9 Degrader-1 (HY-103628).
    CDK9-IN-11
  • HY-169182
    AK-068 2982851-09-0 99.57%
    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-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-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-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-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-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-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
  • HY-44012B
    SMARCA-BD ligand 1 for PROTAC hydrochloride 2380272-56-8 99.23%
    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-150879
    BMS-37 1675202-20-6 98.01%
    BMS-37 is a PD-1/PD-L1 immune checkpoint inhibitor. BMS-37 can be used as PD-L1 ligand to synthesize PROTAC molecules.
    BMS-37
  • 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-131295
    PD0325901-O-C2-dioxolane 2581116-22-3 98.62%
    PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader.
    PD0325901-O-C2-dioxolane
  • 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-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