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 (510):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-130988
    Ipatasertib-NH2 1001382-14-4 99.64%
    Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) 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
  • HY-153918A
    (S)-SKBG-1 2955618-24-1 99.01%
    (S)-SKBG-1 is an inactive and covalent NONO ligand, used for assay control..
    (S)-SKBG-1
  • HY-130992
    Androgen receptor antagonist 1 1338812-36-4 99.64%
    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-49421
    BTK ligand 12 1791402-91-9 98.23%
    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-128837
    Nutlin carboxylic acid 2249750-27-2 98.63%
    Nutlin carboxylic acid is the Nutlin 3-based MDM2 ligand. Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTAC.
    Nutlin carboxylic acid
  • 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-130296
    Palbociclib-propargyl 2366269-23-8
    Palbociclib-propargyl is a ligand for target protein CDK6 for PROTAC, and binds to CRBN ligand via a PEG linker to make a PROTAC CP-10. CP-10 shows a DC50 of 2.1 nM for CDK6. Palbociclib-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.
    Palbociclib-propargyl
  • HY-168685
    c-Myc ligand 1 1942834-87-8 99.93%
    c-Myc ligand 1, a c-Myc inhibitor, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). c-Myc ligand 1 can be used for synthesis PROTAC c-Myc inhibitor 7 (HY-148837).
    c-Myc ligand 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-U00425
    PROTAC ERRα ligand 1 1264754-13-3 98.61%
    PROTAC ERRα ligand 1 is a PROTAC target protein ligand. PROTAC ERRα ligand 1 is an orally active ERRα inverse agonist with IC50 values of 0.6 μM for ERRα. PROTAC ERRα ligand 1 shows no significant activity against a panel of other nuclear receptors, including ERαc, ERRγ, ERβ, PPARα, PPARγ, PPARδ, and RXRα. PROTAC ERRα ligand 1 can provide enhanced insulin sensitivity in vivo. PROTAC ERRα ligand 1 can be used for metabolic diseases research, such as type 2 diabetes and obesity.
    PROTAC ERRα ligand 1
  • HY-130983
    N-piperidine Ibrutinib hydrochloride 2231747-18-3 98.06%
    N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
    N-piperidine Ibrutinib hydrochloride
  • 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-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-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-163563
    JYQ-173 3117543-57-1 99.78%
    JYQ-173, a chemical probe, 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-131388
    ABM-14 1973408-76-2 98.10%
    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-107451
    PROTAC BET-binding moiety 1 2093387-77-8
    PROTAC BET-binding moiety 1 is a key intermediate for the synthesis of high-affinity BET inhibitors.
    PROTAC BET-binding moiety 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-131232
    Desmorpholinyl Navitoclax-NH-Me 2365172-82-1 98.64%
    Desmorpholinyl Navitoclax-NH-Me is a Bcl-xL inhibitor. Desmorpholinyl Navitoclax-NH-Me and a CRBN ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC BCL-XL degrader XZ739 (HY-133557).
    Desmorpholinyl Navitoclax-NH-Me
  • HY-176864
    STAT6 ligand-1 98.94%
    STAT6 ligand-1 is a ligand for STAT6. STAT6 ligand-1 can be used for synthesizing PROTACs such as STAT6 degrader-2 (HY-176857).
    STAT6 ligand-1