bifunctional

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.

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].

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].

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].

Thiol-PEG-CH2COOH (MW 5000) is a polyethylene glycol (PEG) derivative frequently used in the construction of PROTACs, bifunctional compounds designed for targeted protein degradation [1].

CPD-10 is a potent bifunctional PROTAC degrader targeting CCND1 and CDK4 and exhibits antiproliferative effects. It induces apoptosis and reduces the protein expression of Cyclin D1, Cyclin D3, CDK4, and P-Rb(5807 811) in a dose-dependent manner.

CPD-39 is an efficacious and orally active bifunctional PROTAC degrader targeting both CCND1 and CDK4. It exhibits antiproliferative effects.

BTX-6654 is a cereblon-based bifunctional SOS1 PROTAC degrader. This compound exhibits antiproliferative activity against cells with various KRAS mutations by reducing the expression of downstream signaling markers pERK and pS6.

Alkyne-PEG6-acid is a bifunctional PEG crosslinker utilized in biological conjugation and as a component in small molecule synthesis. This crosslinker bears a carboxyl group at one end and an alkyne group at the other. In PROTACs, it is known as 2-2-2-2-2-2-6 PROTAC® linker and is also employed in the synthesis of antibody-drug conjugates.

YB-3-17 is a bifunctional molecule that can inhibit mTOR with an IC50 of 0.22 nM or degrade the G1 to S phase transition 1 gene (GSPT1) through the PROTAC mechanism, with a DC50 of 5 nM. It exhibits antiproliferative activity at nanomolar concentrations in various glioblastoma cell lines. Additionally, YB-3-17 shows antitumor activity in mouse models. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase Cereblon)

FLT3 Ligand-Linker Conjugate 1 consists of an FLT3 ligand and a PROTAC linker that can recruit E3 ligase VHL. This conjugate is useful for synthesizing PROTAC RSS0680, a bifunctional compound designed for targeted protein degradation of kinases.

p-SCN-Bn-TCMC is a bifunctional chelator, it contains a powerful chelator TCMC and reactive tioisocyante linker. TCMC is a powerful chelator with capability to strongly bind radio-isotopic heavy metal ion, which are widely used for radio-diagnostic imagin

DST crosslinker(disuccinimide tartarate) is an isotype bifunctional, cleavable crosslinker (cleavable by an oxidizer) for applications that require crosslinking cleavability and that do not interfere with protein disulfide bonds with reducing agents.