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.
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Target Protein Ligand-Linker Conjugates Related Products (121)
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BI-4464
0 ImagesBI-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. -
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N-Deshydroxyethyl Dasatinib
0 ImagesCat. No.: HY-107447CAS No.: 910297-51-7Synonyms: N-Deshydroxyethyl BMS-354825N-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. -
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- Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH
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- JQ-1-Azidopropylamine
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Ibrutinib-MPEA
0 ImagesCat. No.: HY-43521CAS No.: 1710768-30-1Ibrutinib-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. -
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- Asciminib-NH2
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Palbociclib-PEG3-NHBoc
0 ImagesCat. No.: HY-184538CAS No.: 2361493-13-0Palbociclib-PEG3-NHBoc is a target protein ligand-linker conjugate. Palbociclib-PEG3-NHBoc can be used for the synthesis of PROTAC BSJ-03-123 (HY-111556). -
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ALK protein ligand-1-PEG2-N3
0 ImagesCat. No.: HY-184541CAS No.: 2229036-85-3 -
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K-Ras ligand-Linker Conjugate 6
0 ImagesCat. No.: HY-130991CAS No.: 2378261-89-1K-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. -
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ERRα Ligand-Linker Conjugates 1
0 ImagesCat. No.: HY-130499Purity: 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. -
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BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride
0 ImagesCat. No.: HY-131386ACAS No.: 2691796-83-3BMS-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. -
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- USP7 Ligand-Linker Conjugates 1
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Desmorpholinyl Quizartinib-PEG2-COOH
0 ImagesCat. No.: HY-131230CAS No.: 2292116-14-2Desmorpholinyl 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. -
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- FAK ligand-Linker Conjugate 1
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K-Ras ligand-Linker Conjugate 5
0 ImagesK-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. -
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K-Ras ligand-Linker Conjugate 3
0 ImagesCat. No.: HY-130707CAS No.: 2378261-87-9K-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. -
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- MC-Val-Cit-PAB-Sunitinib
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- FKBP12 Ligand-Linker Conjugate 1
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(Rac)-PROTAC PARP/EGFR ligand 1
0 ImagesCat. No.: HY-141486CAS No.: 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. -
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K-Ras ligand-Linker Conjugate 2
0 ImagesCat. No.: HY-129776CAS No.: 2741300-61-6K-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. -
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