受注:045-509-1970 |
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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 | C16H20N2 |
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分子量 | 240.34 | CAS No. | 749886-87-1 | |
Solubility (25°C)* | 体外 | DMSO | 48 mg/mL (199.71 mM) | |
Ethanol | 16 mg/mL (66.57 mM) | |||
Water | Insoluble | |||
* <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 | JSH-23 is an inhibitor of NF-κB transcriptional activity with IC50 of 7.1 μM in RAW 264.7 cell line. |
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in vitro | JSH-23 inhibits LPS-induced nuclear translocation of NF-κB p65 without affecting IκBα degradation. JSH-23 inhibits LPS-induced apoptotic chromatin condensation, while does not show significant cytotoxic effects on the RAW 264.7 cells at <100 μM. [1] JSH-23 also decreases NO production and neuronal migration in LPS activated cultures primary cultures from developing mouse cerebellum. [2] Moreover, JSH-23 augments cisplatin cytotoxicity in ovarian cancer cells with CI values ranging from 0.35 to 0.85. [3] |
in vivo | JSH-23 (3 mg/kg) significantly reverses the nerve conduction and nerve blood flow deficits by decreasing neuroinflammation and improving antioxidant defence in diabetic rats. [4] |
キナーゼアッセイ | Measurement of NF-κB transcriptional activity | |
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Macrophages RAW 264.7 transfected stably with reporter plasmid of pNF-κB-SEAP-NPT are treated with 1 μg/ml LPS and/or sample for 16 hours. As the reporter, SEAP activity in the cell-free culture media is measured as followed. Single cell-derived stable transfectants are plated in 5 ml of T-25 flask, and the media is decanted 24 h later. At this time, cells are washed twice with phosphate-buffered saline, and incubations are initiated by addition of new media. Chemicals are added to the culture medium after 24 h of incubations. Aliquots (25 ml) of medium from a control or chemical-treated cultures are taken at 0, 3, 20, 24, 48, and 72 h, heated at 65°C for 5 min to eliminate the alkaline phosphatase activity, and used immediately or stored at -20°C. Mixtures consisting of dilution buffer (25 ml), assay buffer (97 ml), culture media (25 ml), and 4-methylumbelliferyl phosphate (MUP, 1 mM, 3 ml) in each well of the 96-well plates are incubated for 60 min in the dark at room temperature. Fluorescence emits the product of the SEAP/MUP is measured at 449 nm using a 96-well plate fluorometer after excitation at 360 nm. | ||
細胞アッセイ | 細胞株 | RAW 264.7 cells |
濃度 | ~300 μM | |
反応時間 | 24 hours | |
実験の流れ | Macrophages RAW 264.7 are incubated with various concentrations of JSH-23 compound for 24 h. The cells are treated with WST-1 solution and absorbance is measured at 450 nm. | |
動物実験 | 動物モデル | STZ-induced diabetic rats |
投薬量 | ~3 mg/kg | |
投与方法 | Oral administration |
Data from [Data independently produced by , , Cell, 2018, 172(4):841-856]
Data from [Data independently produced by , , Blood, 2015, 125(7): 1098-106 ]
Data from [Data independently produced by , , J Mol Med (Berl), 2018, 96(3-4):301-313]
Nlrc3 signaling is indispensable for hematopoietic stem cell emergence via Notch signaling in vertebrates [ Nat Commun, 2024, 15(1):226] | PubMed: 38172511 |
Free heme induces neuroinflammation and cognitive impairment by microglial activation via the TLR4/MyD88/NF-κB signaling pathway [ Cell Commun Signal, 2024, 22(1):16] | PubMed: 38183122 |
TP53 gain-of-function mutations promote osimertinib resistance via TNF-α-NF-κB signaling in EGFR-mutated lung cancer [ NPJ Precis Oncol, 2024, 8(1):60] | PubMed: 38431700 |
Nilotinib boosts the efficacy of anti-PDL1 therapy in colorectal cancer by restoring the expression of MHC-I [ J Transl Med, 2024, 22(1):769] | PubMed: 39143573 |
Fatty Acid Oxidation Promotes Apoptotic Resistance and Proinflammatory Phenotype of CD4+ Tissue-resident Memory T cells in Crohn's Disease [ Cell Mol Gastroenterol Hepatol, 2024, 17(6):939-964] | PubMed: 38423357 |
A2AR-mediated CXCL5 upregulation on macrophages promotes NSCLC progression via NETosis [ Cancer Immunol Immunother, 2024, 73(6):108] | PubMed: 38642131 |
Hexokinase 2 nonmetabolic function-mediated phosphorylation of IκBα enhances pancreatic ductal adenocarcinoma progression [ Cancer Sci, 2024, 10.1111/cas.16204] | PubMed: 38801832 |
ERK1/2-CEBPB Axis-Regulated hBD1 Enhances Anti-Tuberculosis Capacity in Alveolar Type II Epithelial Cells [ Int J Mol Sci, 2024, 25(4)2408] | PubMed: 38397085 |
FGF18 alleviates sepsis-induced acute lung injury by inhibiting the NF-κB pathway [ Respir Res, 2024, 25(1):108] | PubMed: 38419044 |
Matrix metalloproteinase-8 regulates dendritic cell tolerance in late polymicrobial sepsis via the nuclear factor kappa-B p65/β-catenin pathway [ Burns Trauma, 2024, 12:tkad025] | PubMed: 38425412 |
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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