ALV2

Name: ALV2
Brand: TargetMol
SKU: T40099
Rating: 4.5 (1 reviews)

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产品编号 T40099Cas号 2438124-95-7

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

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产品编号 T40099Cas号 2438124-95-7

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产品介绍

生物活性

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.