PROTAC Linker

The length and composition of the linker play critical roles in the physicochemical properties and bioactivity of PROTACs. While linker design has historically received limited attention, the PROTAC field is evolving rapidly and undergoing an important shift from synthetically tractable alkyl and polyethylene glycol to more sophisticated functional linkers. Equally important, linker-mediated binding cooperativity also represents a potential source of affinity for the POI for PROTACs based on weak affinity warheads. However, the current consensus is that the linker composition, and particularly its length and attachment point to the anchor/warhead, must be optimized for each ligand pair.

产品编号	产品名称
T14242	Amino-PEG4-hydrazide-Boc	Amino-PEG4-hydrazide-Boc is a PEGylation-based linker employed for the synthesis of PROTACs[1].
T18140	m-PEG12-Mal	m-PEG12-Mal is a PEG-based PROTAC linker suitable for the synthesis of PROTACs[1].
T16061	Methyltetrazine-PEG8-acid	Methyltetrazine-PEG8-acid is a polyethylene glycol (PEG) derivative commonly employed as a linker in the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T17129	Tos-PEG3	Tos-PEG3, a PEG-based PROTAC linker, is suitable for synthesizing PROTACs and 3'-aminooxy oligonucleotide solid supports[1].
T18412	N-Desthiobiotin-N-bis(PEG4-NHS ester)	N-Desthiobiotin-N-bis(PEG4-NHS ester) is a polyethylene glycol (PEG) derived linker used for synthesizing PROTACs[1].
T14414	Azido-PEG10-amine	Azido-PEG10-amine is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T17233	Vipivotide tetraxetan Linker	Vipivotide tetraxetan Linker (PSMA-617 Linker) is a noncleavable peptide linker utilized in the synthesis of Vipivotide tetraxetan (PSMA-617), a ligand instrumental in producing 177Lu-PSMA-617. This radioactive molecule is applied in the treatment of prostate cancer[1].
T18679	SC-VC-PAB-MMAE	SC-VC-PAB-MMAE is a potent antitumor drug-linker conjugate for antibody-drug conjugates (ADCs), comprising the anti-mitotic agent monomethyl auristatin E (MMAE, a tubulin inhibitor) connected through the cleavable linker SC-VC-PAB[1].
T16175	N-(Aminooxy-PEG3)-N-bis(PEG4-Boc)	N-(Aminooxy-PEG3)-N-bis(PEG4-Boc) is a polyethylene glycol (PEG)-based linker primarily utilized in PROTAC synthesis for the development of proteolysis-targeting chimeras (PROTACs)[1].
T18799	Tetrazine-Ph-OPSS	Tetrazine-Ph-OPSS is an ADC linker employed for synthesizing ADCs, or antibody-drug conjugates [1].
T18472	N3-PEG3-Propanehydrazide	N3-PEG3-Propanehydrazide serves as a PEG-based PROTAC linker, employed for PROTAC synthesis [1].
T16828	S-Acetyl-PEG8-OH	S-Acetyl-PEG8-OH is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T18027	HS-PEG7-CH2CH2COOH	HS-PEG7-CH2CH2COOH is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T14762	Boc-PEG4-sulfonic acid	Boc-PEG4-sulfonic acid is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T17904	Pomalidomide-PEG1-C2-N3	Pomalidomide-PEG1-C2-N3 is a compound that has been synthesized as a conjugate of an E3 ligase ligand-linker. This compound incorporates the cereblon ligand based on Pomalidomide and a 1-unit PEG linker, which are commonly used in PROTAC technology. Utilizing Pomalidomide-PEG1-C2-N3, it is possible to design a selective CDK6 PROTAC degrader known as CP-10. CP-10 effectively induces the degradation of CDK6, displaying a DC50 value of 2.1 nM[1].
T17121	Tos-PEG1-CH2-Boc	Tos-PEG1-CH2-Boc is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T17553	Biotin-PEG-triethoxysilane (MW 1000)	Biotin-PEG-triethoxysilane (MW 1000) is a PEG-based PROTAC linker utilized for the synthesis of PROTACs[1].
T18773	TCO-PEG4-DBCO	TCO-PEG4-DBCO is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T17480	Azido-PEG10-NHS ester	Azido-PEG10-NHS ester is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T18549	(+)-Biotin-PEG2-hydrazide	(+)-Biotin-PEG2-hydrazide is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

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PROTAC Linker