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

Ligands for Target Protein for 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 (360):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-169182
    AK-068 2982851-09-0 99.57%
    AK-068 is a STAT6 ligand, with a Ki of 6 nM and at least >85-fold binding selectivity over STAT5. AK-068 is a ligand for target protein (STAT6) for PROTAC (HY-169179).
    AK-068
  • 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-130988
    Ipatasertib-NH2 1001382-14-4 99.64%
    Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) 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
  • HY-U00425
    PROTAC ERRα ligand 1 1264754-13-3 99.47%
    PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50s of 0.04 and 2.8 μM for ERRα and ERRγ, respectively.
    PROTAC ERRα ligand 1
  • HY-130841
    Apcin-A 1683617-62-0 ≥98.0%
    Apcin-A is a small molecule inhibitor that selectively targets the cell division cycle protein Cdc20 and is a derivative of Apcin (HY-110287). Apcin-A competitively binds to the D-box binding pocket of Cdc20 and inhibits substrate ubiquitination mediated by the anaphase promoting complex APC/C-Cdc20. Apcin-A also blocks the binding of Cdc20 to substrates (such as securin and cyclin B1), inhibiting anaphase initiation and cell cycle exit. Apcin-A can promote or prolong mitotic slippage in coordination with p31comet under conditions of high spindle assembly checkpoint (SAC) activity. Apcin-A can be used to develop anti-mitotic drugs and overcome tumor chemotherapy resistance. Apcin-A can be used to synthesize PROTAC CP5V (HY-130257)[1][2][3].
    Apcin-A
  • 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-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-111606
    DUPA 302941-52-2 ≥98.0%
    DUPA, belongs to a class of glutamate ureas, is used as the targeting moiety in agent conjugate to selectively deliver cytotoxic agents to prostate cancer cells.
    DUPA
  • HY-130979
    EED226-COOH 2467965-71-3 99.88%
    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-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-111671
    VUBI1 2245237-53-8 98.01%
    VUBI1 (SOS1 activator 1) is a benzimidazole derivative and SOS1 activator with a Kd of 44 nM. VUBI1 can significantly activate RAS-GTP and regulate the phosphorylation of ERK. VUBI1 also can serve as a target ligand for synthesizing PROTACs, such as PROTAC SOS1 degrader-1 (HY-145737), to induce SOS1 degradation. VUBI1 can be used in the study of cancer.
    VUBI1
  • HY-75578
    dTAG Targeting Ligand 1 755039-56-6 ≥98.0%
    dTAG Targeting Ligand 1 (SUBSTITUTE SHEET 245) is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). dTAG Targeting Ligand 1 can be used for synthesis PROTACs.
    dTAG Targeting Ligand 1
  • HY-168685
    c-Myc ligand 1 1942834-87-8 99.93%
    c-Myc ligand 1, a c-Myc inhibitor, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). c-Myc ligand 1 can be used for synthesis PROTAC c-Myc inhibitor 7 (HY-148837).
    c-Myc ligand 1
  • HY-107442
    PROTAC BRD4-binding moiety 1 2101200-10-4 99.10%
    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-43723
    PROTAC BET-binding moiety 2 916493-82-8 99.77%
    PROTAC BET-binding moiety 2 is an inhibitor of BET bromodomain.
    PROTAC BET-binding moiety 2
  • 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-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-126534
    Abemaciclib metabolite M18 2704316-81-2 98.01%
    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
  • 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