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ALV2 is a potent and selective Helios degrader compound that binds to the CRBN protein, exhibiting an IC50 value of 0.57 μM. Helios, a zinc-finger transcription factor, plays a crucial role in preserving a stable T reg cell phenotype within the inflammatory tumor microenvironment.
ALV2 is a potent and selective Helios degrader compound that binds to the CRBN protein, exhibiting an IC50 value of 0.57 μM. Helios, a zinc-finger transcription factor, plays a crucial role in preserving a stable T reg cell phenotype within the inflammatory tumor microenvironment.
产品描述 | ALV2 is a potent and selective Helios degrader compound that binds to the CRBN protein, exhibiting an IC50 value of 0.57 μM. Helios, a zinc-finger transcription factor, plays a crucial role in preserving a stable T reg cell phenotype within the inflammatory tumor microenvironment. |
靶点活性 | CRBN:0.57 μM (IC50) |
体外活性 | 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]. |
体内活性 | ALV2 (100 mg/kg; i.p. twice daily for 7 days) induces selective Helios degradation in vivo[1]. Animal Model: Crbn I391V/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. |
分子量 | 523.97 |
分子式 | C26H26ClN5O5 |
CAS No. | 2438124-95-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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