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AX-024 | Inhibitor of T cell antigen receptor (TCR)-dependent T cell activation

AX-024 (1704801-24-0) is a potent (IC50 ~ 1 nM) and specific inhibitor of T cell antigen receptor (TCR)-dependent T cell activation. It inhibited neither B cell proliferation triggered by B cell antigen receptor (BCR), TLR4, CD40 agonists nor IL-2-dependent proliferation of T lymphoblasts. AX-024 binds to the SH3.1 domain of the adaptor protein Nck blocking its interaction with the CD3e subunit on the T cell antigen receptor. AX-024 displayed protective effects in mouse models of psoriasis, allergic asthma, and multiple sclerosis. Importantly, the therapeutic effect of AX-024 persisted after removal of the drug in contrast to fingolimod suggesting a persistent modification of autoimmune T cells. Currently in clinical trials.

References/Citations
1) Borroto et al. (2016), First-in-class inhibitor of the T cell receptor for the treatment of autoimmune diseases; Sci. Transl. Med., 8 370ra184

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Catalog#  10-4895-0005

$90.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1704801-24-0
Catalog Number:
10-4895
Activity:
Inhibitor of T cell antigen receptor (TCR)-dependent T cell activation
Chemical Name:
1-[[4-(4-Fluorophenyl)-6-methoxy-2H-chromen-3-yl]methyl]pyrrolidine hydrochloride
Molecular Weight:
375.86
Molecular Formula:
C21H22FNO2 • HCl
Solubility:
Soluble in DMSO (up to at least 25 mg/ml with warming) or in Water (10 mg/ml with warming).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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