JSH-23
(Synonyms: 4-甲基-N1-(3-苯基丙基)-1,2-苯二胺) 目录号 : GC11438
JSH-23 对核转位和 NF-κB 转录活性具有抑制作用，在脂多糖 (LPS) 刺激的巨噬细胞中 IC50 值为 7.1 μM RAW 264.7 。
Cas No.:749886-87-1
Sample solution is provided at 25 µL, 10mM.
JSH-23, exhibited inhibitory effect on nuclear translocation and NF-κB transcriptional activity with an IC50 value of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 [1].
JSH-23 (1 μM) monotherapy significantly reduced the chemotactic sensitivity of the cells to SDF1. The co-treatment with cordycepin (10 μM) and JSH-23 (1 μM) significantly inhibited the expression of CXCR4 [2].
JSH-23 (1 and 3 mg/kg) treatment significantly reversed the nerve conduction and nerve blood flow deficits seen in diabetic animals [1]. Protein expression studies showed that nuclear translocation of p65/p50 subunit was inhibited by JSH-23 treatment in the sciatic nerve. The treatment also lowered the elevated IL-6, TNF-α, cyclo-oxygenase (COX-2) and inducible nitric oxide synthase (iNOS) levels/expression [1]. Mice were treated with JSH-23 (20 or 40 mg/kg) which directly affects NF-κB transcriptional activity. Kidney function, tubular injury (ATN, serum neutrophil gelatinase-associated lipocalin [NGAL], but not apoptosis) and myeloperoxidase (MPO) activity were significantly improved by JSH-23 (40 mg/kg) [3].
References:
[1]. Kumar A, Negi G, Sharma S S. JSH 23 targets nuclear factor kappa B and reverses various deficits in experimental diabetic neuropathy: effect on neuroinflammation and antioxidant defence[J]. Diabetes, Obesity and Metabolism, 2011, 13(8): 750-758.
[2]. Guo Z, Chen W, Dai G, et al. Cordycepin suppresses the migration and invasion of human liver cancer cells by downregulating the expression of CXCR4[J]. International journal of molecular medicine, 2020, 45(1): 141-150.
[3]. Ozkok A, Ravichandran K, Wang Q, et al. NF-κB transcriptional inhibition ameliorates cisplatin-induced acute kidney injury (AKI)[J]. Toxicology letters, 2016, 240(1): 105-113
JSH-23 对核转位和 NF-κB 转录活性具有抑制作用，在脂多糖 (LPS) 刺激的巨噬细胞中 IC50 值为 7.1 μM RAW 264.7 [1]。
JSH-23 (1 μM) 单一疗法显着降低了细胞对 SDF1 的趋化敏感性。虫草素（10 μM）和JSH-23（1 μM）联合处理显着抑制了CXCR4[2]的表达。
JSH-23（1 和 3 mg/kg）治疗可显着逆转糖尿病动物中观察到的神经传导和神经血流缺陷[1]。蛋白质表达研究表明，坐骨神经中的 JSH-23 处理可抑制 p65/p50 亚基的核转位。该治疗还降低了升高的 IL-6、TNF-α、环氧合酶 (COX-2) 和诱导型一氧化氮合酶 (iNOS) 水平/表达 [1]。用直接影响 NF-κB 转录活性的 JSH-23（20 或 40 mg/kg）处理小鼠。 JSH-23 (40 mg/kg) 显着改善肾功能、肾小管损伤（ATN、血清中性粒细胞明胶酶相关脂质运载蛋白 [NGAL]，但不影响细胞凋亡）和髓过氧化物酶 (MPO) 活性[3].
| Cell experiment [1]: | |
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Cell lines |
Normal human lung epithelial cell line BEAS-2B and human lung cancer cell line A549 |
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Preparation Method |
Cells were treated with different concentrations of NF-κB inhibitor JSH-23 (5, 10, 20, 30, 40, and 50 µM, respectively) for 24 h. |
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Reaction Conditions |
5, 10, 20, 30, 40, and 50 µM for 24 hours |
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Applications |
With the increase in JSH-23 concentration, the inhibition rate for cell viability was gradually increased, and significant differences existed when the JSH-23 concentration was greater than 20 µM. |
| Animal experiment [2]: | |
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Animal models |
Male 12-week-old normotensive Wistar rats and Prague hereditary hypertriglyceridemic (HTG) rats |
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Preparation Method |
Mice were given a total dose of either 20 mg/kg of JSH-23 (10 mg/kg 8 h prior to cisplatin injection and 5 mg/kg on days 1 and 2 after cisplatin injection) or a total dose of 40 mg/kg body weight of JSH-23 (20 mg/kg 8 h prior to cisplatin injection and 20 mg/kg on day 1 after cisplatin injection) or vehicle (DMSO). |
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Dosage form |
Intraperitoneal injection, 5, 10, 20 mg/kg |
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Applications |
JSH-23 (total dose of 40 mg/kg) resulted in a significant decrease in BUN, serum creatinine and serum NGAL. NGAL is an early diagnostic biomarker of cisplatin-induced AKI. JSH-23 had no effect on BUN and serum creatinine in vehicle-treated mice (Fig. 2). |
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References: [1]: Huang L, Li F, Deng P, et al. MicroRNA-223 promotes tumor progression in lung cancer A549 cells via activation of the NF-κB signaling pathway[J]. Oncology research, 2016, 24(6): 405. | |
| Cas No. | 749886-87-1 | SDF | |
| 别名 | 4-甲基-N1-(3-苯基丙基)-1,2-苯二胺 | ||
| 化学名 | 4-methyl-1-N-(3-phenylpropyl)benzene-1,2-diamine | ||
| Canonical SMILES | CC1=CC(=C(C=C1)NCCCC2=CC=CC=C2)N | ||
| 分子式 | C16H20N2 | 分子量 | 240.34 |
| 溶解度 | ≥ 24mg/mL in DMSO | 储存条件 | Store at -20° C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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