PEG

N-Mal-N-bis(PEG4-acid-amido-PEG24-acid) functions as a maleimide PEG reagent with two terminal carboxylic acids and a maleimide (Mal) group. Maleimide (Mal) reacts specifically with sulfhydryl groups to form a stable thioether linkage when the pH is between 6.5 and 7.5. The terminal carboxylic acids can conjugate with amine-containing molecules in the presence of activators (e.g. HATU). The PEG linkages improve the compound's water solubility.

DOTA-PEG8-amine, HCl salt represents a PEG linker possessing a DOTA moiety, which can be used as a chelating agent for cations and is commonly used for imaging diagnostics. The amine group is reactive toward carboxylic acids, activated NHS esters, etc. The hydrophilic PEG chain enhances the solubility of compounds in aqueous media.

A1V1PF2-OEt is an IAP-recruiting ligand, designed via in silico methods, for use in targeted protein degradation and the development of SNIPER technology.

CC-885 serves as a PROTAC which modulates the activity of cereblon (CRBN), a key protein involved in protein regulation. It facilitates the targeted ubiquitination and degradation of PLK1 by specifically engaging CRBN and the ATPase enzyme p97. Through this mechanism, CC-885 alters the stability and turnover of PLK1, a protein involved in cell cycle regulation.

Golcadomide (CC-99282) is a potent, orally active modulator of the CRBN E3 ligase. It engages with the CRL4-CRBN complex, promoting the recruitment and ubiquitin-dependent degradation of the transcription factors Ikaros and Aiolos. This selective modulation of protein degradation pathways highlights its utility for research in cell regulation and related fields.

ALV2 is a potent, selective degrader of the zinc-finger transcription factor Helios, which plays a role in maintaining Treg cell stability. By binding to cereblon (CRBN) with an IC50 of 0.57 μM, ALV2 promotes targeted Helios degradation, making it valuable for research involving transcriptional regulation and immune cell behavior.

VHL-4

Nutlin-3a (Rebemadlin) is the active enantiomer of Nutlin-3 and serves as a potent inhibitor of murine double minute 2 (MDM2) with an IC50 of 90 nM. It disrupts the MDM2-p53 interaction, leading to stabilization of the p53 protein and subsequent induction of cell autophagy and apoptosis. Nutlin-3a is valuable for investigating TP53 wild-type ovarian carcinomas due to its structural specificity in targeting these interactions.

PT-179 is a Thalidomide derivative designed to specifically target cereblon without causing unintended degradation of other proteins. It binds to cereblon and forms a ternary complex with target proteins that are fused to a zinc finger (ZF) degron, facilitating their degradation. For instance, PT-179 interacts with cereblon and forms a complex with SD40, enabling efficient degradation of proteins tagged with SD40 or SD36. This makes PT-179 useful for developing targeted protein degradation systems.