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 (512):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-135832
    Demethyl-RSL3 2375354-13-3 98.40%
    Demethyl-RSL3 is a ligand for target protein for pROTAC.
    Demethyl-RSL3
  • HY-W128709
    SNAP-fusion protein ligand-1 913817-45-5
    SNAP-fusion protein ligand-1 (Compound 3) is a Ligand for Target Protein for PROTAC. SNAP-fusion protein ligand-1 can be used for synthesis of PROTAC VHL-SNAP2-5C (HY-175417).
    SNAP-fusion protein ligand-1
  • HY-111857
    Dasatinib carbaldehyde 2112837-79-1 99.74%
    Dasatinib carbaldehyde (BMS-354825 carbaldehyde), the Dasatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .
    Dasatinib carbaldehyde
  • HY-107444
    PROTAC Her3-binding moiety 1 1603845-36-8 99.64%
    PROTAC HER3-binding moiety 1 (compound 1b) is a Her3 Ligand for PROTAC.
    PROTAC Her3-binding moiety 1
  • HY-19339
    Tenovin-3 1011301-27-1 98.0%
    Tenovin-3 is a p53 activator.
    Tenovin-3
  • HY-126534S
    Abemaciclib metabolite M18-d8 98.00%
    Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.
    Abemaciclib metabolite M18-d<sub>8</sub>
  • HY-168545
    TTK ligand 3 99.50%
    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-168038
    PIN1 ligand-1 3038591-92-0 98.40%
    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
  • HY-132942A
    PROTAC BRD4 ligand-2 hydrochloride 99.65%
    PROTAC BRD4 ligand-2 hydrochloride is a ligand for target BRD4 protein for PROTAC CFT-2718.
    PROTAC BRD4 ligand-2 hydrochloride
  • HY-160937
    AZD-9574-acid 2923687-90-3 99.44%
    AZD-9574-acid (Compound 70D) is a PARP-1 ligand. AZD-9574-acid serves as a Ligand for Target Protein for PROTAC for the synthesis of PARP-1 PROTAC degraders. AZD-9574-acid is applicable to cancer research.
    AZD-9574-acid
  • HY-107443A
    (R)-I-BET762 carboxylic acid 1786401-70-4 99.50%
    (R)-I-BET762 carboxylic acid, the R-enantiomer of I-BET762 carboxylic acid (HY-107443). I-BET762 carboxylic acid is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid is a BRD4 inhibitor with a pIC50 value of 5.1.
    (R)-I-BET762 carboxylic acid
  • HY-150879
    BMS-37 1675202-20-6 98.01%
    BMS-37 is a PD-1/PD-L1 immune checkpoint inhibitor with an IC50 towards the PD-L1/PD-1 complex in the range of 18 to 200 nM. BMS-37 shows unspecific toxicity against modified Jurkat T cells with an EC50 between 3 and 6 µM. BMS-37 can be used for the study of the PD-L1-induced exhaustion of T-cells or as PD-L1 ligand to synthesize PROTAC molecules.
    BMS-37
  • HY-169049
    Smurf1 ligand 1 99.31%
    Smurf1 ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). Smurf1 ligand 1 can be used for synthesis SMART1 (HY-W998345).
    Smurf1 ligand 1
  • HY-168440
    Aurora-A ligand 1 2541626-73-5 98.75%
    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-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-168299
    AR ligand-30 2505498-73-5
    AR ligand-30 is a target protein ligand for PROTAC Bavdegalutamide (HY-138641), which can be used in prostate cancer research.
    AR ligand-30
  • 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