Molecular Weight(MW): 240.34
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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The population of cmyb1kdrl1 cells in Tg(cmyb:GFP/kdrl:mCherry) embryos was decreased in JSH-23–treated embryos. White arrowheads mark cmyb1kdrl1 cells in the AGM region at 36 hpf. Right panel, Quantification of cmyb1kdrl1 cells.
Blood, 2015, 125(7): 1098-106 . JSH-23 purchased from Selleck.
Pancreatic acini exposed for 1 h to 300 μM of oleic acid (OA) or linoleic acid (LA) were pre-treated for 45 min with the vehicle (DMSO), JSH-23 (30 μM) or SH-4-54 (10 μM). CCL2 mRNA expression was analyzed by qRT-PCR with 18S as internal standard. *p<0.05, **p<0.01 as compared with untreated acini, ♦♦p<0.01 as compared with OA- or LA-treated acini.
Biochim Biophys Acta, 2015, 1852(12):2671-7. JSH-23 purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||JSH-23 is an inhibitor of NF-κB transcriptional activity with IC50 of 7.1 μM in RAW 264.7 cell line.|
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.  JSH-23 also decreases NO production and neuronal migration in LPS activated cultures primary cultures from developing mouse cerebellum.  Moreover, JSH-23 augments cisplatin cytotoxicity in ovarian cancer cells with CI values ranging from 0.35 to 0.85. 
|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. |
Measurement of NF-κB transcriptional activity: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.
|In vitro||DMSO||48 mg/mL (199.71 mM)|
|Ethanol||20 mg/mL (83.21 mM)|
* 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.
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