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
T16208	N-Boc-N-bis(PEG4-OH)	N-Boc-N-bis(PEG4-OH) is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T18526	PDB-Pfp	PDB-Pfp is a reducible ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
T14455	Azido-PEG5-Ala-Ala-Asn-PAB	Azido-PEG5-Ala-Ala-Asn-PAB is a cleavable 5-unit polyethylene glycol (PEG) linker employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T17547	Biotin-C10-NHS Ester	Biotin-C10-NHS Ester is an alkyl/ether-based linker compound utilized in the synthesis of PROTACs[1].
T16191	N-(Azido-PEG3)-N-Fluorescein-PEG3-acid	N-(Azido-PEG3)-N-Fluorescein-PEG3-acid is a PEGylated PROTAC linker incorporating azide, fluorescein, and carboxylic acid functional groups.
T17746	DBCO-C3-PEG4-amine	DBCO-C3-PEG4-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.
T14754	Boc-NH-PEG7-acid	Boc-NH-PEG7-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.
T18049	Ibrutinib-biotin	Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, has an IC50 of 0.755-1.02 nM for BTK.
T14654	Bis-propargyl-PEG12	Bis-propargyl-PEG12 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.
T18532	PEG20-Tos	PEG20-Tos 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.
T14660	Bis-propargyl-PEG7	Bis-propargyl-PEG7 is a polyethylene glycol (PEG)-based linker utilized in the synthesis of proteolysis targeting chimeras (PROTACs). It is particularly employed for the synthesis of polymer-linked multimers of guanosine-3',5'-cyclic monophosphates[1].
T18124	m-PEG11-azide	m-PEG11-azide 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.
T15330	Fmoc-PEG3-C2-NHS ester	Fmoc-PEG3-CH2CH2-NHS ester is a PEG-based linker derived from fluorenylmethoxycarbonyl (Fmoc), which is used as a moiety for the efficient synthesis of PROTACs (proteolysis-targeting chimeras)[1]. This compound offers a practical solution for connecting desired molecules and targeting specific proteins for degradation.
T15325	Fmoc-NH-PEG9-CH2CH2COOH	Fmoc-NH-PEG9-CH2CH2COOH is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs) [1].
T15084	Dde Biotin-PEG4-azide	Dde Biotin-PEG4-azide 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.
T18790	Tetrazine-PEG4-oxyamine hydrochloride	Tetrazine-PEG4-oxyamine (hydrochloride) is a cleavable 4-unit polyethylene glycol (PEG) linker, employed for the synthesis of antibody-drug conjugates (ADCs) [1].
T17933	endo-BCN-PEG12-NHS ester	Endo-BCN-PEG12-NHS ester is a polyethylene glycol (PEG) derivative used as a linker for ProTAC synthesis [1].
T18361	MMAE-SMCC	MMAE-SMCC is a drug-linker conjugate designed for antibody-drug conjugates (ADC). It consists of MMAE, a potent inhibitor of mitosis and tubulin, and SMCC, a linker that facilitates the development of ADCs.
T15871	m-PEG4-Boc	m-PEG4-Boc is a cleavable 4-unit polyethylene glycol (PEG) linker, widely employed in the synthesis of antibody-drug conjugates (ADCs) [1]. Additionally, m-PEG4-Boc serves as a PEG-based PROTAC linker, enabling its utilization in the synthesis of PROTACs [2].
T17559	Biotin-PEG12-hydrazide	Biotin-PEG12-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