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JSH-23

现货
Catalog No.
B1645
NF-κB抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 950.00
现货
5mg
¥ 880.00
现货
25mg
¥ 3,290.00
现货

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Background

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.

文献引用

1. Linnan Yang, Jing Sun, et al. "Synergetic Functional Nanocomposites Enhance Immunotherapy in Solid Tumors by Remodeling the Immunoenvironment." Advanced Science. 16 February 2019.
2. Lee YC, Wang LJ, et al. "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
3. Dela Pena-Ponce MG, Jimenez MT, et al. "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

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt240.34
Cas No.749886-87-1
FormulaC16H20N2
Solubility≥24mg/mL in DMSO
Chemical Name4-methyl-1-N-(3-phenylpropyl)benzene-1,2-diamine
SDFDownload SDF
Canonical SMILESCC1=CC(=C(C=C1)NCCCC2=CC=CC=C2)N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

LPS刺激的RAW264.7细胞

溶解方法

在DMSO中的溶解度>12mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0, 1, 3, 10和30 μM

应用

在LPS刺激的RAW264.7细胞中,JSH-23以剂量依赖性方式抑制LPS诱导的SEAP表达,在3μM,10μM和30μM时分别抑制23±3%,68±3%和103±4%。JSH-23也剂量依赖性地降低LPS诱导的NF-κB的DNA结合活性。 JSH-23显示了对LPS诱导的促炎转录物表达的不同抑制效果。

动物实验[2]:

动物模型

顺铂诱导的急性肾损伤(AKI)雄性C57BL / 6小鼠

剂量

20 mg/kg(顺铂注射前8小时给药10 mg/kg,顺铂注射后第1天和第2天为5mg / kg)或40mg / kg(顺铂注射前8小时给药20mg / kg,顺铂注射后第1天为20mg / kg); 腹膜内(IP)注射

应用

在顺铂诱导的AKI雄性C57BL / 6小鼠中,JSH-23(总剂量为40mg / kg)显著降低BUN,血清肌酐和血清NGAL。JSH-23导致肾脏中ATN评分和MPO活性显著降低,但不是肾小管细胞凋亡评分。JSH-23也显著降低IL-1,IL-6,CXCL1和TNF-α。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

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.

生物活性

描述 JSH-23是NF-κB转录活性的抑制剂,IC50值为7.1 μM。
靶点 NF-κB          
IC50 7.1 μM          

质量控制

化学结构

JSH-23

相关生物数据

JSH-23

相关生物数据

JSH-23

相关生物数据

JSH-23