1. Signaling Pathways
  2. NF-κB
  3. NF-κB

NF-κB (核因子κB)

Nuclear factor-κB; Nuclear factor-kappaB

NF-κB(活化 B 细胞的核因子 κ 轻链增强子)是一种控制 DNA 转录的蛋白质复合物。NF-κB 存在于几乎所有动物细胞类型中,并参与细胞对压力、细胞因子、自由基、紫外线照射、氧化 LDL 以及细菌或病毒抗原等刺激的反应。NF-κB 在调节对感染的免疫反应中起着关键作用。NF-κB 的错误调节与癌症、炎症和自身免疫性疾病、感染性休克、病毒感染和免疫发育不当有关。NF-κB 还与突触可塑性和记忆过程有关。哺乳动物 NF-κB 家族中有五种蛋白质:NF-κB1、NF-κB2、RelA、RelB、c-Rel。

NF-κB (Nuclear factor kappa-light-chain-enhancer of activated B cells) is a protein complex that controls transcription of DNA. NF-κB is found in almost all animal cell types and is involved in cellular responses to stimuli such as stress, cytokines, free radicals, ultraviolet irradiation, oxidized LDL, and bacterial or viral antigens. NF-κB plays a key role in regulating the immune response to infection. Incorrect regulation of NF-κB has been linked to cancer, inflammatory, and autoimmune diseases, septic shock, viral infection, and improper immune development. NF-κB has also been implicated in processes of synaptic plasticity and memory. There are five proteins in the mammalian NF-κB family: NF-κB1, NF-κB2, RelA, RelB, c-Rel.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-124179
    IT-901 Inhibitor 99.32%
    IT-901 是一种具有口服活性且有效的 NF-κB 亚基 c-Rel 抑制剂,对 NF-κBc-Rel 与 DNA 结合的 IC50 分别为 0.1 μM,3 μM。IT-901 是一种具有生物活性的萘硫代巴比妥酸酯衍生物,具有用于人类淋巴瘤和改善移植物抗宿主病 (GVHD) 的潜力。
    IT-901
  • HY-147972
    NF-κB/MAPK-IN-1 Inhibitor 98.71%
    NF-κB/MAPK-IN-1 (compound 11a) 是一种有效的 NF-κBMAPK 通路抑制剂。NF-κB/MAPK-IN-1 对 NO 生成具有抑制作用,其 IC50 为6.96 μM。NF-κB/MAPK-IN-抑制 LPS 诱导的 iNOSCOX-2ERΚP38 激活。 NF-κB/MAPK-IN-1 可抑制 LPS 诱导的巨噬细胞炎症反应。 NF-κB/MAPK-IN-1 可用于类风湿关节炎 (RA) 的研究。
    NF-κB/MAPK-IN-1
  • HY-N2056
    11-​Keto-​beta-​boswellic acid

    11-酮-β-乳香酸

    Inhibitor 99.96%
    11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) 是一种五环三萜酸,来自俗称印度乳香 (Indian Frankincense) 的乳香树 (Boswellia serrate) 树皮的油树脂。 11-Keto-beta-boswellic acid 具有抗炎活性,主要是由于抑制 5-脂氧合酶 (5-lipoxygenase; 5-LOX)白三烯 (leukotriene)NF-κB的激活和肿瘤坏死因子 α 的产生。
    11-​Keto-​beta-​boswellic acid
  • HY-128423
    Tylvalosin tartrate

    酒石酸乙酰异戊酰泰乐菌素

    Inhibitor 98.77%
    Tylvalosin (Acetylisovaleryltylosin) tartrate 是一种具有口服活性的,广谱大环内酯抗生素 (antibiotic>),显示抗菌活性。Tylvalosin tartrate 是一种抗病毒试剂,可用于研究 PRRSV 感染。Tylvalosin tartrate 诱导细胞凋亡 (apoptosis)。Tylvalosin tartrate 还具有抗炎活性,缓解氧化应激,并通过抑制 NF-κB 激活来缓解急性肺损伤。
    Tylvalosin tartrate
  • HY-N0747
    Oxypeucedanin

