2. Signaling Pathways
  3. PROTAC
  4. Ligands for Target Protein for PROTAC

Ligands for Target Protein for PROTAC

PROTAC

Target Protein-binding Moiety

Ligands for Target Protein for PROTAC

Related Products

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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 (283):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-112429
    HJB97 2093391-24-1 98.05%
    HJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2). HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity. HJB97 can be used for the synthesis of BETd-260 (HY-101519).
    HJB97
  • HY-75706
    N-Descyclopropanecarbaldehyde Olaparib 763111-47-3 99.27%
    N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib (HY-10162) containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a PARP inhibitor used for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4 (HY-141481). N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled with F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor.
    N-Descyclopropanecarbaldehyde Olaparib
  • HY-129363
    AP1867-3-(aminoethoxy) 2127390-15-0 98.60%
    AP1867-3-(aminoethoxy), the AP1867 based moiety, is a synthetic ligand for FKBP. AP1867-3-(aminoethoxy) can be used in the synthesis of PROTAC FKBP12 F36V degrader.
    AP1867-3-(aminoethoxy)
  • HY-141799
    Dimethyl-F-OICR-9429-COOH 2407458-49-3 98.05%
    Dimethyl-F-OICR-9429-COOH a ligand for WD40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1 intermediate 19. Dimethyl-F-OICR-9429-COOH can be used in the synthesis of PROTACs.
    Dimethyl-F-OICR-9429-COOH
  • HY-130841
    Apcin-A 1683617-62-0 ≥98.0%
    Apcin-A, an Apcin derivative, is an anaphase-promoting complex (APC) inhibitor. Apcin-A interacts strongly with Cdc20, and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V (HY-130257).
    Apcin-A
  • HY-130992
    Androgen receptor antagonist 1 1338812-36-4 99.71%
    Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
    Androgen receptor antagonist 1
  • HY-130979
    EED226-COOH 2467965-71-3 98.53%
    EED226-COOH is an EED226-derived ligand for target protein EED ligand for PROTAC, binds to a ligand for VHL via linker to form UNC6852 (HY-130708) to degrade PRC2.
    EED226-COOH
  • HY-124625
    BI-4464 1227948-02-8 98.64%
    BI-4464 is a highly selective, ATP competitive PTK2/FAK protein kinase inhibitor with an IC50 value of 17 nM. BI-4464 can be used as a PTK2 ligand for constructing proteolysis targeting chimeras (PROTAC).
    BI-4464
  • HY-130983
    N-piperidine Ibrutinib hydrochloride 2231747-18-3 98.06%
    N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
    N-piperidine Ibrutinib hydrochloride
  • HY-130296
    Palbociclib-propargyl 2366269-23-8
    Palbociclib-propargyl is a ligand for target protein CDK6 for PROTAC, and binds to CRBN ligand via a PEG linker to make a PROTAC CP-10. CP-10 shows a DC50 of 2.1 nM for CDK6. Palbociclib-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Palbociclib-propargyl
  • HY-43723
    PROTAC BET-binding moiety 2 916493-82-8 99.10%
    PROTAC BET-binding moiety 2 is an inhibitor of BET bromodomain.
    PROTAC BET-binding moiety 2
  • HY-14217
    Quizartinib dihydrochloride 1132827-21-4 99.81%
    Quizartinib dihydrochloride (AC220 dihydrochloride) is the dihydrochloride salt form of Quizartinib (HY-13001). Quizartinib dihydrochloride is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib dihydrochloride inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib dihydrochloride can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib dihydrochloride induces apoptosis.
    Quizartinib dihydrochloride
  • HY-44012A
    SMARCA-BD ligand 1 for PROTAC dihydrochloride 2369053-68-7 98.56%
    SMARCA-BD ligand 1 for PROTAC dihydrochloride 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 dihydrochloride
  • HY-107442
    PROTAC BRD4-binding moiety 1 2101200-10-4
    PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136). PROTAC BRD4-binding moiety 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC BRD4-binding moiety 1
  • HY-W453397
    Aberrant tau ligand 1 1892461-96-9 99.33%
    Aberrant tau ligand 1 is a ligand for tau proteins with abnormal forms. Aberrant tau ligand 1 can be used for synthesis of PROTAC aberrant Tau degrader QC-01-175 (HY-134850).
    Aberrant tau ligand 1
  • HY-147091
    Tazemetostat de(methyl morpholine)-COOH 2685873-44-1 98.15%
    Tazemetostat de(methyl morpholine)-COOH (compound 7) is a ligand for the PROTAC target protein EZH2, which can be used to synthesis of EZH2 degraders (PROTACs). EZH2 degraders have potent cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphoma.
    Tazemetostat de(methyl morpholine)-COOH
  • HY-107451
    PROTAC BET-binding moiety 1 2093387-77-8
    PROTAC BET-binding moiety 1 is a key intermediate for the synthesis of high-affinity BET inhibitors.
    PROTAC BET-binding moiety 1
  • HY-130852
    CDK9-IN-11 2748368-15-0
    CDK9-IN-11 is a potent CDK9 inhibitor. CDK9-IN-11 is the ligand for the PROTAC CDK9 Degrader-1 (HY-103628).
    CDK9-IN-11
  • HY-150407
    TSPO ligand-1 4560-08-1 ≥98.0%
    TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration.
    TSPO ligand-1
  • HY-131388
    ABM-14 1973408-76-2 98.17%
    ABM-14 is a ligand for targeting androgen receptor (AR) for PROTAC. ABM-14 binds to a ligand for VHL via linker to form ARCC-4 (HY-130492) to degrade AR.
    ABM-14