ALV2 is a potent and selective Helios degrader. ALV2 binds CRBN, with an IC 50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable T reg cell phenotype in the inflammatory tumor microenvironment.

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]. Animal Model: Crbn I391V/I391V mice Dosage: 100 mg/kg Administration: I.p. twice daily for 7 days Result: Reduced Helios, but not Ikaros, levels in splenic CD4 + FoxP3 + Treg cells.

2438124-95-7

C26H26ClN5O5

523.97

ALV2

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years