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ALV2 is a potent and selective Helios degrader that binds to CRBN protein, with an IC50 of 0.57 μM. Helios, a zinc-finger transcription factor, is essential for maintaining a stable T reg cell phenotype in the inflammatory tumor microenvironment.


| Description | ALV2 is a potent and selective Helios degrader that binds to CRBN protein, with an IC50 of 0.57 μM. Helios, a zinc-finger transcription factor, is essential for maintaining a stable T reg cell phenotype in the inflammatory tumor microenvironment. |
| Targets&IC50 | CRBN:0.57 μM (IC50) |
| In vitro | ALV2, within a concentration range of 10 nM to 100 μM, initiates CRBN-Helios dimerization as evidenced by the TR-FRET assay[1]. At lower concentrations (0.1-10 μM), ALV2 specifically facilitates the degradation of Helios in Jurkat cells[1]. Moreover, when pre-administered for 18 hours at a concentration of 1 μM, ALV2 enhances IL-2 secretion in Jurkat cells[1]. |
| In vivo | ALV2, administered intraperitoneally at a dosage of 100 mg/kg twice daily for 7 days, selectively induces Helios degradation in vivo in Crbn I391V/I391V mouse models. This treatment specifically reduced Helios levels without affecting Ikaros in splenic CD4 + FoxP3 + T regulatory cells. |
| Molecular Weight | 523.97 |
| Formula | C26H26ClN5O5 |
| Cas No. | 2438124-95-7 |
| Smiles | Cc1ccc(NC(=O)NC(C)(C)c2cccc(NC3=CC(=O)N(C4CCC(=O)NC4=O)C3=O)c2)cc1Cl |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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