heterobifunctional

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.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

SMCC (N-Succinimidyl 4-(N-maleimidomethyl)cycl) is a heterobifunctional protein crosslinker.

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.

AMAS is a non-claevable heterobifunctional crosslinker with NHS ester and maleimide groups that enables covalent conjugation of amine- and sulfhydryl-containing molecules.

FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.

Bromo-PEG5-phosphonic acid diethyl ester is a polyethylene glycol (PEG)-based linker utilized in the construction of PROteolysis TArgeting Chimeras (PROTACs), which are heterobifunctional molecules designed to induce protein degradation[1].

GMBS, a heterobifunctional cross-linker, possesses an N-hydroxysuccinimide (NHS) ester at one end and a maleimide group at the other. It is commonly used in bioconjugation to link amines and sulfhydryls [thiols], forming stable amide and thioether bonds, respectively, which are useful in creating protein and peptide conjugates.

m-PEG4-phosphonic acid ethyl ester is a PEGylation-based linker used in the design and synthesis of PROTACs, which are heterobifunctional molecules that facilitate targeted protein degradation[1].

m-PEG3-Sulfone-PEG4-propargyl is a polyethylene glycol (PEG)-based prodrug-induced degradation (PROTAC) linker utilized in the efficient synthesis of heterobifunctional molecules designed to selectively target and degrade specific protein targets[1].

Sulfo-LC-SPDP is a heterobifunctional crosslinker characterized by its thiol-cleavable and membrane impermeable properties.

Sulfo-SPP is a heterobifunctional, thiol-cleavable, and membrane-impermeable crosslinker.

SBA crosslinker is a sulfhydryl and amino reactive heterobifunctional protein crosslinking reagent. SBA protein crosslinker is non-cleavable and is among the shortest amine and sulfhydryl reactive crosslinking reagents known with a spacer arm length of on

SMPB crosslinker is a heterobifunctional protein crosslinking reagent that is reactive toward sulfhydryl and amino groups. The SMPB protein crosslinker is an extended chain length analog of MBS crosslinker. SMPB crosslinker's spacer arm is non-cleavable.

Sulfo-EMCS is a heterobifunctional sulfhydryl- and amine-reactive crosslinker.

Sulfo-MBS Crosslinker is a non-cleavable, water-soluble, heterobifunctional protein crosslinking reagent. It is commonly used to crosslink haptens to carrier proteins and enzymes to antibodies.

Sulfo-SIA Crosslinker is a non-cleavable, heterobifunctional protein crosslinker. Sulfo-SIA Crosslinker is useful in making antibody-drug conjugates.

Piperidine-GNE-049-N-Boc is a ligand that specifically binds to the target protein dCBP, facilitating its degradation by a selective and potent heterobifunctional degrader, p300 CBP.

Thalidomide-NH-PEG4-COOH is a conjugate comprising an E3 ligase ligand-linker, utilized in the synthesis of dCBP-1. dCBP-1 itself functions as a powerful and selective heterobifunctional degrader targeting p300 CBP.

CBP/p300 ligand 2 is the target protein ligand for PROTAC dCBP-1, a potent and selective p300/CBP degrader.

ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested.

dBET57 is heterobifunctional degrader of BRD4 based on the PROTAC technology, exhibits significant degradation of BRD4BD1 with a DC50 5h of 500 nM ,and inactive on BRD4BD2

dBRD4-BD1 is a selective BRD4 bromodomain inhibitor. dBRD4-BD1 can selectively degrade BRD4 (DC50 = 280 nM). Notably, dBRD4-BD1 upregulates BRD2 3, a result not observed with degraders using pan-BET ligands. Designing BRD4 selectivity up front enables analysis of BRD4 biology without wider BET-inhibition and simplifies designing BRD4-selective heterobifunctional molecules, such as degraders with new E3 recruiting ligands or for additional probes beyond degraders.

dTAGV-1-NEG TFA, a diastereomer, serves as the heterobifunctional negative control for dTAGV-1. It acts specifically as an FKBP12 F36V-selective degrader [1].