| CAS |
749886-87-1 |
| Chinese Name |
4-甲基-N1-(3-苯基丙基)-1,2-苯二胺 |
| English Name |
JSH 23 |
| Synonyms |
IN1201;JSH-23;FD5025;NF-kappaBActivationInhibitorII,JSH-23 |
| Molecular Formula |
C16H20N2 |
| Molecular Weight |
240.34 |
| Solubility |
Soluble in DMSO |
| Purity |
≥98% |
| Appearance |
Solid |
| Storage |
Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD09753595 |
| SMILES |
NC1=CC(C)=CC=C1NCCCC2=CC=CC=C2 |
| InChIKey |
YMFNPBSZFWXMAD-UHFFFAOYSA-N |
| InChI |
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 |
| PubChem CID |
16760588 |
| Target Point |
NF-kB |
| Passage |
NF-κB |
| Background |
JSH-23 is an NF-κB inhibitor. |
| Biological Activity |
JSH-23是 NF-κB 抑制剂，抑制NF-κB转录活性，IC50 为7.1 μM。SH-23以剂量依赖性方式抑制脂多糖（LPS）诱导的染色质浓缩，对应于3μM时44±4％抑制，10μM时为63±5％，30μM时为93±3％。 [1-4] |
| In Vitro |
JJSH-23(5，10和15μM)显著降低LPS激活细胞中的平均神经元迁移[2]。与转染蛋白或JSH-的作用相比，用JSH-23和临床无效的转移蛋白以其IC50浓度(130μM移植和20μMJSH-23)共同处理A2780细胞72小时也导致细胞活力的更显著降低[3]。 |
| In Vivo |
JSH-23(1和3 mg/kg，po)显著逆转糖尿病动物神经传导和神经血流缺陷，降低神经脂质过氧化，部分补充糖尿病大鼠神经中GSH耗尽水平[4]。 |
| Cell Experiment |
将用JSH-23孵育的巨噬细胞RAW 264.7用1μg/ mL LPS和/或样品处理24小时。将细胞用1μg/ mL DAPI在37℃下染色30分钟，然后使用荧光显微镜在300-500nm激发下进行分析。具有包含明显浓缩的染色质的细胞核或具有片段化细胞核的细胞被评分为细胞凋亡指数。 |
| Animal Experiment |
使用雄性Sprague Dawley大鼠(250-270g)并随意喂食标准大鼠饮食和水。在柠檬酸盐缓冲液中通过单剂量链脲佐菌素(STZ，55mg/kg，腹膜内)诱导糖尿病。 STZ给药后48小时收集血样。血浆葡萄糖水平超过250mg/dL的大鼠被认为是糖尿病患者并且进一步考虑用于研究。实验组包括非糖尿病对照大鼠(ND)，糖尿病对照大鼠(STZ-D)和用两剂JSH-23治疗的糖尿病大鼠(分别为STZ-D + JSH 1和STZ-D + JSH 3，对于1和3mg/kg，在0.5％羧甲基纤维素钠中口服)。诱导糖尿病6周后，每天给药一次，持续2周。在给予最后一剂后24小时进行功能，行为和生物化学实验。 |
| Data Literature Source |
[1]. Shin，H.M.，et al. Inhibitory action of novel aromatic diamine compound on lipopolysaccharide-induced nuclear translocation of NF-kappaB without affecting IkappaB degradation. FEBS Lett，2004. 571(1-3): p. 50-4.
[2]. Arias-Salvatierra，D.，et al. Role of nitric oxide produced by iNOS through NF-kappaB pathway in migration of cerebellar granule neurons induced by Lipopolysaccharide. Cell Signal，2011. 23(2): p. 425-35.
[3]. Kasparkova，J.，et al. Different affinity of nuclear factor-kappa B proteins to DNA modified by antitumor cisplatin and its clinically ineffective trans isomer. FEBS J，2014. 281(5): p. 1393-408.
[4]. Kumar，A.，et al. JSH-23 targets nuclear factor-kappa B and reverses various deficits in experimental diabetic neuropathy: effect on neuroinflammation and antioxidant defence. Diabetes Obes Metab，2011. 13(8): p. 750-8 |
| Unit |
Piece |
| Specification |
5mg 25mg |
English
中文
Manual Download
