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JSH-23
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JSH-23图片
CAS NO:749886-87-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
JSH-23 (JSH23; JSH 23) was designed as a nove and potent inhibitor of NF-κB transcriptional activity with potential anti-inflammatory and anti-diabetic activity. It inhibits NF-κB with an IC50 of 7.1 μM in RAW 264.7 cells.
理化性质和储存条件
Molecular Weight (MW)240.34
FormulaC16H20N2
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)
Other infoChemical Name: 4-methyl-N1-(3-phenylpropyl)benzene-1,2-diamine
InChi Key: YMFNPBSZFWXMAD-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H20N2/c1-13-9-10-16(15(17)12-13)18-11-5-8-14-6-3-2-4-7-14/h2-4,6-7,9-10,12,18H,5,8,11,17H2,1H3
SMILES Code: NC1=CC(C)=CC=C1NCCCC2=CC=CC=C2
SynonymsJSH 23; JSH-23; JSH23;
实验参考方法
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 VivoJSH-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 modelSTZ-induced diabetic rats
Formulation & DosageDissolved 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.