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 (522):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • 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-174798
    PI3Kα Ligand-1 98.0%
    PI3Kα Ligand-1 is the ligand for PI3Kα that can be used for synthesis of PROTACs, such as PI3Kα degrader-1 (HY-174461).
    PI3Kα Ligand-1
  • 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-130845
    AR antagonist 1 1818885-54-9 99.03%
    AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
    AR antagonist 1
  • HY-137159
    Bestatin methyl ester 65322-89-6
    Bestatin methyl ester is a cell permeable Zn2+-binding aminopeptidases inhibitor. Bestatin methyl ester inhibits spore cell differentiation.
    Bestatin methyl ester
  • HY-Y1863
    3-Chlorobenzaldehyde 587-04-2 99.58%
    3-Chlorobenzaldehyde (m-Chlorobenzenecarboxaldehyde) is a kind of biological materials or organic compounds that are widely used in life science research.
    3-Chlorobenzaldehyde
  • HY-130815
    MAK683-CH2CH2COOH 2639882-68-9
    MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 (HY-130614) and PROTAC EED degrader-2 (HY-130615).
    MAK683-CH2CH2COOH
  • HY-107445
    PROTAC BRD9-binding moiety 1 2097512-23-5
    PROTAC BRD9-binding moiety 1 is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
    PROTAC BRD9-binding moiety 1
  • HY-115729
    PROTAC CDK9 ligand-1 3031327-95-1 99.75%
    PROTAC CDK9 ligand-1 is a CDK9 ligand that can be used in the synthesis of PROTACs.
    PROTAC CDK9 ligand-1
  • HY-138679
    Aberrant tau ligand 2 2417159-58-9
    Aberrant tau ligand 2 (Compound 4-12) is the ligand for tau protein and can be used as target protein ligand for synthesis of PROTAC degrader C004019 (HY-138669).
    Aberrant tau ligand 2
  • HY-201580
    ER ligand-8 2229713-97-5
    ER ligand-8 is an ER (Estrogen Receptor/ERR) ligand that can be used to synthesize the PROTAC molecule ERD-1233 (HY-169367).
    ER ligand-8
  • HY-147046
    ET-JQ1-OH 2421153-77-5
    ET-JQ1-OH is an allele-specific BET inhibitor. ET-JQ1-OH can serve as a Ligand for Target Protein for PROTAC, and is used for the development and design of PROTAC Brd4 degraders, such as AB3145 (HY-180923).
    ET-JQ1-OH
  • 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-131187
    BMS-1166-N-piperidine-COOH 2447066-00-2
    BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
    BMS-1166-N-piperidine-COOH
  • HY-141798
    OICR-9429-N-C2-NH2 2407457-55-8
    OICR-9429-N-C2-NH2 is a ligand for Wd40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1, intermediate 2. OICR-9429-N-C2-NH2 can be used in the synthesis of PROTACs.
    OICR-9429-N-C2-NH2
  • HY-203618
    PI3K/mTOR ligand-1 1197160-66-9
    PI3K/mTOR ligand-1 is a ligand for the target protein of PROTAC (PI3K/mTOR). PI3K/mTOR ligand-1 can be used to synthesize GP262 (HY-180261).
    PI3K/mTOR ligand-1
  • HY-179095
    UR241-2 2597345-07-6 99.68%
    UR241-2 is an IRAK4 inhibitor. UR241-2 suppresses IL-1–induced IRAK1/4 signaling, NF-κβ activation, and phosphorylation of p65 and p38. UR241-2 selectively inhibits leukemia stem cell clonogenicity. UR241-2 can serve as a ligand for target proteins for PROTAC, facilitating the development and design of PROTAC degraders for IRAK4. UR241-2 can be used in the research of acute myeloid leukemia.
    UR241-2
  • HY-125001
    JH-VIII-49 2209084-73-9
    JH-VIII-49 (compound 10) is a potent and selective CDK8 inhibitor (IC50=16 nM) with excellent biological activity. JH-VIII-49 promotes CDK8 inhibition through its steroid backbone design. JH-VIII-49 can be used in the synthesis of PROTAC as a target protein ligand of JH-XI-10-02 (HY-111518).
    JH-VIII-49
  • HY-169087
    MJBIA9836 3057446-77-9 99.67%
    MJBIA9836yes PROTACLigands for target proteins can be used to synthesize PROTACMolecules, such as MS41 (HY-169086).
    MJBIA9836
  • HY-169094
    PFI-6-COOH 2768514-05-0
    PFI-6-COOH (Compound 18) is an eleven-nineteen leukemia (ENL) ligand, and can be used for synthesis of MS41 (HY-169093), an ENL PROTAC degrader.
    PFI-6-COOH