ALV2 is a potent and selective Helios degrader. ALV2 binds CRBN, with an IC 50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable T reg cell phenotype in the inflammatory tumor microenvironment.
性状
Solid
IC50 & Target[1][2]
IC50: 0.57 μM (CRBN)
体外研究(In Vitro)
ALV2 (10 nM-100 μM) induces CRBN-Helios dimerization in the TR-FRET assay.ALV2 (0.1-10 μM) preferentially promotes Helios degradation in Jurkat cells.ALV2 (1 μM; pretreated for 18 h) promotes IL-2 secretion in Jurkat cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ALV2 (100 mg/kg; i.p. twice daily for 7 days) induces selective Helios degradation in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Crbn mice
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Wang ES, et, al. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717.
溶解度数据
In Vitro: DMSO : 160 mg/mL (305.36 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)配制储备液