生物活性 | |||
---|---|---|---|
靶点 |
|
||
描述 | STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM. STF-31completely suppressed the glucose uptake activity and induced apoptosis in GLUT1 expressing myeloma cells. Moreover, STF-31 synergistically enhanced the cell death induced by melphalan, doxorubicin, and bortezomib[3]. STF-31 (0.01-10 μM; 10 days) is specifically toxic to RCC4 cells, whereas RCC4/VHL cells are relatively unaffected. RCC4/VHL cells treated with STF-31 (5 μM; 10 days) largely recovery, whereas RCC4 cells under the same conditions does not. STF-31 (1.25-5 μM; 3 days) does not induce autophagy, apoptosis, or DNA damage. STF-31 causes a necrotic cell death. Soluble analog of STF-31 (11.6 mg/kg; i.p.) treatment delays tumor growth in mice with VHL-deficient RCC tumor xenografts[4]. STF-31 (10 mg/kg; i.p.; twice daily for 2 days, followed by once daily for another 3 days) does not affect normal mice body weight, behavior, and ERG responses. STF-31 reduces light-induced CX3CR1gfp/+ mice microglial activation and retinal degeneration[5]. |
细胞研究 | |||||
---|---|---|---|---|---|
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
A2780 cells | Function assay | 48 h | Inhibition of NAMPT in human A2780 cells assessed as reduction in NAD level after 48 hrs by LC-MS/MS analysis, IC50=0.024 μM | 24433859 | |
HCT116 cells | Proliferation assay | 96 h | Antiproliferative activity against human HCT116 cells after 96 hrs by CyQuant-based assay, IC50=0.271 μM | 24433859 | |
HT1080 cells | Proliferation assay | 96 h | Antiproliferative activity against human HT1080 cells after 96 hrs by CyQuant-based assay, IC50=0.213 μM | 24433859 |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.36mL 0.47mL 0.24mL |
11.81mL 2.36mL 1.18mL |
23.61mL 4.72mL 2.36mL |
参考文献 |
---|