|N,N'-(二硫烷二基双(乙烷-2,1-二基))双(2,5-二氯苯磺酰胺)|CsnPharm

CAS No.: 927822-86-4

KC7F2 Catalog No. CSN17251

Synonyms: KC7F2

KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7532 mL
- 8.7661 mL
- 17.5321 mL
- 5 mM
- 0.3506 mL
- 1.7532 mL
- 3.5064 mL
- 10 mM
- 0.1753 mL
- 0.8766 mL
- 1.7532 mL

技术信息

CAS号

927822-86-4

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H16Cl4N2O4S4

运输

蓝冰

分子量

570.38

别名

KC7F2

溶解度

DMSO	99.0 mg/mL (173.6 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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