AX-024 hydrochloride Chemical Properties

storage temp. 

-20°

solubility 

Soluble in DMSO (up to at least 25 mg/ml with warming) or in Water (10 mg/ml with warming).

form 

solid

color 

White

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months.

AX-024 hydrochloride Usage And Synthesis

Description

AX-024 is an inhibitor of the CD3ε-Nck interaction. It binds to the SH3.1 N-terminal domain of Nck1, preventing its binding to the proline-rich sequence of the CD3ε subunit of T cells. AX-024 inhibits T cell receptor-triggered T cell activation (IC₅₀ = 1 nM for human T cells) and selectively decreases proliferation of T cells over B cells. It prevents CD4⁺ T cell and macrophage infiltration to the cerebellum and spinal cord and improves neurological impairments in a MOG_35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at a dose of 10 mg/kg per day for ten days starting on the day of immunization. AX-024 (50 mg/kg) prevents the infiltration of eosinophils, macrophages, and neutrophils into the airway, as well as prevents an increase in IL-4 levels in bronchoalveolar lavage fluid (BALF), in an ovalbumin-sensitized mouse model of allergic airway disease. It does not prevent the memory T cell response to an immunodominant B8R poxvirus antigen peptide or to infection by ectromelia virus (mousepox).

Uses

AX-024 is a T cell receptor inhibitor for the treatment of autoimmune diseases.

in vivo

IC 50

IL-6; IL-10; IL-17A

References

[1] ALDO BORROTO. First-in-class inhibitor of the T cell receptor for the treatment of autoimmune diseases[J]. Science Translational Medicine, 2016, 8 370. DOI:10.1126/scitranslmed.aaf2140

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