Name | ALV2 |
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Description | 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]. |
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Related Catalog | |
Target |
IC50: 0.57 μM (CRBN)[1] |
In Vitro | 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]. |
In Vivo | ALV2 (100 mg/kg; i.p. twice daily for 7 days) induces selective Helios degradation in vivo[1]. Animal Model: CrbnI391V/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. |
References |
Molecular Formula | C26H26ClN5O5 |
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Molecular Weight | 523.97 |