2. Signaling Pathways
  3. PROTAC
  4. Target Protein Ligand-Linker Conjugates

Target Protein Ligand-Linker Conjugates

Target Protein Ligand-Linker Conjugates

Related Products

PDF 0.2 MB

Target Protein Ligand-Linker Conjugate incorporates a ligand for the target protein and a linker. When binding to an E3 ligase ligand, the conjugate will be a PROTAC with ability to induce ubiquitylation and subsequent degradation the protein of interest.

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, transcription factors, epigenetic tools and E3 ligase themselves.

The optimal lengths of the PROTAC linkers are reported varying from 12-carbon to over 20-carbon, and the commonly used linkers in the development of PROTACs are PEGs, Alkyl-Chain and Alkyl/ether.

Target Protein Ligand-Linker Conjugates Related Products (115):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • 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 is a FAK (HY-43760) ligand and linker conjugate. BI-4464 can be used to construct proteolysis targeting chimeras (PROTACs), such as PROTAC FAK degrader 4 (HY-178467). PROTAC FAK degrader 4 is a highly potent and selective FAK PROTAC degrader.
    BI-4464
  • HY-49382
    Fluocinolone acetonide 3-benzylaniline 2166375-81-9 99.93%
    Fluocinolone acetonide 3-benzylaniline (Precursor Example 1) is a glucocorticoid receptor agonist-linker conjugate, which can be used for the synthesis of anti-CD40 antibody-drug conjugates (ADCs).
    Fluocinolone acetonide 3-benzylaniline
  • HY-107447
    N-Deshydroxyethyl Dasatinib 910297-51-7
    N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, Dasatinib is a multi-kinase inhibitor that potently inhibits Bcr-Abl, Src family and platelet-derived growth factor receptor kinases. N-Deshydroxyethyl Dasatinib can be used in cancer and immune disease research.
    N-Deshydroxyethyl Dasatinib
  • HY-174995
    JQ-1-Azidopropylamine 2915642-70-3 99.5700%
    JQ-1-Azidopropylamine is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 (HY-78695) and a PROTAC linker (HY-151862), which recruits E3 ligases. JQ-1-Azidopropylamine can be used for synthesis of PROTAC JY-21 (HY-174975).
    JQ-1-Azidopropylamine
  • HY-147090
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH 2750350-39-9 99.06%
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) incorporates a ligand for EZH2, and a PROTAC linker, which recruit E3 ligases. Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) can be used for the research of lymphoma.
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH
  • HY-181693
    CCW16-C2-Boc
    CCW16-C2-Boc is a conjugate targeting RNF4, formed by coupling the target protein ligand CCW16 (HY-143346) with a PROTAC Linker. CCW16-C2-Boc can be used to synthesize the PROTAC degrader: PROTAC RNF4 degrader-1 (HY-181693).
    CCW16-C2-Boc
  • HY-176950
    Crizotinib-amide-PEG2-NH2 3048497-52-2
    Crizotinib-amide-PEG2-NH2 is a MET ligand (HY-50878) linker conjugate. Crizotinib-amide-PEG2-NH2 can be used for synthesis of MET degrader OZD-MET 01 (HY-177893).
    Crizotinib-amide-PEG2-NH2
  • HY-179515
    FAK ligand-2-C6-amine 2414478-60-5
    FAK ligand-2-C6-amine is a target protein ligand linker conjugate that contains a FAK ligand (HY-151010) and a PROTAC linker (HY-W011561), which can recruit E3 ligases. FAK ligand-2-C6-amine can be used for synthesis of BSJ-04-146 (HY-179512).
    FAK ligand-2-C6-amine
  • HY-43521
    Ibrutinib-MPEA 1710768-30-1 99.71%
    Ibrutinib-MPEA is an orally active, blood-brain barrier permeable inhibitor of BTK and STAT5. As a derivative of Ibrutinib (HY-10997) conjugated with a PROTAC linker, Ibrutinib-MPEA allows the synthesis of a series of PROTAC molecules. Ibrutinib-MPEA significantly reduces the proliferation of neoplastic mast cells and primary mastocytoma cells by inducing apoptosis and inhibiting IgE-dependent histamine release. Ibrutinib-MPEA is applicable to the research of canine mast cell tumors, cerebral ischemia/reperfusion injury in diabetic mice, and neuroinflammation-related diseases.
    Ibrutinib-MPEA
  • HY-130991
    K-Ras ligand-Linker Conjugate 6 2378261-89-1
    K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
    K-Ras ligand-Linker Conjugate 6
  • HY-130499
    ERRα Ligand-Linker Conjugates 1 98.78%
    ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα), and a PROTAC linker, which recruit E3 ligases MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader.
    ERRα Ligand-Linker Conjugates 1
  • HY-131386A
    BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride 2691796-83-3
    BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used in the synthesis of PROTAC PD-1/PD-L1 degrader-1?(HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM.
    BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride
  • HY-131230
    Desmorpholinyl Quizartinib-PEG2-COOH 2292116-14-2
    Desmorpholinyl Quizartinib-PEG2-COOH incorporates a ligand for FLT-3, and a PEG-based PROTAC linker. Desmorpholinyl Quizartinib-PEG2-COOH can be used in the synthesis of PROTAC FLT-3 degrader 1 (HY-114323). PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM.
    Desmorpholinyl Quizartinib-PEG2-COOH
  • HY-44148
    FAK ligand-Linker Conjugate 1 2307461-45-4 98.91%
    FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation.
    FAK ligand-Linker Conjugate 1
  • HY-130823
    K-Ras ligand-Linker Conjugate 5 2378261-85-7 99.79%
    K-Ras ligand-Linker Conjugate 5 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 5 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
    K-Ras ligand-Linker Conjugate 5
  • HY-130707
    K-Ras ligand-Linker Conjugate 3 2378261-87-9
    K-Ras ligand-Linker Conjugate 3 (Compound 001371) incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
    K-Ras ligand-Linker Conjugate 3
  • HY-170987
    FKBP12 Ligand-Linker Conjugate 1 2765059-01-4
    FKBP12 Ligand-Linker Conjugate 1 is the conjugate composed of a target protein ligand for FKBP12 and a linker. FKBP12 Ligand-Linker Conjugate 1 can be used for synthesis of PROTAC degrader MC-25B (HY-170983).
    FKBP12 Ligand-Linker Conjugate 1
  • HY-175360
    USP7 Ligand-Linker Conjugates 1 3098774-65-0 99.92%
    USP7 Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for USP7 (HY-175359) and a PROTAC linker, which recruits E3 ligases. USP7 Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC USP7 Degrader-1 (HY-175358).
    USP7 Ligand-Linker Conjugates 1
  • HY-141486
    (Rac)-PROTAC PARP/EGFR ligand 1 2935073-36-0
    (Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP.
    (Rac)-PROTAC PARP/EGFR ligand 1
  • HY-129776
    K-Ras ligand-Linker Conjugate 2 2741300-61-6
    K-Ras ligand-Linker Conjugate 2 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 2 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
    K-Ras ligand-Linker Conjugate 2