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-161394
    SPRT
    SPRT is a short peptide of RB transcriptional corepressor 1 (RB), serving as a fragment of RB-CO-PEG5-C2-CO-VH032 (HY-161393) for the synthesis of PROTAC.
    SPRT
  • HY-168237
    SMARCA2 ligand-10 3024271-84-6
    SMARCA2 ligand-10 is a ligand for a target protein, used for the synthesis of PROTAC SMARCA2 degrader-28(HY-168236).
    SMARCA2 ligand-10
  • HY-167701
    OBHSA 1404508-27-5
    OBHSA is a selective estrogen receptor (ERα) degrader. OBHSA blocks the cell cycle by degrading cyclin D1, thereby overcoming Tamoxifen (HY-13757A) resistance. OBHSA also triggers excessive activation of the unfolded protein response (UPR) by inducing an increase in intracellular reactive oxygen species, ultimately leading to cell apoptosis. In addition, OBHSA can also be used as an ERα ligand to synthesize PROTAC degraders.
    OBHSA
  • HY-186068
    BCL6 ligand-9
    BCL6 ligand-9, a BCL6 ligand, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). BCL6 ligand-9 can be used for the synthesis of PROTAC BCL6 Degrader-3 (HY-186067).
    BCL6 ligand-9
  • HY-181735
    BET-IN-30
    BET-IN-30 (Compound 11d) is a BTE family protein inhibitor, which can act as a BRD2/BRD3/BRD4 target protein ligand and be used for the synthesis of PROTACs, such as PROTAC BET Degrader-15 (HY-181729). BET-IN-30 exhibits potent anti-proliferative activity against acute myeloid leukemia (AML) cells such as MV4-11. BET-IN-30 can be used for the study of AML.
    BET-IN-30
  • HY-169482
    ALK protein ligand-1 2764870-80-4
    ALK protein ligand-1 (Compound A1), a ligand for the anaplastic lymphoma kinase (ALK) protein, is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs) that exhibits inhibitory effects on ALK. ALK protein ligand-1 can be used in the synthesis of AP-1 (HY-169481).
    ALK protein ligand-1
  • HY-179235
    RIPK1-IN-37 2782024-39-7
    RIPK1-IN-37 is an RIPK1 inhibitor and a ligand for the target protein for PROTAC LD5097 (HY-179234). RIPK1-IN-37 can be used to synthesize PROTAC.
    RIPK1-IN-37
  • HY-181115
    EGFR-IN-193 3065211-08-4
    EGFR-IN-193 is an EGFR inhibitor, which can be used to synthesize PROTACs as target protein ligands, such as PROTAC EGFR degrader 17 (HY-180917).
    EGFR-IN-193
  • HY-150908
    Brigatinib A 1197958-90-9
    Brigatinib A is an GID4 ligand. Brigatinib A can be used for synthesizing PROTAC BCR-ABL Degrader-2 (HY-174368).
    Brigatinib A
  • HY-181952
    BRD9 ligand-11
    BRD9 ligand-11 is a BRD9 PROTAC ligand. BRD9 ligand-11 can be conjugated with E3 ligase Ligand (HY-125845) and linker to synthesize PROTAC BRD9 Degrader-11 (HY-181951). PROTAC BRD9 Degrader-11 can be used for cancer research.
    BRD9 ligand-11
  • HY-176388
    ER ligand-12
    ER ligand-12 is an estrogen receptor (ER) ligand that can be used in the synthesis of PROTACs, such as PROTAC ER Degrader-2 (HY-128528).
    ER ligand-12
  • HY-111852
    GNF5-amido-Me 778277-37-5
    GNF5-amido-Me, the GNF5 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.
    GNF5-amido-Me
  • HY-168611
    PROTAC IRAK4 ligand-4 2434841-55-9
    PROTAC IRAK4 ligand-4 is a Ligand for Target Protein for PROTAC with antitumor activity. PROTAC IRAK4 ligand-4 can be used to synthesize PROTAC IRAK4 degrader-12 (HY-168586).
    PROTAC IRAK4 ligand-4
  • HY-173423
    DOT1L ligand-1
    DOT1L ligand-1 is a DOT1L ligand. DOT1L ligand-1 can be used as a Ligands for Target Protein for PROTAC synthesis, such as MS2133 (HY-173422).
    DOT1L ligand-1
  • HY-168700
    KRAS G12D ligand-2
    KRAS G12D ligand-2 is a Ligand for Target Protein for PROTAC. KRAS G12D ligand-2 can be used to synthesize Setidegrasib (HY-148273).
    KRAS G12D ligand-2
  • HY-178875
    Nrf2 activator-22 3082764-64-2
    Nrf2 activator-22, a Nrf2 activator, is a PROTAC target protein ligand. Nrf2 activator-22 can be used for synthesis PROTAC K-Ras Degrader-7 (HY-178873).
    Nrf2 activator-22
  • HY-169980
    Mivebresib-alkyne 2409674-37-7
    Mivebresib-alkyne (Compound 25), a Mivebresib (HY-100015) derivative, can be used for BRD4 targeted PROTAC synthesis through click reaction.
    Mivebresib-alkyne
  • HY-182297
    PRMT1 ligand-1
    PRMT1 ligand-1 is a PRMT1 ligand. PRMT1 ligand-1 can be used as a target protein ligand to develop and design degraders of PROTAC PRMT1, such as PROTAC PRMT1 degrader-1 (HY-182275). PROTAC PRMT1 degrader-1 inhibits the growth of various cancer cells.
    PRMT1 ligand-1
  • HY-170334
    ER ligand-7
    ER ligand-7 is the ligand for estrogen receptor, and can be used for synthesis of PROTAC ER Degrader-15 (HY-170332) as ligand for target protein.
    ER ligand-7
  • HY-174865
    MMH-165-26 3100147-71-2
    MMH-165-26 is a ligand for RelA/p65. MMH-165-26 reduces the expression of RelA/p65 and has significant cytotoxicity in MEC-1 (LC50 = 0.37 μM) cells. MMH-165-26 can be used for synthesizing PROTACs such as JP-163-16 (HY-174864).
    MMH-165-26