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
T14244	Amino-PEG5-Boc	Amino-PEG5-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.
T17923	(S,R,S)-AHPC-PEG3-NH2	(S,R,S)-AHPC-PEG3-NH2 is a synthetic conjugate of an E3 ligase ligand-linker, incorporating the (S,R,S)-AHPC VHL ligand and a 3-unit PEG linker, which are utilized in PROTAC technology.
T17557	Biotin-PEG11-Mal	Biotin-PEG11-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.
T17982	Fmoc-Val-Cit-PAB-Duocarmycin TM	Fmoc-Val-Cit-PAB-Duocarmycin TM is a drug-linker conjugate designed for antibody-drug conjugation (ADC), utilizing the antitumor antibiotic Duocarmycin TM. It is connected through the linker Fmoc-Val-Cit-PAB.
T15083	Dde Biotin-PEG4-alkyne	Dde Biotin-PEG4-alkyne 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.
T17876	E3 ligase Ligand 18	E3 ligase Ligand 18 is a ligand that binds to E3 ubiquitin ligase, and it can be chemically attached to a protein ligand through a linker to create PROTACs. The resulting PROTACs function as inducers of ubiquitination-mediated degradation, targeting cancer-promoting proteins[1].
T18086	m-PEG-Butyraldehyde (MW 5000)	m-PEG-Butyraldehyde (MW 5000) is a polyethylene glycol (PEG)-based linker compound, utilized in PROTAC synthesis[1].
T18478	NAMPT inhibitor-linker 2	NAMPT inhibitor-linker 2, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises an NAMPT inhibitor payload and a linker. When combined with an anti-c-Kit monoclonal antibody to form ADC-4, it demonstrates potent efficacy against c-Kit expressing cell lines, including GIST-T1 and NCI-H526, with IC50 values of <7 pM and 40 pM, respectively.
T16583	Propargyl-PEG1-acid	Propargyl-PEG1-acid, a PEG-based PROTAC linker, enables the synthesis of BTK-CRBN PROTACs, specifically Ibrutinib-based PROTAC 4 and PROTAC 5. At a concentration of 10 μM, PROTAC 5 facilitates the degradation of BTK and induces the degradation of CSK, LYN, and LAT2[1].
T17612	Bis-PEG10-NHS ester	Bis-PEG10-NHS ester, a cleavable ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
T17967	Fmoc-NH-PEG12-CH2COOH	Fmoc-NH-PEG12-CH2COOH 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.
T17371	Ald-Ph-amido-PEG4-propargyl	Ald-Ph-amido-PEG4-propargyl is a non-cleavable 4-unit polyethylene glycol (PEG) antibody-drug conjugate (ADC) linker employed in ADC synthesis[1].
T15226	endo-BCN-PEG4-acid	endo-BCN-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.
T17898	cIAP1 Ligand-Linker Conjugates 7	cIAP1 Ligand-Linker Conjugates 7 is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a PROTAC linker. It is utilized in the design of SNIPERs[1].
T15899	m-PEG5-phosphonic acid	m-PEG5-phosphonic 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.
T17699	Bromo-PEG24-Boc	Bromo-PEG24-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.
T18181	m-PEG3-S-PEG2-OH	m-PEG3-S-PEG2-OH 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.
T18147	m-PEG13-NHS ester	m-PEG13-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.
T18079	m-PEG-acrylate (MW 20000)	m-PEG-acrylate (MW 20000), a PEG-based PROTAC linker, serves as a useful component in the synthesis of PROTACs[1].
T17643	Boc-Aminooxy-PEG4-CH2-Boc	Boc-Aminooxy-PEG4-CH2-Boc is a PEG-based linker utilized in the synthesis of PROTACs.

注册成功

PROTAC Linker