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ALV2 is a potent and selective Helios molecular glue degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment[1].

ALV2 is a potent and selective Helios degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment[1]. ALV2 (10 nM-100 μM) induces CRBN-Helios dimerization in the TR-FRET assay[1].ALV2 (0.1-10 μM) preferentially promotes Helios degradation in Jurkat cells[1].ALV2 (1 μM; pretreated for 18 h) promotes IL-2 secretion in Jurkat cells[1]. ALV2 (100 mg/kg; i.p. twice daily for 7 days) induces selective Helios degradation in vivo[1].

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[1]. Wang ES, et, al. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717.