产品描述
| 溶解性 | DMSO |
| 存贮条件 | 储存温度-20°C |
| 产品介绍 | Inolitazone(RS5444; CS-7017)是新型PPARγ高亲和性激动剂，EC50为rosiglitazone的五十分之一，对于不表达PPARγ的RIE细胞无抑制性。 |
| 生化机理 | The IC50 for growth inhibition is approximately 0.8 nM while anaplastic thyroid carcinoma (ATC) tumor growth was inhibited three- to fourfold in nude mice. siRNA against PPARgamma and a pharmacological antagonist demonstrated that functional PPARgamma was required for growth inhibitory activity of RS5444. RS5444 upregulated the cell cycle kinase inhibitor, p21WAF1/CIP1 . RS5444inhibited culture growth and caused irreversible G1 arrest, but did not induce apoptosis. In addition, RS5444 caused dramatic changes in cellular morphology which were associated with increased motility and diminished cellular adherence, but no increase in the ability of such cells to digest and invade Matrigel . Treatment with RS5444 leads to the up-regulation of RhoB and subsequent activation of p21, and that silencing of RhoB by RNAi blocks the ability of RS5444 to induce p21 and to inhibit ATC cells proliferation. |
| 别名 | 伊诺他酮; 5-((4-((6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基)甲氧基)苯基)甲基)-2,4-噻唑啉二酮;;Efatutazone; CS-7017; RS5444;5-((4-((6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1h-benzimidazol-2-yl)methoxy)phenyl)methyl)-2,4-thiazolidinedione |
