product name JSH-23
References: FEBS Lett. 2004 Jul 30;571(1-3):50-4; Diabetes Obes Metab. 2011 Aug;13(8):750-8.
240.34
Formula
C16H20N2
CAS No.
749886-87-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 48 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: 20 mg/mL (83.2 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: 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. Cell Assay: 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. |
|---|---|
| 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. |
| Animal model | STZ-induced diabetic rats |
| Formulation & Dosage | Dissolved in 0.5% sodium carboxymethyl cellulose; 3 mg/mL, Oral administration |
| References | FEBS Lett. 2004 Jul 30;571(1-3):50-4; Diabetes Obes Metab. 2011 Aug;13(8):750-8. |
