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-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-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-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-173562
    PRMT5 ligand 2 1616391-79-7
    PRMT5 ligand 2 (Compound 38) is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PRMT5 ligand 2 can be used for synthesis MS115 (HY-173561).
    PRMT5 ligand 2
  • 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-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
    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
  • HY-174355
    HPK1 ligand 3
    HPK1 ligand 3 is a ligand for target protein for PROTAC that can be used to synthesize PROTAC HPK1 Degrader-4 (HY-174135).
    HPK1 ligand 3
  • HY-168542
    TTK ligand 2
    TTK ligand 2 is a monopolar spindle 1 (TTK) ligand that can be used in the synthesis of PROTACT (HY-168540).
    TTK ligand 2
  • HY-151476
    GID4 Ligand 2 3031442-90-4
    GID4 Ligand 2 (compound 67) is a selective GID4 binder (IC50=18.9 μM; Kd=17 μM). GID4 Ligand 2 can be used for the synthesis of PROTACs.
    GID4 Ligand 2
  • HY-169375
    RSL3-4-Me 3049087-33-1
    RSL3-4-Me is the active control of the target protein ligand Demethyl-RSL3 (HY-135832), which can be used for the synthesis of PROTAC .
    RSL3-4-Me
  • HY-161959
    EP300/CBP ligand 1
    EP300/CBP ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). EP300/CBP ligand 1 can be used for synthesis dCE-2 (HY-161958).
    EP300/CBP ligand 1
  • HY-175242
    PROTAC BRD4 ligand-4 2954925-72-3
    PROTAC BRD4 ligand-4 is a BRD4 ligand, which can be used to synthesize PROTAC BRD4 Degrader-37 (HY-175225).
    PROTAC BRD4 ligand-4
  • HY-168691
    PTPN2 ligand 1 3032975-34-8
    PTPN2 ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTAC). PTPN2 ligand 1 can be used to synthesize PVD-06 (HY-149760).
    PTPN2 ligand 1
  • HY-168018
    Demethyl-NSC682769 3058483-40-9
    Demethyl-NSC682769 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). Demethyl-NSC682769 can be used in synthesis PROTAC YAP degrader-1 (HY-168016).
    Demethyl-NSC682769