KC7F2

Catalog No.S7946

KC7F2 Chemical Structure

Molecular Weight(MW): 570.38

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

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1 Customer Review

  • Western blot analysis showed that KC7F2 (10 nM) significantly decreased the expression of HIF-1α, p27 and flt-1, while KC7F2 (10 nM) elevated cyclin D1 and flk-1 levels after 24 h incubation compared with the 1% O2 condition.

    Respir Physiol Neurobiol, 2017, 247:87-95. KC7F2 purchased from Selleck.

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Biological Activity

Description KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay.
Targets
HIF-1α [1]
20 μM
In vitro

KC7F2 inhibits HRE-driven transcription and decreases HIF-1α protein levels in LN229-HRE-AP cells. KC7F2 shows a dose-response cytotoxicity with IC50 of approximately 15 to 25 μM in cancer cells MCF7, LNZ308, A549, U251MG, and LN229. In D54MG glioma cells, KC7F2 inhibits colony formation, especially under hypoxia. [1] In hypoxic microglial cultures, KC7F2 downregulates the expression of TfR and DMT, and reduces the HIF-1α mediated iron accumulation. [2]

In vivo KC7F2 significantly reduces the latent period in the pentylenetetrazole kindling rat model and increases the rate of spontaneous recurrent seizures during the chronic stage in the lithium-pilocarpine rat model. [3]

Protocol

Kinase Assay:[1]
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HIF transcriptional activity assay:

Cells are incubated at 37癈 in a humidified atmosphere containing 5% CO2 and 21% O2 (normoxia) or 1% O2 (hypoxia) in a hypoxia workstation. The LN229-HRE-AP reporter cell line for HIF transcriptional activity is created by stably transfecting LN229 cells with the pACN188 plasmid, which contains an alkaline phosphatase gene driven by six HREs derived from the VEGF gene.
Cell Research:[1]
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  • Cell lines: Human dermal microvascular endothelial cells and mouse neurons; MCF7, LNZ308, A549, U251MG, and LN229 cell lines
  • Concentrations: 72 h
  • Incubation Time: 20 μM
  • Method: Cells are seeded onto 96-well plates (4 × 103/well) and cultured under normoxic (21% O2) and hypoxic (1% O2) conditions with different concentrations of KC7F2 for 72 h or treated for various times with 20 μM KC7F2. For proliferation analysis, cells are fixed with 50% trichloroacetic acid for 1 h at 4°C, followed by staining with 0.4% sulforhodamine B dissolved in 1% acetic acid for 30 min at room temperature. Plates are washed five times with 1% acetic acid to remove unbound dye. Bound dye is dissolved by adding 10 mM unbuffered Tris base. Cell proliferation is calculated by measuring OD values at 564 nm using a spectrophotometer.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (175.32 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 570.38
Formula

C16H16Cl4N2O4S4

CAS No. 927822-86-4
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID