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JSH-23 {[allProObj[0].p_purity_real_show]}

货号:A153850 同义名: NF-κB Activation Inhibitor II

JSH-23是一种 NF-κB 抑制剂,在脂多糖 (LPS) 刺激的 RAW 264.7 巨噬细胞中,以 IC50 为 7.1 μM 抑制 NF-κB 的转录活性。它通过抑制 NF-κB p65 的核转位而不影响 IκBα 的降解。

JSH-23 化学结构 CAS号:749886-87-1
JSH-23 化学结构
CAS号:749886-87-1
JSH-23 3D分子结构
CAS号:749886-87-1
JSH-23 化学结构 CAS号:749886-87-1
JSH-23 3D分子结构 CAS号:749886-87-1
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JSH-23 纯度/质量文件 产品仅供科研

货号:A153850 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 NF-κB 其他靶点 纯度
Ammonium pyrrolidine-1-carbodithioate 98%
QNZ ++++

NF-κB, IC50: 11 nM

99%+
Sodium 4-Aminosalicylate Dihydrate 98%
Sodium Salicylate 95%
Parthenolide p53 97% HPLC
JSH-23 +

NF-κB, IC50: 7.1 μM

98%
Phenethyl caffeate 98%
Andrographolide 98+%
Curcumin Nrf2,HDAC 98%
SC75741 +++

NF-κB, EC50: 200 nM

99%+
CBL0137 HCl ++

NF-κB, EC50: 0.47 μM

p53 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

JSH-23 生物活性

靶点
  • NF-κB

    NF-κB, IC50:7.1 μM

描述 JSH-23 functions as an NF-κB inhibitor, effectively suppressing NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. It achieves this by impeding the nuclear translocation of NF-κB p65 without impacting IκBα degradation[1].
体内研究

JSH-23 (1 mg/kg and 3 mg/kg; orally administered; daily; for 2 weeks) significantly mitigates nerve conduction and nerve blood flow deficits observed in diabetic rats[2].

体外研究

When administered at concentrations below 100 μM for 24 hours, JSH-2 does not induce significant cytotoxic effects on RAW 264.7 cells[1].

Upon exposure to LPS for 1 hour, the nuclear content of NF-κB p65 significantly increases. Treatment with JSH-23 (30 μM; 1 hour) reduces the nuclear content of NF-κB p65 in LPS-stimulated RAW 264.7 cells in a dose-dependent manner[1].

JSH-23 细胞实验

Cell Line
Concentration Treated Time Description References
L428 cells 100 μM 24 h Inhibited IL-6 secretion Cell Death Dis. 2016 Nov 10;7(11):e2457.
BMMs 25 μM 6 h JSH-23 inhibits NF-κB signaling pathway, reducing VEGF-C expression Nat Commun. 2016 Mar 1;7:10824.
primary hepatocytes from WT mice 20 µM 6 h JSH-23 inhibited LPS-induced upregulation of caspase-11 mRNA and protein expression Cell Mol Gastroenterol Hepatol. 2021;12(2):653-664.
PAM212 keratinocytes 20 µM 2 h JSH-23 reduced the TWEAK-enhanced Ro52 expression, indicating that the NF-κB pathway is involved in the TWEAK regulation of Ro52. Front Immunol. 2017 May 31;8:651.
T98G cells 200 µM 48 h To evaluate the effect of JSH-23 on T98G cells, results showed that JSH-23 significantly inhibited cell proliferation and induced apoptosis. Clin Transl Immunology. 2022 May 9;11(5):e1393.
LN229 cells 200 µM 48 h To evaluate the effect of JSH-23 on LN229 cells, results showed that JSH-23 significantly inhibited cell proliferation and induced apoptosis. Clin Transl Immunology. 2022 May 9;11(5):e1393.

JSH-23 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice CLP-induced sepsis model Intraperitoneal injection 20 mg/kg 2 hours before CLP and 12, 24, 48, and 72 hours after CLP To evaluate the therapeutic effect of JSH-23 on sepsis, the results showed that JSH-23 improved organ injury but did not significantly improve survival rate Cell Death Dis. 2022 Jul 28;13(7):653
Mice MCD-induced NASH model Oral gavage 3 mg/kg Once daily for 4 weeks JSH-23 prevented MCD-induced upregulation of caspase-11 mRNA and protein expression Cell Mol Gastroenterol Hepatol. 2021;12(2):653-664.
Mice Trauma-induced heterotopic ossification model Intraperitoneal injection 3 mg/kg Once daily for 3 weeks To evaluate the effect of JSH-23 on trauma-induced heterotopic ossification. The results showed that JSH-23 significantly reduced the senescent cell burden at the injury site and inhibited the eventual heterotopic ossification formation. Adv Sci (Weinh). 2023 Jul;10(19):e2207383
BALB/c nude mice Tumor xenograft model Intraperitoneal injection 5 mg/kg Once daily for 15 days To investigate whether PBK enhances olaparib resistance in ovarian cancer through the NF-κB pathway, results showed that JSH-23 blocked the resistance induced by PBK overexpression Exp Mol Med. 2022 Jul;54(7):999-1010
Nude mice GBM xenograft model Intraperitoneal injection 25 mg/kg Every 2 days for 21 days To evaluate the effect of JSH-23 on the GBM xenograft model, results showed that JSH-23 significantly inhibited tumor growth. Clin Transl Immunology. 2022 May 9;11(5):e1393.
Mice Mmp14/C0//C0 mice Intraperitoneal injection 10 mg/kg Daily for 12 days JSH-23 significantly reduces corneal lymphangiogenesis in Mmp14/C0//C0 mice by inhibiting NF-κB signaling pathway Nat Commun. 2016 Mar 1;7:10824.

JSH-23 动物研究

Dose Rat: 1 mg/kg - 3 mg/kg[3] (p.o.) Mice: 20 mg/kg, 40 mg/kg[4] (i.p.)
Administration p.o., i.p.

JSH-23 参考文献

[1]Shin HM, et al. 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]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 Aug;13(8):750-8.

JSH-23 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.16mL

0.83mL

0.42mL

20.80mL

4.16mL

2.08mL

41.61mL

8.32mL

4.16mL

JSH-23 技术信息

CAS号749886-87-1
分子式C16H20N2
分子量 240.34
SMILES Code NC1=CC(C)=CC=C1NCCCC2=CC=CC=C2
MDL No. MFCD09753595
别名 NF-κB Activation Inhibitor II
运输蓝冰
InChI Key YMFNPBSZFWXMAD-UHFFFAOYSA-N
Pubchem ID 16760588
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

溶解方案

DMSO: 55 mg/mL(228.84 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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