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
T16455	PEG3-bis(phosphonic acid diethyl ester)	PEG3-bis(phosphonic acid diethyl ester) is a polyethylene glycol (PEG) derived linker specifically designed for use in the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T18511	OPSS-Val-Cit-PAB-OH	OPSS-Val-Cit-PAB-OH is an ADC linker utilized for the synthesis of antibody-drug conjugates (ADCs) [1].
T17578	Biotin-PEG36-PFP ester	Biotin-PEG36-PFP 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.
T18625	Boc-NH-C6-amido-C4-acid	Boc-NH-C6-amido-C4-acid (PROTAC Linker 32) is an alkyl ether-based linker extensively employed in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].
T15928	m-PEG8-azide	m-PEG8-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.
T18780	TCO-PEG8-amine	TCO-PEG8-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.
T17479	Azido-PEG10-Boc	Azido-PEG10-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.
T18571	m-PEG12-2-methylacrylate	Propargyl-PEG13-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
T18718	SPP-DM1	SPP-DM1, a drug-linker conjugate for antibody-drug conjugates (ADC), demonstrates potent antitumor activity. It comprises DM1 (a potent microtubule-disrupting agent) connected through the ADC linker SPP[1].
T17907	Pomalidomide-amido-C4-amido-C6-NH-Boc	Pomalidomide-amido-C4-amido-C6-NH-Boc, a synthesized conjugate, is a ligand-linker incorporating the cereblon ligand based on Pomalidomide and a PROTAC technology linker.
T18835	Thiol-PEG10-alcohol	Thiol-PEG10-alcohol 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.
T17794	DBCO-PEG4-alcohol	DBCO-PEG4-alcohol 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.
T15333	Fmoc-PEG5-NHS ester	Fmoc-PEG5-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.
T17834	DM4-SPDP	DM4-SPDP, a drug-linker conjugate, integrates the antitubulin agent DM4 with the linker SMCC, facilitating the creation of antibody drug conjugates[1]. Additionally, SPDP serves as a short-chain crosslinker enabling amine-to-sulfhydryl conjugation, leveraging NHS-ester and pyridyldithiol groups to establish cleavable (reducible) disulfide bonds with cysteine sulfhydryls[2][3].
T17832	DM1-PEG4-DBCO	DM1-(PEG)4-DBCO is a drug-linker conjugate that combines the potent microtubulin inhibitor mertansine (DM1) with the DBCO-PEG4-Ahx linker for the development of antibody-drug conjugates (ADCs). This conjugation aims to mitigate the systemic toxicity associated with maytansine while improving tumor-specific delivery, leveraging DM1’s capabilities as an antibody-conjugatable maytansinoid.
T18487	NH2-C6-NH-Boc	NH2-C6-NH-Boc 是一种属于 alkyl/ether 类的 PROTAC linker ，是基于 PROTAC 技术的 Mcl-1 抑制剂。
T14009	2,2-Oxybis(ethylamine)	2,2-Oxybis(ethylamine) （2,2'-oxydiethanamine）是一种属于 PEG 类的 PROTAC linker，可用于合成 PROTAC 分子。
T15089	Decaethylene glycol	Decaethylene glycol (HO-PEG10-OH) 是一种属于 PEG 类的 PROTAC linker，可用于合成 PROTAC 分子。
T15175	DSP Crosslinker	DSP Crosslinker 是一种可降解的 ADC 连接剂，用于合成可用于合成抗体偶联药物。
T17653	Boc-NH-C4-acid	Boc-NH-C4-acid 是一种属于 Alkyl/ether 类的 PROTAC linker，可用于 PROTAC1 的合成，并且可以降解 PRC2 中的 EED，EZH2，和 SUZ12。

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PROTAC Linker