    氧化前胡素

    Inhibitor 99.50%
    Oxypeucedanin 是可在 Angelica dahurica 中发现的呋喃香豆素衍生物。Oxypeucedanin 是一种具有口服活性的 PI3K/AKT/NF-κBMAPKROS 抑制剂。Oxypeucedanin 可诱导细胞周期阻滞和细胞凋亡 (apoptosis)。Oxypeucedanin 可抑制 hKv1.5 通道电流 (IC50: 76 nM)。Oxypeucedanin 具有抗癌、抗炎、抗氧化和抗心律失常活性。
    Oxypeucedanin
  • HY-N0841
    Bruceine A

    鸦胆子素A

    Inhibitor 99.89%
    Bruceine A (Dihydrobrusatol) 是一种天然的苦木素。Bruceine A 是一种寄生虫 (parasites),NF-κB,和 PFKFB4 (Kd: 44 nM) 抑制剂。Bruceine A 是一种 P38α MAPK 激活剂。Bruceine A 具有抗寄生虫活性。Bruceine A 具有抗肿瘤活性并抑制癌细胞迁移。Bruceine A 可阻断细胞周期并诱导细胞凋亡 (apoptosis)。Bruceine A 可用于寄生虫、胰腺癌和乳腺癌的研究。
    Bruceine A
  • HY-B0130
    Perindopril

    培哚普利

    98.11%
    Perindopril erbumine 是一种血管紧张素转换酶 (angiotensin-converting enzyme) 抑制剂,调节NF-κB 和 STAT3 信号传导,抑制胶质细胞活化和神经炎症,可用于慢性肾脏病和高血压的研究。
    Perindopril
  • HY-P1847A
    IKKγ NBD Inhibitory Peptide TFA 98.20%
    IKKγ NBD 抑制肽 TFA 是一种高度特异性的 NF-κB 抑制剂。IKKγ NBD 抑制肽 TFA 通过阻断 IKKγ/NEMO 结合域 (NBD) 与 IKKα 和 IKKβ 之间的相互作用,而阻断 TNF-α 诱导的 NF-κB 激活。IKKγ NBD 抑制肽 TFA 可显著降低炎症、改善脑缺血所致的神经功能缺损。
    IKKγ NBD Inhibitory Peptide TFA
  • HY-N1193
    Sulfuretin

    硫黄菊素

    Inhibitor 99.36%
    Sulfuretin 通过抑制 NF-κB 通路来抑制炎症反应。 Sulfuretin 可用于过敏性气道炎症的研究。Sulfuretin 减少氧化应激、血小板聚集和诱变。Sulfuretin 是一种竞争性的有效单酚酶和二酚酶活性抑制剂,IC50 为 13.64 μM。
    Sulfuretin
  • HY-19696B
    Tauroursodeoxycholate dihydrate

    牛磺熊去氧胆酸二水合物

    Inhibitor 99.96%
    Tauroursodeoxycholate dehydrate 是口服活性的 Ursodeoxycholic acid (HY-13771) 牛磺酸共轭物。Tauroursodeoxycholate dehydrate 抑制 caspase-3/7、凋亡 (Apoptosis)、IRE1α/TRAF2/NF-κB,预防 JNK 磷酸化,抑制 ROS 生成,激活 Akt 信号传导。Tauroursodeoxycholate dehydrate 预防白内障形成、减轻 2 型糖尿病小鼠中的肾小管损伤、减轻肝脏 I/R 损伤、抑制非酒精性脂肪肝中肠道炎症和屏障破坏。
    Tauroursodeoxycholate dihydrate
  • HY-N6031
    Dendrophenol

