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
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。
T18466	N3-C3-NHS ester	N3-C3-NHS ester 是一种不可切割的 ADC 接头，用于合成抗体-药物偶联物。
T18546	(+)-Biotin-ONP	(+)-Biotin-ONP ((+)-Biotin 4-nitrophenyl ester) 是一种属于 alkyl chain 类的 PROTAC linker，可用于 PROTAC 分子的合成。
T18485	NH2-C4-NH-Boc	NH2-C4-NH-Boc 是一种属于 Alkyl/ether 类的 PROTAC linker，可用于一系列 PROTAC 分子的合成。
T18728	Sulfo-SMCC sodium	Sulfo-SMCC sodium 是一种异双功能、不可裂解的 ADC 交联剂，带有 N-羟基琥珀酰亚胺酯和马来酰亚胺基团，分别与伯胺和巯基反应。
T17352	Acid-C1-PEG5-Boc	Acid-C1-PEG5-Boc 是一种属于 PEG 类的 PROTAC linker，可用于 PROTAC 分子的合成。
T16302	NH-bis(PEG3-azide)	NH-bis(PEG3-azide) 是一种属于 PEG 类的 PROTAC 连接体，可用于合成 PROTAC 分子。
T17637	BM-PEG3	BM-PEG3 (1,11-Bis-maleimidotetraethyleneglycol) 是一种属于 PEG 类的 PROTAC linker，可用于 PROTAC 分子的合成。
T17014	TCO-NHS ester	TCO-NHS ester 是一种 PROTAC linker，属于 alkyl/ether 类。可用于合成 PROTAC 分子。

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PROTAC Linker