KC7F2

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

KC7F2 Chemical Structure

KC7F2 Chemical Structure

CAS: 927822-86-4

Selleck's KC7F2 has been cited by 30 Publications

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Purity & Quality Control

Batch: Purity: 99.42%
99.42

KC7F2 Related Products

Signaling Pathway

Choose Selective HIF Inhibitors

Biological Activity

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

KC7F2 inhibits HIF-1α protein synthesis but not its mRNA transcription. 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]

Kinase Assay 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 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.

Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell proliferation 19789328
Western blot HIF-1α / p-AKT / AKT / p-mTOR / mTOR / S6K / p-4EBP1 / 4EBP1 19789328
In Vivo
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. [3]

Chemical Information & Solubility

Molecular Weight 570.38 Formula

C16H16Cl4N2O4S4

CAS No. 927822-86-4 SDF Download KC7F2 SDF
Smiles C1=CC(=C(C=C1Cl)S(=O)(=O)NCCSSCCNS(=O)(=O)C2=C(C=CC(=C2)Cl)Cl)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (175.32 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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

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