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 (366):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-170330
    AR ligand-33
    AR ligand-33 is the ligand for androgen receptor, that can be used for synthesis of PROTAC AR Degrader-8 (HY-170329) as the target protein ligand.
    AR ligand-33
  • HY-145484
    PROTAC IRAK4 ligand-3 2434848-46-9
    PROTAC IRAK4 ligand-3 is a ligand of PROTAC KT-474 (HY-145483) that can be used in cancer research.
    PROTAC IRAK4 ligand-3
  • HY-45124
    3-Fluoro-desmethyl-cabozantinib 849217-50-1
    3-Fluoro-desmethyl-cabozantinib is an BCL6 ligand that can be used in the synthesis of PROTACs, such as SJF-8240 (HY-123961).
    3-Fluoro-desmethyl-cabozantinib
  • HY-163963
    IBT6A-CO-ethyne 1970122-88-3
    IBT6A-CO-ethyne is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). IBT6A-CO-ethyne can be used for synthesis IBT6A (HY-13036A).
    IBT6A-CO-ethyne
  • HY-170450
    AR ligand-38
    AR ligand-38 is the ligand for androgen receptor, that can be used for synthesis of PROTAC AR Degrader-9 (HY-170448).
    AR ligand-38
  • HY-170860
    CK1δ/CK1ε liagnd-1
    CK1δ/CK1ε liagnd-1 is the ligand for CK1δ/CK1ε that can be used for synthesis of CK1 PROTAC degrader AH078 (HY-170859) as the ligand for target protein.
    CK1δ/CK1ε liagnd-1
  • HY-168287
    HDAC3/8 ligand-1
    HDAC3/8 ligand-1 (compound 40) is a ligand for target protein for PROTAC that can be used in the synthesis of YX968 (HY-164233).
    HDAC3/8 ligand-1
  • HY-162738
    JMV6944 2871774-93-3
    JMV6944 is a PXR agonist. JMV6944 competitively inhibits hPXR ligand-binding domain (LBD) binding to PXR with an IC50 of 680nM. JMV6944 induces CYP3A4 mRNA expression in freshly isolated human primary human hepatocyte cultures. JMV6944 can be used for the synthesis of PROTAC PXR degrader JMV7048 (HY-162704).
    JMV6944
  • HY-159573
    Napabucasin analogue 1133287-34-9
    Napabucasin analogue is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). Napabucasin analogue can be used in synthesis Napabucasin (HY-13919).
    Napabucasin analogue
  • HY-161960
    EP300/CBP ligand 2
    EP300/CBP ligand 2 (compound S19) is a ligand targeting the bromodomain of CREB binding protein (CBP) and E1A-associated protein (EP300). EP300/CBP ligand 2 can be used as a target protein ligand in the PROTAC structure, and can be coupled to the E3 ubiquitin ligase ligand through the PTOTAC Linker to synthesize PROTAC molecules with degradation effects. For example, EP300/CBP ligand 2 can be coupled with the conjugate (E3 ubiquitin enzyme ligand + Linker) Thalidomide-NH-C10-Boc (HY-161961) to produce the PROTAC molecule dCE-2 (HY-161958).
    EP300/CBP ligand 2
  • HY-161709
    FLT3/CDKs ligand-1 2452019-67-7
    FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependent kinase (CDK) and the FMS-like tyrosine kinase 3 (FLT3), inhibits FLT3/CDK related proliferations and survivals of leukemia cells. LT3/CDKs ligand-1 can be used for synthesis of PROTAC FLT3/CDKs degrader-1 (HY-161708).
    FLT3/CDKs ligand-1
  • HY-177432
    TMX-4140 2867519-51-3
    TMX-4140 is a selective PIP4K2C inhibitor with a KD of 7.2 nM for PIP4K2C over PIP4K2B. TMX-4140 can be used for synthesis of PROTAC TMX-4153 (HY-153119).
    TMX-4140
  • HY-175549
    HPK1 ligand 4
    HPK1 ligand 4 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-5 (HY-175547). PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader with anti-tumor activity.
    HPK1 ligand 4
  • HY-400666
    AR ligand-44 2632308-15-5
    AR ligand-44 is an androgen receptor ligand that can be used in the synthesis of PROTACs, such as ARD-2051 (HY-149862).
    AR ligand-44
  • HY-151475
    GID4 Ligand 1 3031442-96-0
    GID4 Ligand 1 (compound 88) is a cell-permeable and high-selective GID4 binder (IC50=5.4 μM; Kd=5.6 μM), binds to GID4 in cells (EC50=558 nM). GID4 Ligand 1 can be used for the synthesis of PROTACs.
    GID4 Ligand 1
  • HY-168658
    CDK12/13 ligand 2
    CDK12/13 ligand 2 is a potent CDK12 and CDK13 ligand. CDK12/13 ligand 2 can be used to synthesize YJ1206 (HY-168555).
    CDK12/13 ligand 2
  • HY-161452
    SOS1 Ligand intermediate-3
    SOS1 Ligand intermediate-3 (Compound 5) is an SOS1 binder that can be used together with pomalidomide (HY-10984) for the synthesis of SOS1 PROTACs.
    SOS1 Ligand intermediate-3
  • HY-168545
    TTK ligand 3
    TTK ligand 3 (Compound 5) is a ligand of monopolar spindle 1 (Mps1, TTK) that can be used in the synthesis of PROTAC (HY-168543).
    TTK ligand 3
  • HY-176183
    STING ligand-4
    STING ligand-4 (Compound 2) is a nitro-free covalent STING inhibitor with an IC50 < 0.2 μM. STING ligand-4 can be used for synthesis of PROTAC STING degrader-4 (HY-176180).
    STING ligand-4
  • HY-168038
    PIN1 ligand-1 3038591-92-0
    PIN1 ligand-1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PIN1 ligand-1 can be used for synthesis PROTAC PIN1 degrader-1 (HY-168037).
    PIN1 ligand-1