产品说明书
KC7F2
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同义名 : | - |
| CAS号 : | 927822-86-4 | |
| 货号 : | A261687 | |
| 分子式 : | C16H16Cl4N2O4S4 | |
| 纯度 : | 98% | |
| 分子量 : | 570.381 | |
| MDL号 : | MFCD22683809 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 30 mg/mL(52.6 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 靶点 |
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| 描述 | The response of mammalian cells to hypoxia is mediated by a family of transcription factors known as HIF (hypoxia-inducible factors). The subunits of HIF, HIF-1α can be degraded rapidly under normoxia. KC7F2 is a HIF-1α inhibitor, which can inhibit the HIF-1α biological activity with IC50 value of 20μM (measured by HIF-1–responsive promoter) under hypoxia (1% O2). Accompanied with the inhibited activity of HIF-1α, treatment with KC7F2 40μM for 24h decreased the transcription of defined HIF-1α target genes, including carbonic anhydrase IX, MMP2, endothelin1 and enolase 1 in LN229 cells. KC7F2 has cytotoxicity in MCF7, LNZ308, A549, U251MG and LN229 with IC50 of approximately 15-25μM for 72h under normoxia, but is more severe under hypoxic conditions in other cell lines, such as D54MG. KC7F2 can also reduce the protein levels of HIF-1α in cancer cell lines of different tissue origin and genetic background, including U251MG, MCF7, PC3 and LNZ308 cells, on concentration of 40μM for 8 or 24 h under hypoxia, as well as in LN229 cells dose-dependently (20-80μM for 6h) [1]. | ||
| 作用机制 | KC7F2 inhibits HIF-1α protein synthesis with no effect on neither the mRNA transcription nor the protein degradation rate of HIF-1α. The accurate mechanism of its action is unknown, but may involve in inhibition of the phosphorylation of 4EBP1 and S6K.[1] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.75mL 0.35mL 0.18mL |
8.77mL 1.75mL 0.88mL |
17.53mL 3.51mL 1.75mL |
