Lipids & Polymers

TBK1 PROTAC 3i serves as a powerful degrader specifically targeting TANK-binding kinase 1 (TBK1) with notable potency. It demonstrates remarkable selectivity and consists of a ligand designed for von-Hippel Lindau (VHL) protein, connected by a linker to a module that targets TBK1.

DT2216 stands as a PROTAC-type protein degrader in clinical development. Its focal point is the degradation of the BCL-XL protein, an anti-apoptotic protein overexpressed in certain cancers, achieved through the Von Hippel-Lindau (VHL) E3 ligase. This development is geared towards potential antitumor activity.

PROTAC FAK degrader 1 stands out as a potent and selective von Hippel-Lindau-based degrader specifically targeting focal adhesion kinase (FAK).

GSK215 represents a highly effective and specific PROTAC designed to degrade focal adhesion kinase (FAK). Engineered with a binding affinity for both the VHL E3 ligase and the FAK inhibitor VS-4718, GSK215 facilitates swift and sustained degradation of FAK, resulting in a durable impact on FAK levels and a notable disconnect between pharmacokinetics/pharmacodynamics (PK/PD).

PT-65 functions as a robust GSK3 Degrader utilizing the PROTAC mechanism. Demonstrating significant activity against GSK3α and GSK3β, it effectively mitigates Okadaic acid-induced tau hyperphosphorylation. Additionally, PT-65 showcases the ability to improve learning and memory deficits in rat models of Alzheimer's disease.

MS67 stands out as a highly effective and specific degrader of WD40 repeat domain protein 5 (WDR5). Notably, MS67 exhibits inactivity against various other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. Its potent anticancer effects further underscore its significance.

ARD-69 represents a potent proteolysis-targeting chimera (PROTAC) designed specifically for the degradation of the androgen receptor (AR). It serves as a proof-of-concept lead to assess the viability of PROTAC technology with AR positivity.

VZ185 is a highly potent and rapid dual degrader probe based on von Hippel-Lindau, exhibiting selectivity for degrading BRD9 and BRD7.

ACBI1 serves as a potent and collaborative degrader for SMARCA2, SMARCA4, and PBRM1. Operating as a PROTAC degrader, ACBI1 exhibits anti-proliferative activity and prompts apoptosis.