research use only
Cat.No.S7946
| Related Targets | EGFR VEGFR JAK PDGFR FGFR Src FLT FLT3 HER2 Bcr-Abl |
|---|---|
| Other HIF Inhibitors | PT2399 PX-478 Dihydrochloride BAY 87-2243 Lificiguat (YC-1) IOX2 CAY10585 (LW 6) Molidustat (BAY 85-3934) PT2385 IDF-11774 MK-8617 |
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In vitro |
DMSO
: 100 mg/mL
(175.32 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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| Molecular Weight | 570.38 | Formula | C16H16Cl4N2O4S4 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 927822-86-4 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | C1=CC(=C(C=C1Cl)S(=O)(=O)NCCSSCCNS(=O)(=O)C2=C(C=CC(=C2)Cl)Cl)Cl | ||
| Targets/IC50/Ki |
HIF-1α
20 μM
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|---|---|
| In vitro |
KC7F2 inhibits HIF-1α protein synthesis but not its mRNA transcription. This compound inhibits HRE-driven transcription and decreases HIF-1α protein levels in LN229-HRE-AP cells. It 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, this chemical inhibits colony formation, especially under hypoxia. In hypoxic microglial cultures, it downregulates the expression of TfR and DMT, and reduces the HIF-1α mediated iron accumulation. |
| Kinase Assay |
HIF transcriptional activity assay
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Cells are incubated at 37°C 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.
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| In vivo |
This compound significantly reduces the latent period in the pentylenetetrazole kindling rat model and increases the rate of spontaneous recurrent seizures during the chronic stage. |
References |
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| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Growth inhibition assay | Cell proliferation |
|
19789328 |
| Western blot | HIF-1α / p-AKT / AKT / p-mTOR / mTOR / S6K / p-4EBP1 / 4EBP1 |
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19789328 |
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