JSH-23
JSH-23 is an inhibitor of NF-κB transcriptional activity with IC50 value of 7.1μM [1].
JSH-23 is developed to inhibit NF-κB transcriptional activity in LPS-stimulated macrophages RAW 264.7. It shows a dose-dependent inhibition. This effect is not due to its cytotoxicity. In the same condition, JSH-23 is found to significantly decrease the LPS-induced DNA binding activity of NF-κB while decrease nuclear amount of NF-κB p65. JSH-23 plays these roles without affecting IκB degradation. In addition, JSH-23 also shows inhibition effects on the expression of the pro-inflammatory transcripts and enzymes, including IL-6, IL-1β, COX-2 and TNF-α. Furthermore, JSH-23 inhibits LPS-induced apoptotic chromatin condensation [1].
References:
[1] Shin HM, Kim MH, Kim BH, Jung SH, Kim YS, Park HJ, Hong JT, Min KR, Kim Y. Inhibitory action of novel aromatic diamine compound on lipopolysaccharide-induced nuclear translocation of NF-kappaB without affecting IkappaB degradation. FEBS Lett. 2004 Jul 30;571(1-3):50-4.
- 1. Jiao Li, Pan Li, et al. "Anemoside B4 alleviates DSS-induced colitis by inhibiting CD1d-dependent NLRP3 inflammasome activation in macrophages." British Journal of Pharmacology. 12 Sep 2023
- 2. Qiongqiong Zhou, Longfeng Zhang, et al. "Pseudorabies Virus Infection Activates the TLR-NF-κB Axis and AIM2 Inflammasome To Enhance Inflammatory Responses in Mice." J Virol. 2023 Mar 30;97(3):e0000323. PMID: 36877049
- 3. "Synergetic Functional Nanocomposites Enhance Immunotherapy in Solid Tumors by Remodeling the Immunoenvironment." Advanced Science. 16 February 2019.
- 4. "ABT-263-induced MCL1 upregulation depends on autophagy-mediated 4EBP1 downregulation in human leukemia cells." Cancer Lett. 2018 Jun 15;432:191-204. PMID:29913235
- 5. "The Helicobacter pylori type IV secretion system promotes IL-8 synthesis in a model of pediatric airway epithelium via p38 MAP kinase." PLoS One. 2017 Aug 15;12(8):e0183324. PMID:28813514
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 240.34 |
| Cas No. | 749886-87-1 |
| Formula | C16H20N2 |
| Solubility | ≥24 mg/mL in DMSO; insoluble in H2O; ≥17.1 mg/mL in EtOH with ultrasonic |
| Chemical Name | 4-methyl-1-N-(3-phenylpropyl)benzene-1,2-diamine |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=C(C=C1)NCCCC2=CC=CC=C2)N |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
LPS-stimulated RAW264.7 cells |
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Preparation method |
The solubility of this compound in DMSO is >12mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0, 1, 3, 10 and 30 μM |
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Applications |
In LPS-stimulated RAW264.7 cells, JSH-23 inhibited LPS-induced SEAP expression in a dose-dependent way by 23±3%, 68±3% and 103±4% at 3 μM, 10 μM and 30 μM, respectively. JSH-23 also dose-dependently decreased LPS-induced DNA binding activity of NF-κB. JSH-23 showed differential inhibitory effects on LPS-induced expressions of the pro-inflammatory transcripts. |
| Animal experiment [2]: | |
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Animal models |
cisplatin-induced acute kidney injury (AKI) male C57BL/6 mice |
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Dosage form |
20 mg/kg (10 mg/kg 8 hours prior to cisplatin injection and 5 mg/kg on days 1 and 2 after cisplatin injection) or 40 mg/kg(20 mg/kg 8 hours prior to cisplatin injection and 20 mg/kg on day 1 after cisplatin injection); intraperitoneal (IP) injection |
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Application |
In cisplatin-induced AKI male C57BL/6 mice, JSH-23 (total dose of 40 mg/kg) significantly reduced BUN, serum creatinine and serum NGAL. JSH-23 resulted in a significant decrease in ATN score and MPO activity but not tubular apoptosis score in the kidney. JSH-23 also significantly decreased IL-1, IL-6, CXCL1 and TNF-α. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Shin HM, Kim MH, Kim BH, Jung SH, Kim YS, Park HJ, Hong JT, Min KR, Kim Y. Inhibitory action of novel aromatic diamine compound on lipopolysaccharide-induced nuclear translocation of NF-kappaB without affecting IkappaB degradation. FEBS Lett. 2004 Jul 30;571(1-3):50-4. [2] Ozkok A1, Ravichandran K1, Wang Q1, et al. NF-κB transcriptional inhibition ameliorates cisplatin-induced acute kidney injury (AKI). Toxicol Lett. 2016 Jan 5;240(1):105-13. |
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| Description | JSH-23 is an inhibitor of NF-κB transcriptional activity with an IC50 value of 7.1 μM. | |||||
| Targets | NF-κB | |||||
| IC50 | 7.1 μM | |||||
Quality Control & MSDS
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