    石斛酚

    Inhibitor 99.93%
    Dendrophenol (Moscatilin) 是一种 NF-κB 抑制剂,可抑制炎症反应。Dendrophenol 对多种肿瘤细胞具有杀伤作用,可诱导细胞周期阻滞和凋亡 (apoptosis)。Dendrophenol 具有抗肿瘤的活性。此外,Dendrophenol 可通过抑制 WNT3/β-catenin 的激活抑制血管钙化。
    Dendrophenol
  • HY-N3945
    Glaucine

    海罂粟碱

    Inhibitor 99.57%
    Glaucine (O,O-Dimethylisoboldine) 是一种从 Glaucium flavum 中提取的生物碱,具有镇咳、支气管扩张、抗炎、镇痛、解热和抗癌等多种活性。Glaucine 是一种选择性的、口服活性的磷酸二酯酶 4 (PDE4) 抑制剂,在人支气管和多形核白细胞中的Ki为 3.4 µM。Glaucine 通过拮抗钙离子通道 (calcium channel) 来诱导人离体支气管的松弛。此外,Glaucine 还可通过抑制 NF-κB 的激活,减少 MMP-9 基因的表达,从而抑制乳腺癌细胞的迁移和侵袭。因此,Glaucine 在哮喘和乳腺癌的研究中具有应用潜力。
    Glaucine
  • HY-N0592A
    Demethyleneberberine chloride Inhibitor 98.90%
    Demethyleneberberine chloride 是一种天然线粒体靶向抗氧化剂。Demethyleneberberine chloride 通过抑制 NF-κB 通路和调节 Th 细胞的平衡来减轻小鼠结肠炎并抑制炎症反应。Demethyleneberberine chloride 可作为 AMPK 激活剂,用于非酒精性脂肪性肝病 (NAFLD) 的研究。
    Demethyleneberberine chloride
  • HY-N2908
    Atraric acid Inhibitor 99.94%
    Atraric acid (Methyl atrarate) 是一种特异的雄激素受体 (androgen receptor) 拮抗剂,具有抗炎和抗癌作用。Atraric acid 抑制 LNCaP 和 C4-2 细胞中内源性前列腺特异性抗原基因的表达。Atraric acid 还能抑制 NO 和细胞因子的合成,抑制 MAPK-NFκB 信号通路。Atraric acid 可用于前列腺疾病和炎症性疾病的研究。
    Atraric acid
  • HY-N0253
    Hederacoside C

    常春藤苷C

    Inhibitor 99.85%
    Hederacoside C (Kalopanaxsaponin B) 是一种可从常春藤叶子中主得到的成分。Hederacoside C 通过抑制 MAPK/NF-κB 及其下游信号通路的激活介导炎症反应。Hederacoside C 具有抗炎和抗菌 (antibacterial) 活性。
    Hederacoside C
  • HY-13010
    Laquinimod

    拉喹莫德

    Inhibitor 99.46%
    Laquinimod (ABR-215062) 是一种可口服的羧酰胺衍生物,是一种有效的免疫调节剂,可防止中枢神经系统的神经变性和炎症。Laquinimod 减少星形胶质细胞 NF-κB 的活化以防止铜酮 (Cuprizone) 诱导的脱髓鞘。Laquinimod 具有用于多发性硬化症 (MS;RRMS 或 CPMS) 的复发缓解 (RR) 和慢性进行性 (CP) 形式以及神经退行性疾病研究的潜力。
    Laquinimod
  • HY-B0900
    Anethole

    茴香脑

    Inhibitor 99.81%
    Anethole 是一类具有口服活性的芳香族化合物,用作调味剂,广泛存在于自然界中。Anethole 具有抗癌、抗炎、抗氧化、抗菌、抗真菌、麻醉、雌激素、中枢神经系统抑制、催眠、杀虫剂、和胃保护作用。Anethole 可以用于氧化应激相关皮肤病、前列腺癌的研究 。
    Anethole
  • HY-10072
    SPC 839 Inhibitor 99.86%
    SPC 839 (compound 10) 是一种具有口服活性的 AP-1NF-kB 介导的转录激活抑制剂,其 IC50 值为 0.008 μM。
    SPC 839
  • HY-N0267
    Hypaconitine

