JSH-23

JSH-23  纯度: 99.11%

JSH-23 是 NF-κB 抑制剂,作用于脂多糖刺激的巨噬细胞 RAW 264.7,抑制 NF-κB 转录活性,IC50 为 7.1 μM。JSH-23 抑制 NF-κB p65 的核易位而不影响 IκBα 降解。

JSH-23

JSH-23 Chemical Structure

CAS No. : 749886-87-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1191 In-stock
5 mg ¥1083 In-stock
10 mg ¥1469 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

JSH-23 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Diabetes Related Compound Library
  • Oxygen Sensing Compound Library
  • Pyroptosis Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Obesity Compound Library
  • Transcription Factor Targeted Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library

生物活性

JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation[1].

IC50 & Target[1]

NF-κB

7.1 μM (IC50, in RAW 264.7 cells)

体外研究
(In Vitro)

JSH-2 (1-300 μM; 24 hours) at <100 μm does not show significant cytotoxic effects on the raw 264.7 cells[1].
Nuclear amount of NF-κB p65 is markedly increased upon exposure to LPS for 1 h. Treatment of JSH-23 (30 μM; 1 hours) to LPS- stimulated RAW 264.7 cells decreases nuclear content of NF-κB p65 in a dose-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: Macrophages RAW 264.7
Concentration: 1, 3, 10, 30, 100, 300 μM
Incubation Time: 24 hours
Result: Did not show significant cytotoxic effects at <100 μM.

Western Blot Analysis[1]

Cell Line: Macrophages RAW 264.7 with LPS-stimulated
Concentration: 30 μM
Incubation Time: 1 hour
Result: Decreased nuclear content of NF-κB p65 in a dose-dependent manner, corresponding to 49±4% inhibition at 3 μM, 75±7% at 10 μM and 95±8% at 30 μM.

体内研究
(In Vivo)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague Dawley diabetic rats (250-270 g)[1]
Dosage: 1 mg/kg, 3 mg/kg
Administration: Orally administered; daily; for 2 weeks
Result: Produced significant improvement in motor nerve conduction velocity (MNCV).

分子量

240.34

Formula

C16H20N2

CAS 号

749886-87-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 56 mg/mL (233.00 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.40 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.40 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.40 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.40 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
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.