573109

STAT3 Inhibitor VIII, 5,15-DPP

The STAT3 Inhibitor VIII, 5,15-DPP, also referenced under CAS 22112-89-6, controls the biological activity of STAT3.

• 别名: STAT3 Inhibitor VIII, 5,15-DPP, 5,15-Diphenylporphyrin
• 经验公式（希尔记法）: C₃₂H₂₂N₄
• CAS号: 22112-89-6
• 分子量: 462.54
• MDL编号: MFCD08276335
• UNSPSC代码: 12352200

属性

• 质量水平: 100
• 方案: ≥90% (HPLC)
• 表单: solid
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; protect from light
• 颜色: deep blue to deep purple
• 溶解性: DMSO: <1 mg/mL
• 运输: ambient
• 储存温度: 2-8°C

说明

一般描述

A cell-permeable porphyrin compound that binds STAT3 (K_D = 880 nM by SPR) and prevents STAT3 SH2 domain-mediated ligand binding (IC₅₀ = 280 nM) and dimerization (~60% inhibition at 50 µM in HEK293), while exhibiting much reduced activity against STAT1 ligand binding (IC₅₀ = 10 µM) and no activity againt Grb2 ligand binding even at concentrations as high as 20 µM. One day 5,15-DPP pre-treatment (50 µM) of MDA-MB-468 cultures is shown to greatly inhibit IL-6-induced STAT3, but not STAT1/5a/5b, nuclear translocation (by >90%) and nuclear STAT3 c-myc promoter binding activity, resulting in a more than 90% reduction in cellular c-myc protein level.

A cell-permeable porphyrin compound that directly binds to STAT3, prevents STAT3 dimerization and acts as a STAT3-SH2 domain antagonist with selectivity over STAT1 and Grb2 (IC₅₀ = 0.28, 10 and >20 µM, respectively). Shown to preferentially suppress STAT3 nuclear translocation and subsequent DNA binding in MDA-MB-468 cells with negligible effect on STAT1, STAT5a and STAT5b; further, reduce c-myc promoter binding and c-myc protein expression in IL-6 induced HEK-293-STAT3 cells. Does neither affect JAK kinase activity nor lower the expression or the phosphorylation levels of STAT3.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Uehara, Y., et al. 2009. Biochem. Biophys. Res. Commun.380, 627.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 3
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable