1. NF-κB
  2. NF-κB

NF-κB

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.

View NF-κB Pathway Map

NF-κB Isoform Specific Products:

  • NF-κB

  • NF-κB1/p50

  • RelA/p65

  • RelB

NF-κB 相关产品 (69):

Cat. No. Product Name Effect Purity
  • HY-13453
    BAY 11-7082 Inhibitor 99.42%
    BAY 11-7082 是一种 NF-κB 抑制剂。BAY 11-7082 通过抑制 TNF-α 诱导的 IκB-α 磷酸化导致 NF-κB 降低。 抑制泛素特异性蛋白酶 USP7USP21IC50 分别为 0.19 μM 和 0.96 μM。
  • HY-18738
    Pyrrolidinedithiocarbamate ammonium Inhibitor 99.61%
    Pyrrolidinedithiocarbamate ammonium是选择性的NF-κB抑制剂。
  • HY-P0151
    SN50 Inhibitor
    SN50是可渗透细胞的 NF-κB 易位抑制剂。
  • HY-10257
    BAY 11-7085 Inhibitor 98.84%
    BAY 11-7085是NF-κB激活和IκBα磷酸化的抑制剂,稳定IκBα的IC50值为10 μM。
  • HY-13982
    JSH-23 Inhibitor 99.10%
    JSH-23 是一种 NF-κB 抑制剂,作用于 LPS 刺激的巨噬细胞 RAW 264.7,IC50 值为 7.1 μM。JSH-23 抑制 LPS 诱导的 NF-κB p65 核易位而不影响 IκB 降解。
  • HY-N2065
    Withaferin A Inhibitor 99.68%
    Withaferin A 是从南非醉茄中分离到的甾体内酯,可以抑制 NF-kB 的活性,靶作用于波形蛋白 (vimentin),具有抗炎,抗肿瘤等功效。
  • HY-N0773
    Isovitexin Inhibitor 98.94%
    Isovitexin 是从亚洲水稻种得到的黄酮类物质,具有抗氧化、抗炎的活性;Isovitexin 作用与 JNK1/2 的抑制剂类似,能够抑制 NF-κB 的活化。
  • HY-N0436
    Engeletin Inhibitor 98.88%
    Engeletin 是从 hymenaea martiana 中得到的黄酮苷类物质,能够抑制 NF-κB 信号通路的激活,具有抗炎、镇痛、利尿、消肿、抗菌等作用。
  • HY-14645
    (-)-DHMEQ Inhibitor 98.05%
    (–)-DHMEQ 是一种有效的 NF-κB inhibitor.
  • HY-N0176
    Dihydroartemisinin Inhibitor >99.0%
    Dihydroartemisinin 通过阻断 RelA/p65 易位至细胞核来抑制 NF-κB 活性。Dihydroartemisinin 还激活肿瘤细胞中的自噬诱导。
  • HY-N0822
    Shikonin Inhibitor 99.64%
    Shikonin 是 TMEM16A 氯化物通道的抑制剂,其 IC50 值为 6.5 μM。Shikonin 也是一种特异性的 PKM2 抑制剂,而且可以抑制肿瘤坏死因子-α (TNF-α),阻止核因子-κB (NF-κB) 通路的激活。
  • HY-N2149
    Tomatidine Inhibitor >98.0%
    Tomatidine 通过阻断 NF-κBJNK 信号发挥抗炎作用。
  • HY-13812
    QNZ Inhibitor 98.46%
    QNZ 强抑制 NF-κB 转录激活和 TNF-α 产生,IC50 分别为 11 和 7 nM。QNZ 是一种保护神经的钙池操纵的钙通道 (SOC) 抑制剂。
  • HY-N0197
    Baicalin Inhibitor 98.01%
    Baicalin 是一种从 Scutellaria baicalensis 中分离出来的类黄酮糖苷。Baicalin 降低 NF-κB 表达。
  • HY-14655
    Sulfasalazine Inhibitor 99.42%
    Sulfasalazine是治疗类风湿关节炎和溃疡性结肠炎的药物。报道显示Sulfasalazine可抑制 NF-κB 的活性。
  • HY-N0141
    Parthenolide Inhibitor 99.13%
    Parthenolide 是一种 NF-κB 抑制剂,可降低组蛋白脱乙酰酶 1 (HDAC-1) 和 DNA 甲基转移酶 1。
  • HY-13010
    Laquinimod Inhibitor 99.84%
    Laquinimod 是一种有效的免疫调节剂。
  • HY-N0603
    Ginsenoside Rg3 Inhibitor >98.0%
    Ginsenoside Rg3 是红参的主要成分。Ginsenoside Rg3 抑制 Na+hKv1.4 通道,IC50 分别为 32.2±4.5 和 32.6±2.2 μM。Ginsenoside Rg3 还抑制 NF-κB 活性和 COX-2 表达。
  • HY-N0191
    Andrographolide Inhibitor
    Andrographolide 是一种 NF-κB 抑制剂,通过共价修饰内皮细胞中 p50 的半胱氨酸残基而抑制 NF-κB 活化,而不影响 IκBα 降解或 p50/p65 核易位。
  • HY-N0441
    Neferine Inhibitor 99.92%
    Neferine 是一种双苄基异喹啉类生物碱。Neferine 强效抑制 NF-κB 激活。
nf-kappa-b-map.png

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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