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。


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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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| 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. |
| 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. |
| 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. |
| 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 |
|
| 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 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
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