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
T18584	Propargyl-PEG4-S-PEG4-Boc	Propargyl-PEG4-S-PEG4-Boc is a polyethylene glycol (PEG) based linker, specifically designed for the synthesis of PROTACs [1].
T17436	Amino-PEG6-amido-bis-PEG5-N3	Amino-PEG6-amido-bis-PEG5-N3 is a cleavable 11-unit polyethylene glycol (PEG) linker that finds application in the synthesis of antibody-drug conjugates (ADCs) [1].
T17841	DNP-PEG6-Boc	DNP-PEG6-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.
T14102	Acid-PEG3-mono-methyl ester	Acid-PEG3-mono-methyl ester, an alkyl/ether-based PROTAC linker, facilitates the synthesis of PROTACs[1].
T14632	Bis-PEG2-NHS ester	Bis-PEG2-NHS ester, utilized in antibody-drug conjugation (ADC), functions as a non-cleavable linker with two polyethylene glycol (PEG) units.
T18638	Boc-C5-O-C5-O-C6-Cl	Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a chemical compound commonly employed as a linker in PROTAC applications. Its primary function is to connect a specific tyrosine kinase inhibitor (TKI) with the E3 recruiting ligand.
T16639	Propargyl-PEG6-acid	Propargyl-PEG6-acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T17573	Biotin-PEG3-aldehyde	Biotin-PEG3-aldehyde is a three-unit PEG linker with cleavable properties, specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1].
T18397	N'-Boc-N-(Gly-Oleoyl)-Lys	N'-Boc-N-(Gly-Oleoyl)-Lys is an alkyl chain-derived proteolysis targeting chimera (PROTAC) linker suitable for PROTAC synthesis [1].
T17962	Fmoc-N-PEG36-acid	Fmoc-N-amido-PEG36-acid is a polyethylene glycol (PEG)-based linker utilized in PROTAC synthesis. It has been designed specifically for constructing PROTACs, which are bifunctional molecules capable of recruiting target proteins to an E3 ubiquitin ligase for degradation[1].
T18333	mDPR(Boc)-Val-Cit-PAB	mDPR(Boc)-Val-Cit-PAB is a cleavable linker employed in antibody-drug conjugates (ADCs) [1]. This chemical compound serves as a reliable linker in the formation of ADCs, which are biopharmaceuticals that combine the specificity of monoclonal antibodies with the potency of cytotoxic drugs for targeted cancer therapy [1].
T17889	cIAP1 Ligand-Linker Conjugates 14	cIAP1 Ligand-Linker Conjugates 14 consist of an IAP ligand that targets the E3 ubiquitin ligase and a PROTAC linker. These conjugates, known as cIAP1 Ligand-Linker Conjugates 14, are used in the development of SNIPERs[1].
T17828	Diketone-PEG4-Biotin	Diketone-PEG4-Biotin 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.
T15293	Fluorescein-PEG4-acid	Fluorescein-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.
T17696	BRD7-IN-1 free base	BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), interacts with a VHL ligand through a linker, constituting the PROTAC VZ185 (targeting BRD7/9 with DC50 values of 4.5 and 1.8 nM, respectively)[1].
T17398	Amine-PEG-thiol (MW 2000)	Amine-PEG-thiol (MW 2000) is a PEG-based PROTAC linker employed in PROTAC synthesis[1].
T15869	m-PEG4-amino-Mal	m-PEG4-amino-Mal 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.
T18359	Methyltetrazine-SS-PEG4-Biotin	Methyltetrazine-SS-PEG4-Biotin is a cleavable four-unit polyethylene glycol (PEG) linker employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T16692	Pyrene-amido-PEG4-CH2CH2COOH	Pyrene-amido-PEG4-CH2CH2COOH is a polyethylene glycol (PEG) derived linker, designed specifically for constructing proteolysis targeting chimeras (PROTACs)[1].
T18190	m-PEG36-alcohol	m-PEG36-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.

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PROTAC Linker