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Background: STAT6 (signal transducer and activator of transcription 6) is a member of the STAT family of proteins which activate gene expression by relaying signals from cytokines that bind to their receptors on the cell surface to the nucleus. STAT6 is mainly activated by IL-4 (interleukin-4) and IL-13, via phosphorylation by JAKs (Janus kinases). Once phosphorylated, STAT6 forms a homodimer that translocate to the nucleus and binds to DNA via the DNA-binding domain, activating gene transcription. STAT6 signaling is involved in T-helper type 2 (Th2) cell development and differentiation, macrophage activation, and it impacts the levels of CD20 on the surface of B lymphocytes. Gene fusions products of STAT6 with NGFI-A-binding protein 2 (NAB2) are responsible for fibrous tumors. Dysfunction of the STAT6 pathway leads to allergic reactions (asthma, atopic dermatitis, food allergies) and cancer (Hodgkin, central nervous system and follicular lymphoma). STAT6 can serve as a diagnostic and prognostic tool. Inhibitors have been shown to reduce acute inflammation in animal models, and future developments may lead to new therapeutical tools for STAT6 related pathologies.
CAS Number: 919486-40-1
Description: AS1517499 is a potent and brain-permeable STAT6 phosphorylation inhibitor with an IC50 of 21 nM.1
Format: Solid.
Purity: ≥90%
Storage Stability: Powder-20°C3 years 4°C2 yearsIn solvent-80°C2 years -20°C1 year
Target: STAT6
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Nagashima S, et al., 2007 Bioorg Med Chem. 15(2): 1044-55.
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