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
T18554	Pomalidomide-PEG1-azide	Pomalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that combines the cereblon ligand based on Pomalidomide with a linker. This compound is instrumental in designing PROTAC BRD4 Degrader-1[1].
T17878	Lenalidomide-C4-NH2 hydrochloride	Lenalidomide-C4-NH2 hydrochloride is a Cereblon ligand derived from Lenalidomide. It serves as a recruiting agent for the CRBN protein. The compound, known as PROTAC (Compound 24), can be formed by linking Lenalidomide-C4-NH2 hydrochloride to the ligand for the protein. It exhibits inhibitory effects with IC50s of 0.98 nM and 13.7 nM against the growth of RS4;11 and MOLM-13 acute leukemia cell lines, respectively[1].
T14441	Azido-PEG4-Amido-tri-(t-butoxycarbonylethoxymethyl)-methane	Azido-PEG4-Amido-tri-(t-butoxycarbonylethoxymethyl)-methane, a PEG-derived PROTAC linker, is employed for PROTAC synthesis[1].
T14173	Ald-Ph-amido-PEG3-C2-NH2	Ald-Ph-amido-PEG3-C2-NH2 is a PEG-based PROTAC linker employed in PROTACs synthesis[1].
T17491	Azido-PEG16-NHS ester	Azido-PEG16-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.
T17355	Acid-PEG4-S-PEG4-acid	Acid-PEG4-S-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.
T17833	DM4-SMCC	DM4-SMCC, a non-cleavable drug-linker conjugate for antibody-drug conjugates (ADC), leverages the antitumor efficacy of DM4 (an antitubulin agent) through attachment with the SMCC linker, exhibiting antitumor activity[1].
T17957	Fmoc-N-PEG-CH2COOH (MW 3400)	Fmoc-N-amido-PEG-CH2COOH (MW 3400) is a PEG-based PROTAC linker utilized in PROTAC synthesis[1].
T14174	Ald-Ph-amido-PEG4-C2-acid	Ald-Ph-amido-PEG4-C2-acid is a noncleavable linker utilized in the development of antibody-drug conjugates (ADC).
T18823	Thalidomide-O-amido-PEG4-propargyl	Thalidomide-O-amido-PEG4-propargyl is a polyethylene glycol (PEG)-based linker employed for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T15231	endo-BCN-PEG8-NHS ester	Endo-BCN-PEG8-NHS ester is a polyethylene glycol (PEG) derivative functionalized with N-hydroxysuccinimide (NHS) ester moiety, utilized as a linker in the synthesis of proteolysis-targeting chimeras (PROTACs)[1].
T14425	Azido-PEG3-aminoacetic acid-NHS ester	Azido-PEG3-aminoacetic acid-NHS ester is a PEGylation-based linker for the development of PROTACs[1]. It can be utilized in the synthesis of PROTACs, offering a versatile and efficient approach.
T14104	Acid-PEG3-SS-PEG3-acid	Acid-PEG3-SS-PEG3-acid is a cleavable 6 unit polyethylene glycol (PEG) linker employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T14707	Boc-Aminooxy-PEG1-C2-NH2	Boc-Aminooxy-PEG1-C2-NH2 is a polyethylene glycol (PEG)-derived linker compound, specifically designed for incorporation into proteolysis targeting chimeras (PROTACs)[1].
T14650	Bis-PEG8-acid	Bis-PEG8-acid, a PEG-based PROTAC linker, is utilized in the synthesis of PROTACs and antibody-drug conjugates (ADCs)[1]. It serves as a cleavable ADC linker, facilitating the development of specialized compounds.
T16592	Propargyl-PEG1-SS-PEG1-propargyl	Propargyl-PEG1-SS-PEG1-propargyl refers to a cleavable di-functional polyethylene glycol (PEG) linker composed of two units. This specific linker is employed in the synthesis of antibody-drug conjugates (ADCs), where it plays a critical role in linking the antibody to the drug. [1]
T18874	WSPC Biotin-PEG3-DBCO	WSPC Biotin-PEG3-DBCO 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.
T18004	HO-PEG-mal (MW 3400)	HO-PEG-mal (MW 3400) 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.
T17915	Thalidomide-O-amido-PEG3-C2-NH2	Thalidomide-O-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 3) is an E3 ligase ligand-linker conjugate which is designed using Thalidomide-based cereblon ligand and a 3-unit PEG linker. This compound is synthesized specifically for utilization in PROTAC technology.
T18236	Mal-amido-PEG12-acid	Mal-amido-PEG12-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.

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PROTAC Linker