Bulk Inquiry
AX-024 hydrochloride
- Parent CAS: 1370544-73-2
- Soluble in water and DMSO
- MF: C21H22FNO2.HCl
- MW: 375.86
Description
AX-024 hydrochloride is an orally available small-molecule inhibitor of T-cell receptor (TCR) signaling. It was originally reported to disrupt the interaction between the proline-rich region of CD3ε and the SH3.1 domain of NCK, producing potent inhibition of TCR-triggered T-cell activation with a reported IC50 of approximately 1 nM.
AX-024 suppresses T-cell proliferation and has shown activity in mouse models of psoriasis, allergic asthma, and experimental autoimmune encephalomyelitis. Subsequent mechanistic studies indicate that its antiproliferative effects may not be explained exclusively by disruption of the CD3ε–NCK interaction, so AX-024 is best used as a functional TCR-signaling inhibitor with appropriate pathway controls. The salt form, AX-024 hydrochloride, provides improved aqueous handling without changing the core pharmacology.
Key Features
- Orally available TCR signaling inhibitor
- IC50: approximately 1 nM for inhibition of TCR-triggered T-cell activation
- A disruptor of the CD3ε–NCK interaction
- Suppresses T-cell proliferation
- Active in multiple autoimmune and inflammatory mouse models
Applications
- T-cell receptor signaling and activation assays
- CD3ε and NCK adaptor-protein studies
- Psoriasis and allergic asthma research
- Autoimmune and neuroinflammation disease research
More Information
| Parent CAS No. | 1370544-73-2 |
|---|---|
| Chemical Name | 1-((4-(4-Fluorophenyl)-6-methoxy-2H-chromen-3-yl)methyl)pyrrolidine hydrochloride |
| SMILES | C1C(F)=CC=C(C2=C(CN3CCCC3)COC3C=CC(OC)=CC2=3)C=1.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C21H22FNO2.ClH/c1-24-18-8-9-20-19(12-18)21(15-4-6-17(22)7-5-15)16(14-25-20)13-23-10-2-3-11-23;/h4-9,12H,2-3,10-11,13-14H2,1H3;1H |
| InChiKey | DGBCIMPGYRVTPD-UHFFFAOYSA-N |
| CID | 129909862 |
| Short Description | T cell receptor inhibitor |
References
- A Borroto et al. First-in-class inhibitor of the T cell receptor for the treatment of autoimmune diseases. Sci Transl Med. 2016 Dec 21;8(370):370ra184.
- Richter, K., et al. Small molecule AX-024 reduces T cell proliferation independently of CD3ε-Nck1 interaction, which is governed by a domain-swap in the Nck1-SH3. 1 domain. J. Biol. Chem. 2020 April 21, jbc-RA120.
- List of publications using Ax-024 (Axon 2692) purchased from Axon Medchem
