SML1539

TDFA trifluoroacetate salt

≥98% (HPLC)

• Sinónimos: N-Acetyl-L-threonyl-L-α-aspartyl-N5-(2-fluoro-1-iminoethyl)-L-ornithinamide trifluoroacetate salt, Thr-Asp-F-amidine trifluoroacetate salt
• Fórmula empírica (notación de Hill): C₁₇H₂₉FN₆O₇ · xC₂HF₃O₂
• Peso molecular: 448.45 (free base basis)
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥98% (HPLC)
• Formulario: powder
• condiciones de almacenamiento: desiccated
• color: white to beige
• solubilidad: H₂O: 10 mg/mL, clear
• Condiciones de envío: dry ice
• temp. de almacenamiento: −70°C

Descripción

Descripción general

TDFA trifluoroacetate salt or tripeptide F-amidine analog is a derivative synthesized to increase the selectivity, bioavailability and potency of Cl-amidine, which is a member of protein arginine deiminases (PADs) compounds.[1]

Acciones bioquímicas o fisiológicas

Selective inhibitor of PAD4 (peptidyl arginine deiminase 4)

TDFA (Thr-Asp-F-amidine) is a selective inhibitor of peptidyl arginine deiminase 4 (protein arginine deiminase 4, PAD4 or PADI4), a transcriptional coregulator that catalyzes the calcium-dependent conversion of specific arginine residues in proteins to citrulline, a process called citrullination. PAD4 is upregulated in cancer and inflammatory diseases, and may be involved in rheumatoid arthritis onset and progression. It has recently been found to be involved in the regulation of pluripotency: important for stem-cell gene activation, induced pluripotent stem (iPS) cell reprogramming, and maintenance of pluripotent cells in the early mouse embryo. TDFA has an IC₅₀ value of 2.3 μM and is ≥15-fold selective for PAD4 versus PAD1 and ≥50-fold selective versus PADs 2 and 3.

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable