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 (87):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-139304
    PROTAC Bcl-xL ligand-1 3029365-95-2
    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-130850
    CDK9-IN-10 3542-63-0 98.00%
    CDK9-IN-10 is a potent CDK9 inhibitor. CDK9-IN-10 is the ligand for the PROTAC CDK9 degrader-2 (HY-112811).
    CDK9-IN-10
  • 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-126534S
    Abemaciclib metabolite M18-d8 98.47%
    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[1][2].
    Abemaciclib metabolite M18-d<sub>8</sub>
  • HY-107445A
    PROTAC BRD9-binding moiety 1 hydrochloride 2448414-41-1 98.07%
    PROTAC BRD9-binding moiety 1 hydrochloride is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
    PROTAC BRD9-binding moiety 1 hydrochloride
  • HY-44103
    Desmethyl-QCA276 2126819-55-2
    Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM. Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Desmethyl-QCA276
  • 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-110167
    TFC 007 927878-49-7 ≥98.0%
    TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon).
    TFC 007
  • 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-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-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
  • HY-107453
    SirReal1-O-propargyl 1862237-99-7
    SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2. SirReal1-O-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.
    SirReal1-O-propargyl
  • HY-136857
    PROTAC BRD4 Degrader-7 2413382-30-4
    PROTAC BRD4 Degrader-7 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC50s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively. PROTAC BRD4 Degrader-7 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 Degrader-7
  • HY-130845
    AR antagonist 1 1818885-54-9
    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-130813
    BET-IN-6 2570470-39-0
    BET-IN-6 is a potent and high affnity BRD2/BRD4 inhibitor. BET-IN-6 is the ligand for target protein BRD2/4, and is used for the systhesis of PROTAC BRD2/BRD4 degrader-1 (HY-130612).
    BET-IN-6
  • HY-125908
    A-1210477-piperazinyl 2351218-72-7
    A-1210477-piperazinyl is a compound binds to protein myeloid cell leukemia 1 (MCL1) used for PROTAC technology.
    A-1210477-piperazinyl
  • HY-134592
    Piperidine-GNE-049-N-Boc 1936431-36-5 98.82%
    Piperidine-GNE-049-N-Boc is a ligand for target protein for PROTAC of dCBP-1 (HY-134582). dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.
    Piperidine-GNE-049-N-Boc
  • 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