1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethyl]amino]-

Biological Activity

Thalidomide-NH-C2-PEG3-OH is an E3 ligase ligand-linker conjugate that incorporates Thalidomide based cereblon ligand and a linker used for PROTAC BCL-XL degrader XZ739[1]. XZ739, a CRBN-dependent PROTAC BCL-XL degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis[1].

References

[1]. Xuan Zhang,et al. Discovery of PROTAC BCL-X L Degraders as Potent Anticancer Agents With Low On-Target Platelet Toxicity. Eur J Med Chem. 2020 Apr 15;192:112186.