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PROTACTarget Protein Ligand-Linker Conjugate
Target Protein Ligand-Linker Conjugate is the name given to the target protein ligand and linker when they are joined together. When this ligand binds to an E3 ligase, it induces ubiquitination of the target protein thereby having the ability to degrade the protein of interest. Target proteins are usually proteins that are overexpressed or accumulate in disease, and de-riveting these aberrant proteins by target proteins can either degrade these proteins or inhibit the function of these proteins, and have been developed to include kinases, transcription factors, epigenetic tools, and E3 ligases themselves. Optimal lengths of PROTAC linkers have been reported to vary from 12-20 carbons, and PEGs, Alkyl-Chain and Alkyl/ether are commonly used as linkers for PROTACs.
SLF
T13888195513-96-3
SLF is a synthetic ligand for FKBP12, which increases Ca2+ efflux and protein synthesis to improve skeletal muscle function, and is used in the study of central nervous system diseases and cancer.
- $99
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K-Ras ligand-Linker Conjugate 4
T180572378261-83-5
K-Ras ligand-Linker Conjugate 4 is a chemical compound combining a K-Ras recruiting ligand with a PROTAC linker, responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. It has the potential to be used in synthesizing PROTAC K-Ras Degrader-1, which shows a degradation efficacy of ≥70% in SW1573 cells[1].
- $75
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DDR1 ligand 1-piperidine
T2072853081612-71-4
DDR1ligand 1-piperidine is a conjugate of a target protein ligand and linker, utilized in the synthesis of PROTAC DDR1 degrader-1.
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EN884
T2083332189497-60-5
EN884 is a BRD4 degrader that functions through an SKP1 and proteasome-dependent degradation pathway. It is utilized in the synthesis of proteolysis-targeting chimeras (PROTAC).
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SMARCA2 ligand-12-3-methylazetidine
T203685
SMARCA2 ligand-12-3-methylazetidin is a target protein ligand-linker conjugate that includes a ligand for SMARCA2 and a PROTAC linker, capable of recruiting E3 ligase. It is utilized in the synthesis of PROTAC SMARCA2 degrader-25.
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K-Ras ligand-Linker Conjugate 5
T180582378261-85-7
K-Ras ligand-Linker Conjugate 5 is a chemical compound combining a K-Ras recruiting ligand with a PROTAC linker for E3 ligases, such as VHL, CRBN, MDM2, and IAP. This conjugate is crucial for synthesizing PROTAC K-Ras Degrader-1, displaying a degradation efficacy of ≥70% in SW1573 cells [1].
- $85
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FAK ligand-Linker Conjugate 1
T179432307461-45-4
FAK ligand-Linker Conjugate 1 is a chemical compound designed to facilitate PROTAC-mediated protein degradation. This compound consists of a ligand specifically targeting FAK and a PROTAC linker module, which acts as a recruitment agent for E3 ligases including VHL, CRBN, MDM2, and IAP[1].
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Ahx-DM1 TFA
T2082071702356-22-6
Ahx-DM1 (TFA) (compound 2A) is a conjugate of proteins/peptides that can combine with therapeutic, diagnostic, or labeling agents.
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KDM4 Ligand-Linker Conjugate 1
T206221
KDM4Ligand-Linker Conjugate 1 is a conjugate comprising a KDM4 target protein ligand and a linker, used in the synthesis of PROTACKDM4 degrader-1.
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K-Ras ligand-Linker Conjugate 1
T18054
K-Ras ligand-Linker Conjugate 1 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, facilitating the recruitment of E3 ligases VHL, CRBN, MDM2, and IAP. It can be utilized in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells [1].
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Ahx-DM1
T2082061702356-21-5
Ahx-DM1 (compound 2A) is a conjugate of proteins/peptides that can be combined with therapeutic, diagnostic, or labeling agents.
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PROTAC SMARCA2 degrader-1
T2082472892523-73-6
PROTACSMARCA2 degrader-1 (compound ex7) is a potent BRM (SMARCA2) degrader with a DC50 of less than 0.1 μM. It functions as a linker for E3 ubiquitin ligase, making it useful in cancer research, and is a conjugate of a target protein ligand and linker.
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MS1262-C3-amide-C10-amine
T206748
MS1262-C3-amide-C10-amine is an E3 Ligase Ligand-Linker conjugate. It includes a GLP ligand targeting the E3 ligase SPOP and a PROTAC linker. This compound can be utilized in designing PROTACs such as example [MS479].
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(Rac)-PROTAC PARP/EGFR ligand 1
T2081772935073-36-0
(Rac)-PROTAC PARP/EGFR ligand 1 is a compound that includes ligands for target proteins PARP and EGFR, along with a PROTAC linker that recruits E3 ligases such as VHL, CRBN, MDM2, and IAP. It is utilized in the synthesis of PROTAC DP-C-4, a dual CRBN-based PROTAC designed for the concurrent degradation of EGFR and PARP.
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FKBP12 Ligand-Linker Conjugate 2
T206397
FKBP12 Ligand-Linker Conjugate 2 is a conjugate composed of an FKBP12 target protein ligand and a linker. It is utilized in the synthesis of FKBP12PROTACFM4.
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K-Ras ligand-Linker Conjugate 3
T180562378261-87-9
K-Ras ligand-Linker Conjugate 3 (Compound 001371) is a chemical compound comprising a ligand for the K-Ras recruiting moiety and a PROTAC linker, responsible for recruiting E3 ligases (e.g., VHL, CRBN, MDM2, and IAP). This compound is essential for synthesizing PROTAC K-Ras Degrader-1, a potent degrader with a degradation efficacy of ≥70% in SW1573 cells[1].
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ERRα Ligand-Linker Conjugates 1
T17941
ERRα Ligand-Linker Conjugates 1 refers to a chemical compound that consists of a ligand targeting estrogen-related receptor alpha (ERRα), and a PROTAC linker that facilitates the recruitment of E3 ligases MDM2. It finds utility in the synthesis of a range of PROTACs, including one known as PROTAC ERRalpha Degrader-1. With its capability to induce degradation of ERRα, PROTAC ERRalpha Degrader-1 functions as an ERRα degrader[1].
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K-Ras ligand-Linker Conjugate 2
T18055
K-Ras ligand-Linker Conjugate 2 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in synthesizing PROTAC K-Ras Degrader-1, a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1].
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