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。
生物活性 | JSH-23 is anNF-κBinhibitor which inhibitsNF-κBtranscriptional activity with anIC50of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation ofNF-κBp65 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].
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[2].
Animal Model: | Male Sprague Dawley diabetic rats (250-270 g)[2] | 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 | |
性状 | |
Formula | |
CAS 号 | |
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 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。 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本网站选购。
|