Helios degrader ALV2 (ALV-04-019-01) is a potent and selective Helios degrader with IC50 of 0.57 uM in CRBN-binding TR-FRET assay.
ALV2 recruited the E3 ubiquitin ligase substrate receptor cereblon to Helios.
ALV2 bound CRBN in vitro with greater potency than lenalidomide but less than CC-885.
ALV2 also induced CRBN-Helios dimerization in the TR-FRET assay, with greater activity than either CC-885.
ALV2 exhibited relative selectivity for Helios, but not ALV1, exhibited potent degradation of ZNF692 and ZNF653.
