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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C16H16Cl4N2O4S4 |
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分子量 | 570.38 | CAS No. | 927822-86-4 | ||||||||||||
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (175.32 mM) | ||||||||||||
Water | Insoluble | ||||||||||||||
Ethanol | Insoluble | ||||||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or 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. |
製品説明 | KC7F2 is a selective HIF-1α transcription inhibitor with IC50 of 20 μM in a cell-based assay. |
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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] |
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] |
キナーゼアッセイ | HIF transcriptional activity assay | |
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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. | ||
細胞アッセイ | 細胞株 | Human dermal microvascular endothelial cells and mouse neurons; MCF7, LNZ308, A549, U251MG, and LN229 cell lines |
濃度 | 72 h | |
反応時間 | 20 μM | |
実験の流れ | 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. |
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Data from [Data independently produced by , , Respir Physiol Neurobiol, 2017, 247:87-95]
Inhibiting the glycerophosphodiesterase EDI3 in ER-HER2+ breast cancer cells resistant to HER2-targeted therapy reduces viability and tumour growth [ J Exp Clin Cancer Res, 2023, 42(1):25] | PubMed: 36670508 |
Hypoxia Primes Human ISCs for Interleukin-Dependent Rescue of Stem Cell Activity [ Cell Mol Gastroenterol Hepatol, 2023, 10.1016/j.jcmgh.2023.07.012] | PubMed: 37562653 |
Hypoxia Primes Human ISCs for Interleukin-Dependent Rescue of Stem Cell Activity [ Cell Mol Gastroenterol Hepatol, 2023, 16(5):823-846] | PubMed: 37562653 |
Dimethyloxalylglycine Attenuates Steroid-Associated Endothelial Progenitor Cell Impairment and Osteonecrosis of the Femoral Head by Regulating the HIF-1α Signaling Pathway [ Biomedicines, 2023, 11(4)992] | PubMed: 37189610 |
Identification of Hif1α as a Potential Participant in Autoimmune Uveitis Pathogenesis Using Single-Cell Transcriptome Analysis [ Invest Ophthalmol Vis Sci, 2023, 64(5):24] | PubMed: 37227746 |
Targeting SELPLG/P-selectin glycoprotein ligand 1 in preclinical ARDS: Genetic and epigenetic regulation of the SELPLG promoter [ Pulm Circ, 2023, 13(1):e12206] | PubMed: 36873461 |
Aquaporin 11 alleviates retinal Müller intracellular edema through water efflux in diabetic retinopathy [ Pharmacol Res, 2022, 187:106559] | PubMed: 36403720 |
FOXA1 inhibits hypoxia programs through transcriptional repression of HIF1A [ Oncogene, 2022, 10.1038/s41388-022-02423-6] | PubMed: 35931888 |
Elucidating the Novel Mechanism of Ligustrazine in Preventing Postoperative Peritoneal Adhesion Formation [ Oxid Med Cell Longev, 2022, 2022:9226022] | PubMed: 35308169 |
Cardamonin attenuates cerebral ischemia/reperfusion injury by activating the HIF-1α/VEGFA pathway [ Phytother Res, 2022, 10.1002/ptr.7409] | PubMed: 35142404 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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