Lipids & Polymers

SIAIS178 represents an innovative proteolysis-targeting chimeric (PROTAC) degrader—a unique hybrid molecule intertwining the BCR-ABL kinase inhibitor dasatinib with a ligand designed for the Von Hippel-Lindau (VHL) E3 ubiquitin ligase through an optimized linker. It effectively directs the BCR-ABL protein for degradation through VHL-mediated mechanisms.

CPS2, a pioneering compound, is a potent, selective, and irreversible PROTAC CDK2 degrader, marking a significant advancement in this class of molecules. This innovative agent, CPS2, holds promise for research applications in the study of acute myeloid leukemia.

PROTAC RIPK degrader-6 is a Cereblon-based molecular agent developed to target the degradation of RIP Kinase. Within its structure, a RIP2 kinase inhibitor is intricately linked to a cereblon binder through a specialized linker.

MD-224 is a novel PROTAC-based small molecule designed to specifically degrade the MDM2 proto-oncogene. As a pioneering and highly effective degrader, MD-224 represents a new class of anticancer agents with significant potential in targeted therapy. Functioning as a click chemistry reagent, it harbors an alkyne group, enabling it to engage in copper-catalyzed azide-alkyne cycloaddition (CuAAC) with molecules featuring Azide groups.

INY-03-041 emerges as a potent and highly selective pan-AKT degrader utilizing the PROTAC approach. This compound comprises the ATP-competitive AKT inhibitor Ipatasertib linked to Lenalidomide. With its inhibitory action, INY-03-041 effectively targets and suppresses AKT1, AKT2, and AKT3.

SD-36, a potent and selective STAT3 degrader, induces complete degradation of the STAT3 protein in both xenograft tumor tissue and normal mouse tissues upon a single dose administration. SD-36 establishes itself as a powerful and effective solution for STAT3 degradation.

QCA570 stands out as an exceptionally potent and effective Proteolysis Targeting Chimera (PROTAC) degrader specifically designed for the Bromodomain and Extra-Terminal (BET) proteins. It not only demonstrates remarkable potency but also exhibits the capability to induce complete and enduring tumor regression.

SNIPER(ER)-87 stands out as a powerful and targeted degrader of estrogen receptor α (ERα), functioning as a Specific and Nongenetic IAP-dependent Protein Eraser (SNIPER). This compound is composed of the IAP binding ligand LCL 161, connected by a linker to the estrogen-binding component, 4-hydroxytamoxifen.

KB02-SLF represents a molecular glue-derived nuclear FKBP12 degrader built on the PROTAC framework. This compound enhances the degradation of nuclear FKBP12 by covalently altering DCAF16 (the E3 ligase), thereby bolstering the resilience of protein degradation within biological systems. The linkage of SLF to the ubiquitin E3 ligase ligand KB02 results in the formation of KB02-SLF.