纯度:>98% by HPLC,;NMR (Conforms)
分子式:C14H5ClF9N3O
分子量:437.65
溶剂:DMSO (>25 mg/mL)
性状:Off-white solid
存储:-20°C
Activity (short version):Dual NF-kB / AP-1 inhibitor
Function / Pharmacology:SP100030 is a potent dual inhibitor of NF-kB- and AP-1-mediated gene expression (IC50’s = 50 nM for both in transfected Jurkat T-cells).1 It was able to specifically block IL-2 and IL-8 in Jurkat T-cells (IC50’s = 30 nM for both).1 SP100030 treatment significantly decreased arthritis severity in DBA/1J mice.2 It selectively inhibited CD8(+) T-cells and mRNA expression of TH1 and Th2 cytokines in a rat model of asthma but did not inhibit allergen-induced eosinophilia and bronchial hyperresponsiveness.3 SP100030 ameliorated muscle wasting in a cancer cachexia rat model.4 SP100030 suppression of T cell activation has been attributed to targeting of XPO1 (with minimal impact on nuclear export and cell viability).5