NF-κB

Nuclear factor-κB; Nuclear factor-kappaB

NF-κB

NF-κB Isoform Specific Products:

NF-κB Isoform Comparison

NF-κB Related Products (1746)
Antibodies (32)
NF-κB Signaling Pathway
NF-κB Isoform Comparison

By Effects:	Inhibitors (1432) Agonists (6) Degraders (3) Controls (7) Ligands (2) Antagonist (1) Activators (130) Modulators (33) Inducers (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-119831

Rohitukine	Inhibitor
Rohitukine is an orally active CDK9/T1 inhibitor with an IC₅₀of 0.3 μM. Rohitukine blocks ATP binding sites of CDK2/A and CDK9/T1, suppresses PPARγ, AKT, mTOR, C/EBPα, SREBP-2, and NF-κB signaling, and increases hepatic LXRα expression. Rohitukine induces S-phase cell cycle arrest, ROS generation, apoptosis, and exhibits anti-inflammatory activity. Rohitukine can be used for the research of leukemia, pancreatic cancer, prostate cancer, breast cancer, CNS cancer, ovarian cancer, lung cancer, dyslipidemia, inflammatory diseases, inflammatory bowel disease, and arthritis.

HY-163478

TNIK-IN-9	Inhibitor
TNIK-IN-9 (Compound 54) is a selective and potent NIK inhibitor, with an IC₅₀ of 1.27 nM. TNIK-IN-9 can inhibit pro-inflammatory cytokines and nitric oxide production. TNIK-IN-9 exhibits significant anti-inflammatory effects, improved mortality, and hepatoprotective effects in sepsis models.

HY-N17909

Broussin	Control
Broussin ((S)-7-hydroxy-4'-methoxyflavane) is a flavane compound present in the branches and twigs of Broussonetia papyrifera. Broussin shows no significant antioxidant activity.

HY-N9731

6-O-p-Hydroxybenzoylglutinoside	Inhibitor
6-O-p-Hydroxybenzoylglutinoside acts as a selective NF-κB inhibitor that suppresses the transcriptional activity of TNF-α-activated NF-κB (IC₅₀=52.78 μM). 6-O-p-Hydroxybenzoylglutinoside shows no significant inhibitory activity against sEH, AChE, or BChE. 6-O-p-Hydroxybenzoylglutinoside is a caged chlorinated iridoid glycoside identified from the seeds of Catalpa bungei (Manchurian catalpa).

HY-181762

Multitarget AD-IN-6	Inhibitor
Multitarget AD-IN-6 (Compound 39) is a multi-target inhibitor, with an IC₅₀ of 15.54 μM against PDE4B, 15.15 μM against PDE7A, 8.39 μM against PDE3A, and a K_d of 37.7 μM against CHIT1. Multitarget AD-IN-6 acts as a TRPA1 antagonist, reduces the level of the NLRP3 inflammasome multiprotein complex to inhibit its activation, while inhibiting PDE4B, PDE7A and CHIT1, and decreasing the phosphorylation of NF-κB. Multitarget AD-IN-6 improves the pathology of elastase-induced emphysema in mice. Multitarget AD-IN-6 is applicable for the research of chronic obstructive pulmonary disease.

HY-P1181

Pam2CSK4	Activator
Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis.

HY-N9765

threo-Guaiacylglycerol β-coniferyl ether	Control
threo-Guaiacylglycerol β-coniferyl ether (compound 9) is a potentially active compound, but its inhibitory activity against NF-κB, nitric oxide production, aromatase, quinone reductase 2, and cyclooxygenase (COX-1/-2) is not significant. threo-Guaiacylglycerol β-coniferyl ether can be naturally extracted from the 95% ethanol extract of the whole plant of Lepisorus contortus (Christ) Ching (a plant of the Polypodiaceae family).

HY-175445

GNE-5472	Activator
GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer.

HY-B0289S

Erdosteine-¹³C₄	Inhibitor
Erdosteine-¹³C₄ is a ¹³C-labeled Erdosteine. Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects.

HY-179488

(±)8(9)-EET	Inhibitor
(±)8(9)-EET is one of the main metabolites produced by the metabolism of arachidonic acid (HY-109590) through the cytochrome P450 epoxide pathway. (±)8(9)-EET is an effective substrate for COX-1 and COX-2. (±)8(9)-EET activates PPARα in HEK293 cells and inhibits the activity of NF-κB induced by IL-1β in a PPARα-dependent and -independent manner. The (8S,9R)-isomer of (±)8(9)-EET ([(8S,9R)-EET]) causes vasoconstriction, thereby reducing renal plasma flow and glomerular filtration rate.

