NF-κβ activator 1是一种有效的NF-κβ信号通路激活剂，其EC50值为0.9μM，并可诱导超氧化物歧化酶（SOD2）mRNA的表达。
Cas No.:2387524-59-4
Sample solution is provided at 25 µL, 10mM.
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NF-κβ activator 1 is a potent activator of the NF-κβ signaling pathway, with an EC₅₀ value of 0.9μM, NF-κβ activator 1 can induce the expression of superoxide dismutase (SOD2) mRNA[1-2]. By activating the NF-κβ pathway, NF-κβ activator 1 is involved in regulating inflammatory responses and immune cell functions. NF-κβ activator 1 can be used in research related to inflammatory diseases and immune-related disorders [3-4].
In vitro, PC3 prostate cancer cells overexpressing MGLL were pretreated with NF-κβ activator 1 (1μM) for 6h, followed by incubation with Docetaxel (10nM) for 48h. NF-κβ activator 1 significantly reversed the inhibitory effects of MGLL overexpression on NF-κβ p65 phosphorylation and nuclear translocation, restored the expression of senescence-associated secretory phenotype (N-SASP) factors such as IL6 and CXCL8, and attenuated the suppression of cell proliferation induced by the combination of MGLL overexpression and Docetaxel[5]. In PC12 neuronal-like cells, pretreatment with NF-κβ activator 1 (1μM) for 6h, followed by treatment with the CX3CR1 inhibitor AZD8797 (1μM) for 12h, reversed the AZD8797-induced inhibition of NF-κβ pathway proteins p-IκB and p-p65 expression and restored the expression level of the 5-hydroxytryptamine receptor 2A (5-HTR2a)[6].
References:
[1] Mathew B, Ruiz P, Dutta S, et al. Structure-activity relationship (SAR) studies of N-(3-methylpyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine (SRI-22819) as NF-ҡB activators for the treatment of ALS. Eur J Med Chem. 2021 Jan 15;210:112952.
[2] He Y, Song W, Deng Y, et al. Liraglutide promotes osteogenic differentiation of mesenchymal stem cells by inhibiting M1 macrophage polarization and CXCL9 release in vitro. Mol Cell Endocrinol. 2025 Feb 1;597:112441.
[3] Wang S, Li F, Zhang L, et al. HMGB1 inhibits the IFN-γ-induced PD-L1 expression in NSCLC. J Immunol. 2025 Sep 1;214(9):2480-2488.
[4] Wu W, Yue S, Wang X, et al. Docosahexaenoic acid mitigates experimental autoimmune prostatitis by inhibiting Th17 cell differentiation via the PPARγ/NF-κB/IL-17A pathway. Clin Exp Immunol. 2025 Jan 21;219(1):uxaf055.
[5] Yu J, Zhang M, Li T, et al. Monoacylglycerol lipase blockades the senescence-associated secretory phenotype by interfering with NF-κB activation and promotes docetaxel efficacy in prostate cancer. Oncogene. 2024 Sep;43(38):2835-2849.
[6] Pei J, Zou Y, Wan C, et al. CX3CR1 mediates motor dysfunction in mice through 5-HTR2a. Behav Brain Res. 2024 Mar 12;461:114837.
NF-κβ activator 1是一种有效的NF-κβ信号通路激活剂，其EC50值为0.9μM，并可诱导超氧化物歧化酶（SOD2）mRNA的表达[1-2]。NF-κβ activator 1通过激活NF-κB通路，参与调节炎症反应及免疫细胞功能，NF-κβ activator 1可用于炎症性疾病及免疫相关疾病的相关研究[3-4]。
在体外，NF-κβ activator 1（1μM）预处理MGLL过表达的PC3前列腺癌细胞6小时，随后使用Docetaxel（10nM）孵育细胞48小时，NF-κβ activator 1显著逆转MGLL过表达对NF-κβ p65磷酸化及核转位的抑制作用，并恢复IL6、CXCL8等衰老相关分泌表型（N-SASP）因子的表达，同时削弱MGLL过表达联合Docetaxel对细胞增殖的抑制效果[5]。NF-κβ activator 1（1μM）处理PC12神经元样细胞6小时，随后使用CX3CR1抑制剂AZD8797（1μM）孵育12h，NF-κβ activator 1可逆转AZD8797对NF-κβ通路蛋白p-Iκβ及p-p65表达的抑制，并恢复5-羟色胺受体2A（5-HTR2a）的表达水平[6]。
| Cell experiment [1]: | |
Cell lines | PC3 cells (human prostate cancer cell line) and PC12 cells (rat neuronal cell line). |
Preparation Method | PC3 cells were maintained in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS). PC12 cells were cultured in RPMI-1640 medium containing 10% FBS. For treatment, PC3 cells stably overexpressing MGLL (Over-MGLL) and control (Vector) cells were pretreated with NF-κβ activator 1 (1µM) for 6 hours, followed by Docetaxel (10nM) treatment for 48 hours. PC12 cells were treated with the CX3CR1 inhibitor AZD8797 (1µM) for 12 hours, with or without NF-κβ activator 1 (1µM) pretreatment for 6 hours. |
Reaction Conditions | 1μM; 6h (pretreatment). |
Applications | In PC3 cells, NF-κβ activator 1 significantly reversed the MGLL overexpression-induced suppression of NF-κβ p65 phosphorylation (Ser536) and IκBα phosphorylation (Ser32/36), and restored the nuclear translocation of NF-κβ p65. Consequently,NF-κβ activator 1 rescued the expression of NF-κβ-driven senescence-associated secretory phenotype (N-SASP) factors, including IL6 and CXCL8, and attenuated the growth inhibition caused by the combination of MGLL overexpression and Docetaxel. |
References: | |
| Cas No. | 2387524-59-4 | SDF | |
| 分子式 | C16H11FN2O2S | 分子量 | 314.33 |
| 溶解度 | DMSO : 125 mg/mL (397.67 mM; Need ultrasonic) | 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 | 3.1814 mL | 15.9068 mL | 31.8137 mL |
| 5 mM | 636.3 μL | 3.1814 mL | 6.3627 mL |
| 10 mM | 318.1 μL | 1.5907 mL | 3.1814 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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