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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
JSH-23 (JSH23; JSH 23) is a novel NF-κB transcriptional activity inhibitor with potential anti-inflammatory and anti-diabetic properties. With an IC50 of 7.1 μM in RAW 264.7 cells, it inhibits NF-κB.
| Targets |
NF-κB (IC50 = 7.1 μM)
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|---|---|
| ln Vitro |
JSH-23 inhibits LPS-induced nuclear translocation of NF-κB p65 without affecting IκBα degradation. JSH-23 inhibits LPS-induced apoptotic chromatin condensation but has negligible cytotoxic effects on RAW 264.7 cells at concentrations below <100 μM. [1] In primary cultures from developing mouse cerebellum that have been exposed to LPS, JSH-23 also reduces NO production and neuronal migration. [2] Additionally, JSH-23 increases the cytotoxicity of cisplatin in ovarian cancer cells, with CI values ranging from 0.35 to 0.85. [3]
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| ln Vivo |
JSH-23 (3 mg/kg) significantly improves antioxidant defense, reduces neuroinflammation, and restores nerve conduction and blood flow deficits in diabetic rats. [4]
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| Enzyme Assay |
LPS (1 g/ml) and/or sample are administered to RAW 264.7 macrophages that have been stable transfected with the reporter plasmid of pNF-κB-SEAP-NPT for 16 hours. In the cell-free culture media, SEAP activity serves as the reporter, and is tallied as follows. The media is decanted 24 hours after plating single cell-derived stable transfectants in a 5 ml T-25 flask. Cells are now given two phosphate-buffered saline washes, and incubations are started by adding fresh media. Following a 24-hour incubation period, chemicals are added to the culture medium. At 0, 3, 20, 24, 48, and 72 hours, aliquots (25 ml) of medium from a control or chemically treated cultures are taken, heated at 65°C for 5 min to kill alkaline phosphatase activity, and then used right away or stored at -20°C. In each well of the 96-well plates, mixtures made up of dilution buffer (25 ml), assay buffer (97 ml), culture media (25 ml), and 4-methylumbelliferyl phosphate (MUP, 1 mM, 3 ml) are incubated for 60 min at room temperature and in the dark. Using a 96-well plate fluorometer and excitation at 360 nm, the SEAP/MUP'sproduct's fluorescenceis measured at 449 nm.
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| Cell Assay |
For 24 hours, different concentrations of the JSH-23 compound are incubated with RAW 264.7 macrophages. After applying WST-1 solution to the cells, the absorbance at 450 nm is measured.
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| Animal Protocol |
STZ-induced diabetic rats
~3 mg/kg Oral administration |
| References | |
| Additional Infomation |
JSH-23 is a diamine that is 1,2-phenylenediamine carrying a methyl substituent at position 4 and a 3-phenylpropyl substituent at position N1. It has a role as a NF-kappaB inhibitor. It is a diamine and a substituted aniline. It is functionally related to a 1,2-phenylenediamine.
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| Molecular Formula |
C16H20N2
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|---|---|---|
| Molecular Weight |
240.34
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| Exact Mass |
240.162
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| Elemental Analysis |
C, 79.96; H, 8.39; N, 11.66
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| CAS # |
749886-87-1
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| Related CAS # |
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| PubChem CID |
16760588
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| Appearance |
white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
418.7±40.0 °C at 760 mmHg
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| Melting Point |
104.4-105.0℃
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| Flash Point |
245.0±30.9 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.630
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| LogP |
3.66
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
18
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| Complexity |
223
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N([H])(C1C([H])=C([H])C(C([H])([H])[H])=C([H])C=1N([H])[H])C([H])([H])C([H])([H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H]
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| InChi Key |
YMFNPBSZFWXMAD-UHFFFAOYSA-N
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| 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
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| Chemical Name |
4-methyl-1-N-(3-phenylpropyl)benzene-1,2-diamine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1608 mL | 20.8039 mL | 41.6077 mL | |
| 5 mM | 0.8322 mL | 4.1608 mL | 8.3215 mL | |
| 10 mM | 0.4161 mL | 2.0804 mL | 4.1608 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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