    次乌头碱

    Inhibitor 99.49%
    Hypaconitine 抑制 KCNH2 电流,IC50 为 8.1 nM,并表现出心脏毒性。Hypaconitine 通过抑制 NF-κB 核转位来抑制 TGF-β1 诱导的 A549 细胞上皮间质转化(EMT)。Hypaconitine 可以用作神经肌肉阻滞剂。Hypaconitine 具有口服活性。
    Hypaconitine
  • HY-122778
    δ-Tocotrienol Inhibitor 98.10%
    δ-Tocotrienol 是蔬菜,水果,种子,坚果,谷物和油中的一种维生素 E。维生素 E 是一种抗氧化剂、神经保护剂和抗癌剂,可以降低胆固醇和其他脂质,保护心血管疾病。
    δ-Tocotrienol
目录号 产品名 / 同用名 应用 反应物种

NF-κB transcription factors are critical regulators of immunity, stress responses, apoptosis and differentiation. In mammals, there are five members of the transcription factor NF-κB family: RELA (p65), RELB and c-REL, and the precursor proteins NF-κB1 (p105) and NF-κB2 (p100), which are processed into p50 and p52, respectively. NF-κB transcription factors bind as dimers to κB sites in promoters and enhancers of a variety of genes and induce or repress transcription. NF-κB activation occurs via two major signaling pathways: the canonical and the non-canonical NF-κB signaling pathways[1]

 

The canonical NF-κB pathway is triggered by signals from a large variety of immune receptors, such as TNFR, TLR, and IL-1R, which activate TAK1. TAK1 then activates IκB kinase (IKK) complex, composed of catalytic (IKKα and IKKβ) and regulatory (NEMO) subunits, via phosphorylation of IKKβ. Upon stimulation, the IKK complex, largely through IKKβ, phosphorylates members of the inhibitor of κB (IκB) family, such as IκBα and the IκB-like molecule p105, which sequester NF-κB members in the cytoplasm. IκBα associates with dimers of p50 and members of the REL family (RELA or c-REL), whereas p105 associates with p50 or REL (RELA or c-REL). Upon phosphorylation by IKK, IκBα and p105 are degradated in the proteasome, resulting in the nuclear translocation of canonical NF-κB family members, which bind to specific DNA elements, in the form of various dimeric complexes, including RELA-p50, c-REL-p50, and p50-p50. Atypical, IKK-independent pathways of NF-κB induction also provide mechanisms to integrate parallel signaling pathways to increase NF-κB activity, such as hypoxia, UV and genotoxic stress.

 

The non-canonical NF-κB pathway is induced by certain TNF superfamily members, such as CD40L, BAFF and lymphotoxin-β (LT-β), which stimulates the recruitment of TRAF2, TRAF3, cIAP1/2 to the receptor complex. Activated cIAP mediates K48 ubiquitylation and proteasomal degradation of TRAF3, resulting in stabilization and accumulation of the NFκB-inducing kinase (NIK). NIK phosphorylates and activates IKKα, which in turn phosphorylates p100, triggering p100 processing, and leading to the generation of p52 and the nuclear translocation of p52 and RELB[2][3].

 

Reference:

[1]. Oeckinghaus A, et al. The NF-kappaB family of transcription factors and its regulation.Cold Spring Harb Perspect Biol. 2009 Oct;1(4):a000034. 
[2]. Taniguchi K, et al. NF-κB, inflammation, immunity and cancer: coming of age. Nat Rev Immunol. 2018 May;18(5):309-324.
[3]. Perkins ND,et al. Integrating cell-signalling pathways with NF-kappaB and IKK function. Nat Rev Mol Cell Biol. 2007 Jan;8(1):49-62.

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