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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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VUBI1-octanoic acid
T212169
VUBI1-octanoic acid is a conjugate of both the SOS1 ligand and linker, and it is applied in the synthesis of (4S)-PROTAC SOS1 degrader-1.
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N-Deshydroxyethyl Dasatinib-C3-NH2
N-Deshydroxyethyl BMS-354825-C3-NH2
T2117191430089-58-9
N-Deshydroxyethyl Dasatinib-C3-NH2 is a target protein ligand-linker conjugate, comprising an LCK ligand and a PROTAC linker, designed to recruit E3 ligase. It is utilized in the synthesis of [PROTACSJ11646].
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BRAF ligand-Linker Conjugate 1
T2120723094183-96-4
BRAF ligand-Linker Conjugate 1 is a target protein ligand-linker conjugate used for synthesizing PROTACCST905.
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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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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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HPK1 ligand 3-dimethylph tetrahydropyridine
T211091
HPK1 ligand 3-dimethylph tetrahydropyridine is a Target Protein Ligand-Linker Conjugate. It is utilized in the synthesis of PROTACHPK1 Degrader-4.
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HDAC6 ligand-Linker Conjugate 1
T211301
HDAC6ligand-Linker Conjugate 1 is a conjugate of the ligand and linker for HDAC6 (Target Protein Ligand-Linker Conjugate) and can be utilized in the synthesis of PROTACs such as PROTACHDAC6 degrader5.
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USP7 Ligand-Linker Conjugates 1
T211917
USP7Ligand-Linker Conjugates 1 is a Target Protein Ligand-Linker Conjugate comprising a USP7 ligand and a PROTAC linker, capable of recruiting E3 ligase. It is utilized in the synthesis of PROTACUSP7 Degrader-1.
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3-Fluoro-desmethyl-cabozantinib-C3-O-C3-PEG-acid
T2123662230826-10-3
3-Fluoro-desmethyl-cabozantinib-C3-O-C3-PEG-acid is a target protein ligand-linker conjugate combining a c-Met ligand with a PROTAC linker to recruit E3 ligase. It is applicable for synthesizing PROTACs, such as SJF-8240.
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Ad-JQ1
T2120542497485-14-8
Ad-JQ1 (Compound 16) is a Target Protein Ligand-Linker Conjugate incorporating a BRD4 ligand and a PROTAC linker capable of recruiting E3 ligase. It is utilized in the synthesis of PROTACβ-NF-JQ1.
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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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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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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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K-Ras ligand-Linker Conjugate 6 formate
T212098
K-Rasligand-Linker Conjugate 6 formate includes a target protein K-Ras ligand (K-Ras recruitment motif) and a PROTAC linker, capable of recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. It is utilized in synthesizing PROTACK-Ras Degrader-1, a potent PROTACK-Ras degrader, achieving a K-Ras degradation rate of ≥70% in SW1573.
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PXR ligand-Linker Conjugate 1
T211944
PXR ligand-Linker Conjugate 1 is a conjugate of a PXR ligand and a linker, suitable for synthesizing [PROTACMI1013].
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c-Met ligand-Linker Conjugate 1
T212090
c-Met ligand-Linker Conjugate 1 is a Target Protein Ligand-Linker Conjugate that consists of a c-Met ligand and a PROTAC linker, capable of recruiting E3 ligase. This compound is used in the synthesis of PROTACc-Met degrader-5.
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308-R-C4-PEG3-C1-Boc
T2121002376722-89-1
308-R-C4-PEG3-C1-Boc is an SGK3 ligand-linker conjugate, utilized in the synthesis of PROTAC SGK3 degrader-2.
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