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Chemical Structure : Helios degrader ALV2
Catalog No.: PC-38303Not For Human Use, Lab Use Only.
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.
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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.
| M.Wt | 523.974 | |
| Formula | C26H26ClN5O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Eric S Wang, et al. Nat Chem Biol. 2021 Jun;17(6):711-717.
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