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 (102):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-130981
    FN-1501-propionic acid 2408642-48-6
    FN-1501-propionic acid is a CDK2/9 ligand for PROTAC. FN-1501-propionic acid and a CRBN ligand have been used to design PROTAC CDK2/9 degrader (HY-130709).
    FN-1501-propionic acid
  • HY-44012
    SMARCA-BD ligand 1 for Protac 1997319-92-2
    SMARCA-BD ligand 1 for Protac is a compound that binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC.
    SMARCA-BD ligand 1 for Protac
  • HY-130988A
    Ipatasertib-NH2 dihydrochloride 1001264-73-8
    Ipatasertib-NH2 dihydrochloride is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase.
    Ipatasertib-NH2 dihydrochloride
  • HY-107447S
    N-Deshydroxyethyl Dasatinib-d8 1189998-96-6
    N-Deshydroxyethyl Dasatinib-d8 is the deuterium labeled N-Deshydroxyethyl Dasatinib. N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825), the Dasatinib-based moiety, binds to IAP ligand via a linker to form SNIPER to degrade ABL[1].
    N-Deshydroxyethyl Dasatinib-d<sub>8</sub>
  • 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-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-44012B
    SMARCA-BD ligand 1 for Protac hydrochloride 2380272-56-8 99.23%
    SMARCA-BD ligand 1 hydrochloride for Protac is a compound that binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC.
    SMARCA-BD ligand 1 for Protac hydrochloride
  • HY-115729A
    (R)-PROTAC CDK9 ligand-1 2411021-95-7
    (R)-PROTAC CDK9 ligand-1 (Compound 19.4) is a CDK9-targeting degrader that can be used to synthesize PROTAC with antitumor activity.
    (R)-PROTAC CDK9 ligand-1
  • HY-107444
    PROTAC Her3-binding moiety 1 1603845-36-8
    PROTAC HER3-binding moiety 1 (compound 1b) is a Her3 Ligand for PROTAC.
    PROTAC Her3-binding moiety 1
  • HY-111849
    Imatinib carbaldehyde 1436868-85-7
    Imatinib carbaldehyde (CGP-57148B carbaldehyde), the Imatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.
    Imatinib carbaldehyde
  • HY-158430
    CYP1B1 ligand 2 2836297-58-4
    CYP1B1 ligand 2 is a target protein ligand of PROTAC CYP1B1 degrader-2 (HY-158429). CYP1B1 ligand 2 can be used to study lung cancer.
    CYP1B1 ligand 2
  • 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-161709
    FLT3/CDKs ligand-1 2452019-67-7
    FLT3/CDKs ligand-1 (Compound 14) is a ligand for target protein, which promotes the degradation of cyclin-dependent kinase (CDK) and the FMS-like tyrosine kinase 3 (FLT3), inhibits FLT3/CDK related proliferations and survivals of leukemia cells. LT3/CDKs ligand-1 can be used for synthesis of PROTAC FLT3/CDKs degrader-1 (HY-161708).
    FLT3/CDKs ligand-1
  • HY-151475
    GID4 Ligand 1 3031442-96-0
    GID4 Ligand 1 (compound 88) is a cell-permeable and high-selective GID4 binder (IC50=5.4 μM; Kd=5.6 μM), binds to GID4 in cells (EC50=558 nM). GID4 Ligand 1 can be used for the synthesis of PROTACs.
    GID4 Ligand 1
  • HY-161452
    SOS1 Ligand intermediate-3
    SOS1 Ligand intermediate-3 (Compound 5) is an SOS1 binder that can be used together with pomalidomide (HY-10984) for the synthesis of SOS1 PROTACs.
    SOS1 Ligand intermediate-3
  • HY-10997R
    Ibrutinib (Standard) 936563-96-1
    Ibrutinib (Standard) is the analytical standard of Ibrutinib. This product is intended for research and analytical applications. Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
    Ibrutinib (Standard)
  • HY-160151
    TP1L
    TP1L is a selective TC-PTP PROTAC degrader for cancer immunotherapy with a DC50 value of 35.8 nM.
    TP1L
  • HY-163563
    JYQ-173
    JYQ-173 is a selective inhibitor for human Parkinson disease protein 7 (PARK7), with an IC50 of 19 nM. JYQ-173 exhibits good cell permeability. JYQ-173 is the ligand for target protein PARK7, which can be utilized for synthesis of PROTAC Degrader JYQ-194 (HY-163564).
    JYQ-173
  • HY-160094
    BCN-sulfonamide-PEG2-sulfonamide-N-bis(ethanol) 2126749-81-1
    BCN-sulfonamide-PEG2-sulfonamide-N-bis ethanol (compound 71) is a Ligands for Target Protein for PROTAC that contains a sulfonamide linker to increase the solubility of the linker-conjugate. BCN-sulfonamide-PEG2-sulfonamide-N-bis ethanol can be used to synthesize PROTACs with antitumor activity.
    BCN-sulfonamide-PEG2-sulfonamide-N-bis(ethanol)
  • HY-46340
    AZD9496 deacrylic acid phenol 2173404-70-9
    AZD9496 deacrylic acid phenol is a fragment of target protein ligand of PROTAC ER Degrader-4 (HY-135309).
    AZD9496 deacrylic acid phenol