bifunctional

CB1954(Tretazicar (NSC-115829)), an anticancer prodrug, is activated by NAD(P)H quinone oxidoreductase 2. It is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent.

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.

dCBP-1 is a chemical degrader of p300/CBP. dCBP-1 hijacks the E3 ubiquitin ligase CRBN for selective degradation of p300/CBP. Degradation of p300/CBP by dCBP-1 leads to effective multiple myeloma cell killing.

Macropa-NCS is a macropa bifunctional analog with antitumor activity and can be used to study prostate cancer.

Macropa-NH2 is a bifunctional analog of macropa, a carrier molecule that is often coupled to antibodies and is often used as a chelator in cancer research.

Adipic dihydrazide (ADH) is a dihydrazide with a symmetrical C4 skeleton, commonly used as a bifunctional cross-linking agent for water-in-oil emulsions and a curing agent for epoxy resins. ADH exhibits antibacterial activity against E. coli and P. aeruginosa.

dTRIM24 is a selective bifunctional TRIM24 degradation agent based on PROTAC technology, consisting of the ligands von Hippel-Lindau and TRIM24.

Ald-Ph-amido-C2-PEG3-NH-Boc is a polyethylene glycol (PEG)-based bifunctional linker used in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].

Alkyne-PEG4-maleimide is a PEG-based bifunctional linker designed for the construction of PROTAC molecules, enabling covalent conjugation between ligand moieties via its terminal alkyne and maleimide groups, and facilitating selective protein degradation through ubiquitin–proteasome system recruitment.

Aminooxy-PEG3-C2-NH-Boc is a PEGylated PROTAC linker used in synthesizing PROTACs, a new class of bifunctional molecules for targeted protein degradation [1].

Azido-PEG4-hydrazide-Boc is a polyethylene glycol (PEG)-based bifunctional linker compound used in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].

N-(Azido-PEG2)-N-Boc-PEG4-Boc is a PEG-based bifunctional linker used in the synthesis of PROTACs (proteolysis-targeting chimeras).

N-Mal-N-bis(PEG4-NHS ester) is a polyethylene glycol (PEG)-based bifunctional linker used for synthesizing Proteolysis Targeting Chimeras (PROTACs) [1].

Propargyl-PEG4-Tos is a PEG-based PROTAC linker used for constructing bifunctional degraders and for synthesizing cleavable ADC linkers. Propargyl-PEG4-Tos provides a reactive propargyl group suitable for click chemistry and a tosyl leaving group that facilitates controlled conjugation steps, making it essential in targeted protein-degradation research and antibody–drug conjugate engineering.

Treosulfan (NSC 39069) is a bifunctional alkylating agent used in the treatment of advanced ovarian cancer.[2]

Azide-PEG3-Sulfone-PEG3-azide is a polyethylene glycol (PEG)-based bifunctional molecule, designed as a PROTAC linker for PROTAC synthesis [1].

Boc-Aminooxy-PEG2-bromide is a bifunctional, cleavable polyethylene glycol (PEG) linker used specifically in the synthesis of antibody-drug conjugates (ADCs) [1].

Fmoc-N-amido-PEG36-acid is a polyethylene glycol (PEG)-based linker used in PROTAC synthesis, designed to construct bifunctional molecules that recruit target proteins to an E3 ubiquitin ligase for degradation[1].

m-PEG-acrylate (MW 30000) is a polyethylene glycol (PEG)-based bifunctional linker commonly used in the chemical synthesis of proteolysis targeting chimeras (PROTACs)[1].

N-Desthiobiotin-N-bis(PEG4-t-butyl ester) is a PEG-based linker compound used in the synthesis of PROTACs, which are bifunctional molecules aimed at targeted protein degradation[1].

Sulfo-SIAB sodium is a non-cleavable monovalent bifunctional linker.

Sulfo-SMCC sodium, a widely utilized non-cleavable, hetero-bifunctional crosslinker for antibody-drug conjugates (ADCs), features both N-hydroxysuccinimide (NHS) ester and maleimide groups. These functionalities enable it to specifically react with primary amines and sulfhydryl groups, respectively.

t-Boc-Aminooxy-PEG7-bromide is a polyethylene glycol (PEG)-based bifunctional linker used in synthesizing proteolysis targeting chimeras (PROTACs)[1].

TCO-PEG3-TCO is a PEG-based linker commonly used in PROTAC development to connect two essential ligands within a single molecule. By facilitating the formation of bifunctional degraders, TCO-PEG3-TCO linker supports targeted protein degradation through the ubiquitin–proteasome system, enabling precise modulation of intracellular protein levels.