For research use only. Not for therapeutic Use.
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].
| Catalog Number | I044682 |
| CAS Number | 2438124-95-7 |
| Synonyms | 1-(3-chloro-4-methylphenyl)-3-[2-[3-[[1-(2,6-dioxopiperidin-3-yl)-2,5-dioxopyrrol-3-yl]amino]phenyl]propan-2-yl]urea |
| Molecular Formula | C26H26ClN5O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H26ClN5O5/c1-14-7-8-17(12-18(14)27)29-25(37)31-26(2,3)15-5-4-6-16(11-15)28-19-13-22(34)32(24(19)36)20-9-10-21(33)30-23(20)35/h4-8,11-13,20,28H,9-10H2,1-3H3,(H2,29,31,37)(H,30,33,35) |
| InChIKey | YKFHBIMJVFQOQL-UHFFFAOYSA-N |
| SMILES | CC1=C(C=C(C=C1)NC(=O)NC(C)(C)C2=CC(=CC=C2)NC3=CC(=O)N(C3=O)C4CCC(=O)NC4=O)Cl |
| Reference | [1]. Wang ES, et, al. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717. |
