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

Target Protein Ligand-Linker Conjugates

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 (114):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-131386
    BMS-1166-N-piperidine-CO-N-piperazine 2447066-14-8
    BMS-1166-N-piperidine-CO-N-piperazine incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine 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
  • HY-129775
    K-Ras ligand-Linker Conjugate 1 2749492-84-8
    K-Ras ligand-Linker Conjugate 1 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 1 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 1
  • HY-130822
    K-Ras ligand-Linker Conjugate 4 2378261-83-5 98.76%
    K-Ras ligand-Linker Conjugate 4 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 4 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 4
  • HY-171159
    MC-Val-Cit-PAB-Sunitinib
    MC-Val-Cit-PAB-Sunitinib is the conjugate of a payload Sunitinib (HY-10255A) and a linker. MC-Val-Cit-PAB-Sunitinib can be used for synthesis of HR97-Sunitinib.
    MC-Val-Cit-PAB-Sunitinib
  • HY-169490
    SMARCA2 ligand-13 PYR-Pip-spiro[3.3]heptane-acid
    SMARCA2 ligand-13 PYR-Pip-spiro[3.3]heptane-acid is a conjugate generated by linking a target protein ligand (HY-44824) to a linker (HY-169489). SMARCA2 ligand-13 PYR-Pip-spiro[3.3]heptane-acid can be used in the synthesis of PROTACs (e.g. PROTAC SMARCA2 degrader-21 (HY-169272)).
    SMARCA2 ligand-13 PYR-Pip-spiro[3.3]heptane-acid
  • HY-176918
    K-Ras ligand-Linker Conjugate 8
    K-Ras ligand-Linker Conjugate 8 is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for KRAS (HY-162960) and a PROTAC linker, which recruits E3 ligases. K-Ras ligand-Linker Conjugate 8 can be used for synthesis of PROTAC KRAS(on) degrader ACBI-4 (HY-176792).
    K-Ras ligand-Linker Conjugate 8
  • HY-176391
    Ad-JQ1 2497485-14-8
    Ad-JQ1 (Compound 16) is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 (HY-78695) and a PROTAC linker (HY-176390), which recruits E3 ligases. Ad-JQ1 can be used for synthesis of PROTAC β-NF-JQ1 (HY-130256).
    Ad-JQ1
  • HY-176187
    DDR1 ligand 1-piperidine 3081612-71-4
    DDR1 ligand 1-piperidine is a target protein ligand and linker conjugate, which can be used for the synthesis of PROTAC DDR1 degrader-1 (HY-176184).
    DDR1 ligand 1-piperidine
  • HY-176788
    EGFR Ligand-Linker Conjugates 1 2768472-86-0
    EGFR Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for EGFR (HY-150905) and a PROTAC linker, which recruits E3 ligases. EGFR Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC EGFR degrader 3 (HY-144605).
    EGFR Ligand-Linker Conjugates 1
  • 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-176335
    TBK1 ligand 2-C-O-C4-O-C3-O-C-amide 2052306-12-2
    TBK1 ligand 2-C-O-C4-O-C3-O-C-amide is a conjugate of TBK1 ligand and linker, which can be used in the synthesis of PROTAC TBK1 degrader-2 (HY-112557).
    TBK1 ligand 2-C-O-C4-O-C3-O-C-amide
  • HY-147050
    Ahx-DM1 1702356-21-5
    Ahx-DM1 (compound 2A) is a conjugate of protein/peptide which can be combined with a therapeutic, diagnostic or labelling agent.
    Ahx-DM1
  • HY-130991A
    K-Ras ligand-Linker Conjugate 6 formate 98.93%
    K-Ras ligand-Linker Conjugate 6 formate 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 formate 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 formate
  • HY-178046
    OSBP ligand-Linker Conjugate 1
    OSBP ligand-Linker Conjugate 1 is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for OSBP (HY-178035) and a PROTAC linker, which recruits E3 ligases. OSBP ligand-Linker Conjugate 1 can be used for synthesis of PROTAC OSBP Degrader-1 (HY-178034).
    OSBP ligand-Linker Conjugate 1
  • HY-183017
    N-Descyclopropanecarbaldehyde olaparib-CO-C9-NHBoc 2925181-85-5
    N-Descyclopropanecarbaldehyde olaparib-CO-C9-NHBoc (Compound 6h) is a target protein ligand-linker conjugate that can be used for the synthesis of PROTACs, such as PROTAC PARP2 degrader-1 (HY-183013).
    N-Descyclopropanecarbaldehyde olaparib-CO-C9-NHBoc
  • HY-178361
    Remodelin-C6-COOH 2966791-35-3
    Remodelin-C6-COOH is a synthesized target protein ligand-linker conjugate that can be used for synthesis of NP1192 (HY-178360). NP1192 is a potent NAT10 PROTAC degrader with anti-tumor activity.
    Remodelin-C6-COOH
  • HY-172067
    ER ligand-9 3026011-20-8
    ER ligand-9 is a conjugate of an estrogen receptor (Estrogen Receptor/ERR) and a linker, which can be used to synthesize PROTAC ERD-1233 (HY-169367).
    ER ligand-9
  • HY-175268
    PXR ligand-Linker Conjugate 1
    PXR ligand-Linker Conjugate 1 is a conjugate of PXR ligand and linker, which can be used to synthesize PROTAC MI1013 (HY-175266).
    PXR ligand-Linker Conjugate 1
  • HY-175860
    KRAS G12D ligand-Linker Conjugate 2
    KRAS G12D ligand-Linker Conjugate 2 is a conjugate of the KRAS (G12D) ligand (HY-175859) and the linker (HY-168698). KRAS G12D ligand-Linker Conjugate 2 can be used for synthesizing PROTAC KRAS (G12D) degrader ASP-3082 (HY-157505).
    KRAS G12D ligand-Linker Conjugate 2
  • HY-176365
    Palbociclib-C4-Boc 2139329-48-7
    Palbociclib-C4-Boc is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for CDK4/6 Palbociclib (HY-50767) and a PROTAC linker (HY-W007803), which recruits E3 ligases. Palbociclib-C4-Boc can be used for synthesis of PROTAC BSJ-03-204 (HY-136250).
    Palbociclib-C4-Boc