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 (387):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • 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-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-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-151069
    TMX-2039 2488892-01-7 99.42%
    TMX-2039 is a pan-CDK inhibitor for both cell cycle CDKs (CDK1, CDK2, CDK4, CDK5 and CDK6) and transcriptional CDKs (CDK7 and CDK9), with IC50s of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5 and 25 nM, respectively. TMX-2039 acts as a Ligands for Target Protein for PROTACs.
    TMX-2039
  • 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-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-135832
    Demethyl-RSL3 2375354-13-3 98.40%
    Demethyl-RSL3 is a ligand for target protein for pROTAC.
    Demethyl-RSL3
  • HY-107444
    PROTAC Her3-binding moiety 1 1603845-36-8 99.64%
    PROTAC HER3-binding moiety 1 (compound 1b) is a Her3 Ligand for PROTAC.
    PROTAC Her3-binding moiety 1
  • 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-163563
    JYQ-173 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-168440
    Aurora-A ligand 1 2541626-73-5 98.75%
    Aurora-A ligand 1 is a high-affinity and specific Aurora-A inhibitor with a dissociation constant (Kd) value of 0.85 nM. Aurora-A ligand 1 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC Aurora-A degraders with antitumor activity. Aurora-A ligand 1 can be used for the synthesis of HLB-0532259 (HY-168439). HLB-0532259 shows anti-tumor activity against neuroblastoma.
    Aurora-A ligand 1
  • HY-139304
    PROTAC Bcl-xL ligand-1 3029365-95-2 99.06%
    PROTAC Bcl-xL ligand-1 is a ligand for Bcl-xL that can be used in the synthesis of PROTACs.
    PROTAC Bcl-xL ligand-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-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-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-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-162946
    Alkyne-P60 99.95%
    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-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-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