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
T17689	Boc-Pip-alkyne-Ph-COOH	Boc-Pip-alkyne-Ph-COOH, a PROTAC linker characterized by its alkyl/ether composition, plays a crucial role in synthesizing PROTACs including ARD-266. This compound demonstrates significant efficacy in promoting the degradation of androgen receptor (AR) protein across AR-positive prostate cancer cell lines such as LNCaP, VCaP, and 22Rv1, showcasing DC50 values ranging from 0.2-1 nM[1].
T18244	Mal-amido-PEG8-val-gly-PAB-OH	Mal-amido-PEG8-val-gly-PAB-OH is an eight-unit PEG cleavable linker frequently employed in the synthesis of antibody-drug conjugates (ADCs)[1].
T16151	Ms-PEG7-Ms	Ms-PEG7-Ms 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.
T17970	Fmoc-NH-PEG19-CH2CH2COOH	Fmoc-NH-PEG19-CH2CH2COOH is a Polyethylene Glycol (PEG)-based linker for the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].
T17768	DBCO-NHCO-PEG3-acid	DBCO-NHCO-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.
T17846	DOTA-(t-butyl)3-PEG5-azide	DOTA-(t-butyl)3-PEG5-azide is a polyethylene glycol (PEG) derived linker designed specifically for the synthesis of proteolysis targeting chimeras (PROTACs)[1].
T15693	L-Azidohomoalanine	L-Azidohomoalanine, an alkyl chain-derived PROTAC linker, is utilized in the synthesis of PROTACs[1].
T14436	Azido-PEG3-Val-Cit-PAB-PNP	Azido-PEG3-Val-Cit-PAB-PNP is a cleavable 3 unit PEG ADC linker employed for synthesizing antibody-drug conjugates (ADCs)[1]. It also serves as a PEG-based PROTAC linker for the synthesis of PROTACs[2].
T16825	S-acetyl-PEG4-propargyl	S-acetyl-PEG4-propargyl is a PEG-based PROTAC linker employed for synthesizing PROTACs[1].
T18855	Tos-PEG9-Tos	Tos-PEG9-Tos 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.
T15978	Mal-PEG2-acid	Mal-PEG2-acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). It can be conjugated to Tubulysin and its derivative cytotoxic molecule [1].
T15925	m-PEG7-NHS ester	m-PEG7-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.
T18562	Propargyl-NH-PEG3-C2-NHS ester	Propargyl-NH-PEG3-C2-NHS ester is a non-cleavable triethylene glycol linker with propargyl and N-hydroxysuccinimide functional groups. It is utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T15123	Diethyl 8-bromooctylphosphonate	Diethyl 8-bromooctylphosphonate is an alkyl chain-based linker utilized for synthesizing PROTACs[1].
T14266	Aminooxy-PEG3-C2-Boc	Aminooxy-PEG3-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.
T17865	DSPE-PEG5-azide	DSPE-PEG5-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.
T14107	Acid-PEG4-S-S-PEG4-acid	Acid-PEG4-S-S-PEG4-acid is a polyethylene glycol (PEG)-based PROTAC linker, which serves as a key component in the synthesis of PROTACs.
T17136	Tos-PEG6-C2-Boc	Tos-PEG6-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.
T14269	Aminooxy-PEG3-propargyl	Aminooxy-PEG3-propargyl is a polyethylene glycol (PEG)-based linker for the synthesis of proteolysis targeting chimera (PROTACs)[1].
T16615	Propargyl-PEG4-alcohol	Propargyl-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.

注册成功

PROTAC Linker