Chemicals & Small Molecules

VHL Ligand 8 is a small molecule ligand for the VHL E3 ligase, serving as a key component in the synthesis of ARD-266, a potent PROTAC degrader targeting the androgen receptor (AR). ARD-266 facilitates AR degradation in specific cell lines, with a high degree of efficiency, indicated by DC50 values ranging from 0.2 to 1 nM. This highlights the usefulness of VHL Ligand 8 in developing targeted protein degradation tools.

Nutlin-3 is a commercially available inhibitor that specifically targets the interaction between p53 and MDM2, leveraging its structural properties to modulate this protein-protein interaction.

Nutlin carboxylic acid (MDM2 ligand 1) is a Nutlin 3-derived ligand specific for MDM2. It can be linked to a target protein via a linker to create a PROTAC, enabling targeted protein degradation.

VH032-OH is a VH032-derived VHL ligand that can be linked to a protein-targeting ligand via a linker to create PROTACs, facilitating targeted protein degradation.

Caylin-1 is an analog of Nutlin-3 that functions as an MDM2 inhibitor. It also demonstrates binding affinity to Bcl-XL and has applications in studying multi-target protein interactions.

PROTAC MDM2 Degrader-2 is a compound designed to degrade MDM2 using PROTAC technology. It features a strong MDM2 inhibitor, a linker, and a ligand that targets E3 ubiquitin ligase, facilitating the targeted degradation of MDM2. This structural design enhances its effectiveness in modulating protein levels within cellular pathways.

PROTAC BRD4 Degrader-12 is designed with ligands for von Hippel-Lindau and BRD4, facilitating targeted degradation of the BRD4 protein. This compound can be conjugated with antibodies against STEAP1 and CLL1, enhancing its specificity for degrading BRD4 in PC3 prostate cancer cells. The structural design allows for effective engagement with the ubiquitin-proteasome system for protein modulation.

β-NF-JQ1 is a PROTAC that employs Aryl Hydrocarbon Receptor (AhR) E3 ligase for targeted protein degradation. Utilizing β-NF as an AhR ligand, it specifically engages bromodomain-containing (BRD) proteins, promoting their interaction with AhR. This compound demonstrates significant efficacy in reducing BRD protein levels, which is associated with enhanced anticancer activity.

MS170 is a selective PROTAC designed to target and degrade AKT proteins. It effectively reduces overall cellular AKT levels through its binding interactions with AKT1, AKT2, and AKT3, showcasing its potential for modulating AKT signaling pathways.