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 (186):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-13030
    (+)-JQ-1 1268524-70-4 99.90%
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
    (+)-JQ-1
  • HY-10997
    Ibrutinib 936563-96-1 99.97%
    Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
    Ibrutinib
  • HY-13001
    Quizartinib 950769-58-1 99.01%
    Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis.
    Quizartinib
  • HY-12870
    AZD9496 1639042-08-2 99.40%
    AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally bioavailable selective oestrogen receptor degrader (SERD), served as one of Ligands for Target Protein for PROTAC.
    AZD9496
  • HY-129603
    SI-109 2429877-30-3 99.91%
    SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36.
    SI-109
  • HY-W453397
    Aberrant tau ligand 1 1892461-96-9 ≥98.0%
    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-153918A
    (S)-SKBG-1 2955618-24-1 99.01%
    (S)-SKBG-1 is an inactive and covalent NONO ligand, used for assay control..
    (S)-SKBG-1
  • HY-163926
    SMARCA2/4-IN-2 1339378-93-6 99.27%
    SMARCA2/4-IN-2 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). SMARCA2/4-IN-2 can be used for synthesis PROTAC SMARCA2/4-degrader-5 (HY-159456).
    SMARCA2/4-IN-2
  • HY-114872
    SLF 195513-96-3 99.91%
    SLF is a synthetic ligand for FK506-binding protein (FKBP) with an affinity of 3.1 μM for FKBP51 and an IC50 of 2.6 μM for FKBP12. SLF can be used in the synthesis of PROTAC.
    SLF
  • HY-158101
    BMS-986365 2446928-30-7 99.92%
    BMS-986365 (CC-94676) is an orally active and selective heterobifunctional PROTAC ligand-directed degrader that targets androgen receptors (AR). BMS-986365 demonstrated significant in vivo potency, degrading AR, inhibiting AR signaling, and inhibiting tumor growth in animal models of advanced prostate cancer.
    BMS-986365
  • HY-133017
    Amcenestrant 2114339-57-8 99.79%
    SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonsit (EC50=0.2 nM), belonging to Ligands for Target Protein for PROTAC. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER+ breast cancer.
    Amcenestrant
  • HY-136242
    UT-34 2168525-92-4 98.61%
    UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR, belonging to Ligands for Target Protein for PROTAC. UT-34 has anti-prostate cancer efficacy.
    UT-34
  • HY-133073
    CCR7 Ligand 1 681514-83-0 99.62%
    CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM.
    CCR7 Ligand 1
  • HY-129939
    PROTAC BRD4 ligand-1 2313230-51-0 99.85%
    PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT GNE-987 (HY-129937A).
    PROTAC BRD4 ligand-1
  • HY-107443
    I-BET762 carboxylic acid 1300019-38-8 99.55%
    I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.
    I-BET762 carboxylic acid
  • HY-126534A
    Abemaciclib metabolite M18 hydrochloride 2704316-82-3 98.01%
    Abemaciclib metabolite M18 (LSN3106729) hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.
    Abemaciclib metabolite M18 hydrochloride
  • HY-138539
    CBP/p300 ligand 2 2484741-78-6 98.17%
    CBP/p300 ligand 2 is a ligand for target protein for PROTAC of dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.
    CBP/p300 ligand 2
  • HY-44432
    Navitoclax-piperazine 2143096-93-7 99.73%
    Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor. Navitoclax-piperazine and a VHL ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC DT2216 (HY-130604) with anti-tumor activity.
    Navitoclax-piperazine
  • HY-114420
    AP1867-2-(carboxymethoxy) 2230613-03-1 99.85%
    AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules.
    AP1867-2-(carboxymethoxy)
  • HY-107452
    SLF-amido-C2-COOH 1092369-24-8 99.82%
    SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) is a synthetic ligand for FKBP (SLF). SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) can be used in the synthesis of PROTACs.
    SLF-amido-C2-COOH