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 (294):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-168864
    POI ligand 1
    POI ligand 1 is a template for the non-selective HDAC inhibitor Vorinostat (HY-10221). POI ligand 1 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC HDAC degraders with antitumor activity. POI ligand 1 can be used for the synthesis of FF2049 (HY-168863).
    POI ligand 1
  • HY-111855
    HG-7-85-01-Decyclopropane 2444044-44-2
    HG-7-85-01-Decyclopropane, the HG-7-85-01 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .
    HG-7-85-01-Decyclopropane
  • HY-168440
    Aurora-A ligand 1 2541626-73-5
    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-168868
    RET ligand-2 3053537-08-6
    RET ligand-2 is a selective RET inhibitor. RET ligand-2 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC RET degraders with antitumor activity. RET ligand-2 can be used for the synthesis of RD-23 (HY-168867).
    RET ligand-2
  • HY-169487
    SMARCA2 ligand-12 2755762-94-6
    SMARCA2 ligand-12 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). SMARCA2 ligand-12 can be used for synthesis PROTAC SMARCA2 degrader-25 (HY-169276).
    SMARCA2 ligand-12
  • HY-111839
    ATRA-hydroxyimino 135325-47-2
    ATRA-hydroxyimino (CRABP-II ligand 1), the Retinoic acid (ATRA)-based moiety, binds to cIAP1 ligand (Bestatin) via a linker to form SNIPER to degrade CRABP-II in IMR-32 cells.
    ATRA-hydroxyimino
  • HY-168036
    PIN1 inhibitor 3 3039570-04-9
    PIN1 inhibitor 3 (Compound A0) is a PIN1 inhibitor, with a KD of 25 nM and an IC50 of 150 nM. PIN1 inhibitor 3 can be used as a target protein ligand for the synthesis of PROTAC. PIN1 inhibitor 3 can be utilized in cancer research.
    PIN1 inhibitor 3
  • HY-161495
    CBP/p300 ligand 4
    CBP/p300 ligand 4 (Compound 4) is an orally active inhibitor for CBP/p300 bromodomain, with IC50 of 91.4 nM. CBP/p300 ligand 4 serves as a ligand for target protein XYD190 (HY-161495). XYD190 is a PROTAC degrader for CBP/p300.
    CBP/p300 ligand 4
  • HY-150885
    BTK ligand 1 330785-90-5
    BTK ligand 1 (compound 1) is a ligand targeting Bruton’s tyrosine kinase (Btk). BTK ligand 1 can combine with E3 ligase ligand (Ligand for E3 Ligase) through PROTAC Linker to form PROTAC. PROTACs targeting Btk can be used in the study of chronic lymphocytic leukemia (CLL) and other BK cell malignancies.
    BTK ligand 1
  • HY-173126
    BTK ligand-14
    BTK ligand-14 is a PROTAC target protein ligand that targets BTK and can be used for the synthesis of FDU73 (HY-173125).
    BTK ligand-14
  • HY-161790
    Mpro ligand 1
    Mpro ligand 1 is the ligand for target protein for PROTAC SARS-CoV-2 Mpro degrader-3 (HY-161789). Mpro ligand 1 is the active form of Mpro ligand 2 (HY-161791).
    Mpro ligand 1
  • HY-159615
    Cbl-b-IN-21 2851878-87-8
    Cbl-b-IN-21 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). Cbl-b-IN-21 can be used for synthesis PROTAC Cbl-b-IN-1 (HY-159608).
    Cbl-b-IN-21
  • HY-169152
    DCAF1 ligand 1 3036941-01-9
    DCAF1 ligand 1 (compound I-653) is the ligand for target protein for PROTAC BRD4-DCAF1 degrader-1 (HY-169151) which has a DC50 of 10~100 nM.
    DCAF1 ligand 1
  • HY-173373
    AR ligand-39 2156591-18-1
    AR ligand-39, an orally active and selective androgen receptor (AR) antagonist, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). AR ligand-39 can be used for synthesis PROTAC AR Degrader-10 (HY-173372).
    AR ligand-39
  • HY-163949
    SMARCA2/4-IN-3
    SMARCA2/4-IN-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). SMARCA2/4-IN-3 can be used for synthesis PROTAC SMARCA2/4-degrader-19 (HY-163877).
    SMARCA2/4-IN-3
  • 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-168271
    ER ligand-2
    ER ligand-2 (Ligands for Target Protein for Compound 24) is the ligand of ER. ER ligand-2 can be used for synthesis PROTAC ER Degrader-11 (HY-168270).
    ER ligand-2
  • HY-161791
    Mpro ligand 2 2816967-14-1
    Mpro ligand 2 (Compound 8) is the ligand for target protein, which can be used for synthesis of PROTAC SARS-CoV-2 Mpro degrader-3 (HY-161789).
    Mpro ligand 2
  • HY-170817
    SMI-1074 3033592-13-8
    SMI-1074 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). SMI-1074 can be used for synthesis SMD-3236 (HY-170824) and SMD-1087 (HY-170828).
    SMI-1074
  • HY-W150930
    mTOR ligand 1 7597-22-0
    mTOR ligand 1 (compound T2) is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). mTOR ligand 1 can serve as an active control for the target protein ligand of PD-M6 (HY-176166).
    mTOR ligand 1