
AX-024 NEW
Price | $67 | $1160 |
Package | 2mg | 100mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2025-05-01 |
Product Details
Product Name: AX-024 | CAS No.: 1370544-73-2 |
Supply Ability: 10g | Release date: 2025/05/01 |
Product Introduction
Bioactivity
Name | AX-024 |
Description | AX-024 is a novel chemical compound that acts as an orally available inhibitor of the TCR-Nck interaction. Its primary mechanism of action is the selective inhibition of T cell activation triggered by TCR stimulation. With an IC50 value of approximately 1 nM, AX-024 effectively modulates cell signaling by specifically targeting SH3 domains. Additionally, AX-024 demonstrates desirable characteristics such as low acute toxicity, high potency, and excellent selectivity. Notably, it exhibits strong inhibitory effects on the production of IL-6, TNF-α, IFN-γ, IL-10, and IL-17A. |
In vitro | AX-024 demonstrates exceptional efficacy, being over 10,000 times more effective than the earlier compound AX-000 in inhibiting T-cell proliferation prompted by T-cell receptor (TCR) activation, with an IC50 of 1 nM and observable inhibitory actions at concentrations as low as 1 pM. Furthermore, it significantly suppresses cytokine release from human peripheral blood mononuclear cells, including interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), interferon-γ (IFN-γ), IL-10, and IL-17A, at 10 nM concentration when stimulated with anti-CD3, outperforming AX-000 in efficiency. In the specific context of CD8+ T cells from OT1 TCR transgenic (OT1 Tg) mice, AX-024 drastically reduces T cell proliferation at just 0.1 nM in cells with a wild-type (WT) PRS mutation. Coimmunoprecipitation assays reveal that, while Nck typically associates with the TCR following activation, this interaction is dose-dependently obstructed by AX-024 starting at 1 nM concentrations, highlighting its potent inhibitory mechanism [1]. |
In vivo | The AX-024-treated group exhibited fewer scales and a reduction in skin thickening compared to the vehicle group. It significantly lessened the thickening of skin layers, particularly the dermis, closely mirroring the effects seen in mice treated with a control cream without imiquimod (IMQ). Moreover, AX-024 notably decreased the presence of airway inflammatory cells in both assays. Additionally, mice administered AX-024 showed rapid recovery from neurological impairments and weight loss, achieving a symptom-free state by day 30—a stark contrast to mice receiving the vehicle, which continued to exhibit ataxia and a loss of the righting reflex [1]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries, 10000+ Noval Small Molecucles,16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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- Since: 2011-01-07
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