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
T18113	m-PEG-Tresyl (MW 5000)	m-PEG-Tresyl (MW 5000) 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.
T15989	Mal-PEG4-acid	Mal-PEG4-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.
T18299	Mal-PEG8-Val-Cit-PAB-MMAE	Mal-PEG8-Val-Cit-PAB-MMAE is a cleavable 8-unit PEG ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T18251	MAL-di-EG-Val-Cit-PAB-MMAF	MAL-di-EG-Val-Cit-PAB-MMAF refers to a chemical compound that comprises the linker (MAL-di-EG-Val-Cit-PAB) and the potent blocker of tubulin polymerization (MMAF, Monomethyl auristatin F)[1].
T13990	1,3-Bis-aminooxy propane	1,3-Bis-aminooxy propane is an alkyl chain-derived PROTAC linker utilized for synthesizing PROTACs[1].
T18652	RTC-30	RTC-30 is an optimized phenothiazine compound possessing potent anti-cancer properties. It is formulated with a hydroxylated linker (N) which enhances its oral bioavailability[1].
T17141	Tos-PEG9	Tos-PEG9 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.
T18322	MC-Val-Cit-PAB-clindamycin	MC-Val-Cit-PAB-clindamycin is an antibody-drug conjugate (ADC) linker that combines the potent antitumor properties of clindamycin, a protein synthesis inhibitor, with the ADC linker MC-Val-Cit-PAB, to enhance its ability to target and kill cancer cells effectively.
T16316	NH2-PEG6-CH2CH2COOH	NH2-PEG6-CH2CH2COOH is a cleavable 6-unit PEG ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs) [1].
T17084	THP-PEG6-OH	THP-PEG6-OH is a polyethylene glycol (PEG)-based PROTAC linker, utilized in the synthesis of PROTACs[1]. It is also a non-cleavable three-unit PEG linker for antibody-drug conjugates (ADCs)[2].
T15522	Hydroxy-PEG3-acrylate	Hydroxy-PEG3-acrylate 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.
T14712	Boc-Aminooxy-PEG3-acid	Boc-Aminooxy-PEG3-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.
T15929	m-PEG8-Br	m-PEG8-Br 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.
T17767	DBCO-NHCO-PEG2-NHS ester	DBCO-NHCO-PEG2-NHS ester, a PEG-based PROTAC linker, enables the synthesis of PROTACs[1].
T14099	Acid-PEG2-C2-Boc	Acid-PEG2-C2-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.
T17380	Ald-Ph-amido-PEG1-C2-Pfp ester	Ald-Ph-amido-PEG1-C2-Pfp ester is a non-cleavable 1-unit PEG linker employed in antibody-drug conjugation (ADC) to connect antibodies with drugs.
T18237	Mal-amido-PEG12-NHS ester	Mal-amido-PEG12-NHS ester is a polyethylene glycol (PEG)-derived linker for proteolysis-targeting chimeras (PROTACs)[1]. It is employed in the synthesis of PROTACs, enabling the conjugation of desired target-specific ligands for protein degradation[1].
T18708	SPDP-C6-Gly-Leu-NHS ester	SPDP-C6-Gly-Leu-NHS ester is a cleavable linker employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T16203	N-Boc-N-bis(C2-PEG1-azide)	N-Boc-N-bis(C2-PEG1-azide) is an alkyl/ether-based PROTAC linker suitable for synthesizing PROTACs[1].
T18087	m-PEG-CH2COOH (MW 2000)	m-PEG-CH2COOH (MW 2000) is a PEG-based PROTAC linker, suitable for synthesizing PROTACs[1].

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PROTAC Linker