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|---|---|---|---|---|---|---|---|
| {[ item.pr_size ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} | 现货 | 1周 咨询 | - + | 
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| 产品名称 | HIF ↓ ↑ | HIF1 ↓ ↑ | PHD1 ↓ ↑ | PHD2 ↓ ↑ | PHD3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| KC7F2 | + HIF-1α, IC50: 20 μM | + HIF-1α, IC50: 20 μM | 98% | ||||||||||||||||
| Roxadustat | ✔ | 98+% | |||||||||||||||||
| Lificiguat | ✔ | 99%+ | |||||||||||||||||
| BAY 87-2243 | ✔ | 99%+ | |||||||||||||||||
| PX-478·2HCl | ✔ | 98%+ | |||||||||||||||||
| 2-Methoxyestradiol | ✔ | 98% | |||||||||||||||||
| LW6 | ++ HIF, IC50: 4.4 μM | BCRP | 99%+ | ||||||||||||||||
| Daprodustat | ✔ | 98+% | |||||||||||||||||
| DMOG | ✔ | 98% | |||||||||||||||||
| FG 2216 | ++ PHD2, IC50: 3.9 μM | 99%+ | |||||||||||||||||
| IOX2 | +++ PHD2, IC50: 21 nM | 99% | |||||||||||||||||
| Molidustat | ++ PHD1, IC50: 480 nM | +++ PHD2, IC50: 280 nM | +++ PHD3, IC50: 450 nM | 98+% | |||||||||||||||
| MK-8617 | ++++ PHD1, IC50: 1 nM | ++++ PHD2, IC50: 1 nM | ++++ PHD3, IC50: 14 nM | 99%+ | |||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 | 
 | 
| 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] | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 1.75mL 0.35mL 0.18mL | 8.77mL 1.75mL 0.88mL | 17.53mL 3.51mL 1.75mL | |
| CAS号 | 927822-86-4 | 
| 分子式 | C16H16Cl4N2O4S4 | 
| 分子量 | 570.38 | 
| SMILES Code | O=S(C1=CC(Cl)=CC=C1Cl)(NCCSSCCNS(C2=CC(Cl)=CC=C2Cl)(=O)=O)=O | 
| MDL No. | MFCD22683809 | 
| 别名 | |
| 运输 | 蓝冰 | 
| InChI Key | REQLACDIZMLXIC-UHFFFAOYSA-N | 
| Pubchem ID | 16047442 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C | 
| 溶解方案 | 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
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