ALV2 是一种有效和选择性的 Helios 降解剂。ALV2 可以结合 CRBN，IC50 为 0.57 μM。Helios 是一种锌指转录因子，可以在炎症性肿瘤微环境中维持稳定的 Treg 细胞表型。
货号:ajcx35872
CAS:2438124-95-7
分子式:C26H26ClN5O5
分子量：523.97
溶解度:DMSO : 160 mg/mL (305.36 mM; Need ultrasonic)|H2O :< 0.1 mg/mL (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

[1]. Wang ES, et, al. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717.