| 应用 |
STF-62247 may be used as positive control in autophagy inducing cell signaling studies. |
| 产品介绍 |
STF-62247是一个TGN抑制剂，在RCC4 和RCC4/VHL细胞中的IC50分别是0.625 μM和16 μM。 |
| 备注 |
STF-62247 shows selectivtoxicity and growth inhibition of renal cells lacking VHL; 25-fold greater sensitivity observed for cells with VHL deficiency compared to wild-type (VHL+). |
| 生化机理 |
Autophagy Inducer, STF-62247 is a small molecule agonist that induces autophagy and selectively causes lethality in renal cell carcinoma (RCC) cells that have lost the von Hippel-Lindau (VHL) tumor suppressor activity (IC50 = 625 nM). It significantly reduces the growth rate of tumors formed from VHL-deficient cells in mice. STF-62247 induces cytotoxicity in VHL-positive RCC cells only at higher concentrations (IC50 = 16 μM). Selectively induces non-apoptotic cell death in VHL- (von Hippel-Lindau) deficient, but not VHL-expressing, renal carcinoma cells both in vitro (IC50 = 0.625 and 16 μM in RCC4 and RCC4/VHL killing, respectively) and in mice. Although STF-62247 induces autophagy regardless of cellular VHL-expression level, STF-62247 treatment is shown to result in more enhanced/acidified autolysomes formation in VHL-deficient cells, implicating an important role of VHL in maintaining normal vesicular trafficking between ER, TNG, and lysosomes. |
| 别名 |
STF62247;STF 62247;N-(3-甲基苯基)-4-(4-吡啶基)-1,3-噻唑-2-胺;STF62247;STF 62247;N-(3-Methylphenyl)-4-(4-pyridinyl)-2-thiazolamine |
