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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
T17415 Amino-PEG16-acid Amino-PEG16-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.
T16453 PEG2-bis(phosphonic acid diethyl ester) PEG2-bis(phosphonic acid diethyl ester) is a polyethylene glycol (PEG) derivative commonly employed as a linker in proteolysis-targeting chimeras (PROTACs) synthesis[1].
T18509 Oleoyl-Gly-Lys-N-(m-PEG11) Oleoyl-Gly-Lys-N-(m-PEG11) is a cleavable 11 unit PEG linker utilized for the synthesis of antibody-drug conjugates (ADCs)[1].
T14438 Azido-PEG4-alcohol Azido-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.
T18022 HS-PEG24-CH2CH2COOH HS-PEG24-CH2CH2COOH 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.
T14403 Azido-PEG1-Boc Azido-PEG1-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.
T15334 Fmoc-PEG6-NHS ester Fmoc-PEG6-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.
T17650 Boc-N-Amido-PEG5-Ms Boc-N-Amido-PEG5-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.
T15072 DBCO-PEG4-Maleimide DBCO-PEG4-Maleimide is a cleavable linker employed for the synthesis of antibody-drug conjugates (ADCs)[1].
T17769 DBCO-NHCO-PEG3-Fmoc DBCO-NHCO-PEG3-Fmoc 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.
T17747 DBCO-C3-PEG4-NH-Boc DBCO-C3-PEG4-NH-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.
T18348 Methyltetrazine-PEG4-acid Methyltetrazine-PEG4-acid is a PEG-based linker utilized in the synthesis of PROTACs[1].
T15764 Lipoamido-PEG4-acid Lipoamido-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.
T15901 m-PEG5-succinimidyl carbonate m-PEG5-succinimidyl carbonate is a non-cleavable PEG linker with 5 units, utilized in the synthesis of antibody-drug conjugates (ADCs).
T17597 Biotin-PEG9-CH2CH2COOH Biotin-PEG9-CH2CH2COOH 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.
T18192 m-PEG36-azide m-PEG36-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.
T18577 Propargyl-PEG25-acid Propargyl-PEG25-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.
T17811 DBCO-SS-aldehyde DBCO-SS-aldehyde is an ADC linker employed for ADC synthesis[1]. This cleavable linker is designed to facilitate the conjugation of antibodies and drugs, resulting in antibody-drug conjugates (ADCs).
T18701 SPDB-DM4 SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) applications, employing the maytansine-based payload DM4 (a tubulin inhibitor) connected through a SPDB linker. This compound demonstrates significant anti-tumor efficacy.
T18489 NH2-O-C5-COOH hydrobromide NH2-O-C5-COOH (hydrobromide) is an alkyl chain-derived PROteolysis TArgeting Chimera (PROTAC) linker employed for PROTAC synthesis [1].
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