HY-N0017R

Bergenin (Standard)
Bergenin (Standard) is the analytical standard of Bergenin. This product is intended for research and analytical applications. Bergenin is a cytoprotective and antioxidative polyphenol found in many medicinal plants. Bergenin has a wide spectrum activities such as hepatoprotective, antiinflammatory, immunomodulatory, antitumor, antiviral, and antifungal properties.

HY-149351

NF-κB-IN-10	Inhibitor
NF-κB-IN-10 (compound E1) is an NF-κB inhibitor that can improve heart failure by reducing oxidative stress and inflammation by regulating Nrf2/NF-κB signaling pathway. NF-κB-IN-10 inhibits LPS-induced NO production and expression of iNOS and COX-2 in RAW264.7 cells. NF-κB-IN-10 can be used in the research of cardiovascular diseases.

HY-114214

CKD-712	Inhibitor
CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway. CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway. CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells. CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer.

HY-15027S2

5-Aminosalicylic acid-¹³C₆
5-Aminosalicylic acid-¹³C₆ is the ¹³C labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.

HY-N1380S

Guaiacol-d₇
Guaiacol-d₇ is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.

HY-168207

TH023	Inhibitor
TH023 is an inhibitor for the TLR4 signaling pathway, that targets especially the formation of TLR4 homodimer. TH023 inhibits secreted embryonic alkaline phosphatase in cell HEK-Blue hTLR4 with an IC₅₀ of 0.354 μM, and inhibits the NO expression in RAW264.7 with an IC₅₀ of 1.61μM. TH023 also inhibits the activation of NF-κB, reduces the nuclear translocation of NF-κB p65. TH023 exhibits anti-inflammatory efficacy in LPS (HY-D1056)-induced mouse acute sepsis model, and ameliorates the mouse lung injury.

HY-144224S

Tianeptine-d₆ (hydrochloride)	Inhibitor
Tianeptine-d₆ hydrochloride is the deuterium labeled Tianeptine hydrochloride. Tianeptine hydrochloride is an atypical antidepressant. Tianeptine hydrochloride is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine hydrochloride is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine hydrochloride increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine hydrochloride exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine hydrochloride inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine hydrochloride can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.

HY-P10972

GIP (22-51) human	Activator
GIP (22-51) human (Glucose-dependent Insulinotropic Peptide (22-51) human) is a potent proatherosclerotic peptide hormone consisting of 30 amino acids. GIP (22-51) human can activate the NF-κB signaling pathway, promote the expression of MMP-8, and induce the expression of proinflammatory and proatherosclerotic proteins. GIP (22-51) human can also increase the level of intracellular free Ca²⁺ in THP-1-induced macrophages. GIP (22-51) human can be used in the research of atherosclerosis.

HY-N6908R

Continentalic acid (Standard)	Inhibitor
Continentalic acid (Standard) is the analytical standard of Continentalic acid (HY-N6908). This product is intended for research and analytical applications. Continentalic acid is a diterpenoid organic acid. Continentalic acid exhibits multiple activities including anti-inflammatory, antioxidant, neuroprotective, antibacterial and antitumor effects. Continentalic acid alleviates oxidative stress, reduces pro-inflammatory cytokine production, inhibits MAPK phosphorylation and neutrophil infiltration, and induces growth inhibition and apoptosis of cancer cells. Continentalic acid can be used in research related to traumatic brain injury, cancer, inflammation and infections.

HY-146421

Anti-inflammatory agent 21	Inhibitor
Anti-inflammatory agent 21 (compound 9o) is an orally active and low cytotoxic anti-inflammatory agent, with an IC₅₀ value of 0.76 μM for NO. Anti-inflammatory agent 21 acts via accumulation ROS and blocks the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 21 can ameliorate cartilage destruction and inflammatory cell infiltration in arthritis rats model.

LAT TCR CD3 BCR PLCγ1 ZAP70 PKC ELKs NEMO ATM NEMO PIASy PIDD RIP1 PARP1 NEMO ATM cIAP1 NEMO ATM c-IAP1/2, c-FLIP, XIAP, Bcl-XL, Bcl-2, gadd45β,
TRAF1/2, A1/Bfl-1, p100, IL-1, IL-6, IL8, IL-1β, TNF-α, A20,
IκBα, COX2, MIP-1β, MIP-2, VCAM-1,GM-CSF, CCL2, etc. IκBα TRAF6 ATM Tyr kinase LYN SYK BLK BLNK PLCγ2 BTK CARMA1 MALT1 BCL-10 IκBα CK2 p50 RELA IL-1 IL-1R MyD88 IRAK1 IRAK4 TRAF6 TNF TNFR1 TRADD RIPK1 TRAF2/5 cIAP1/2 TAB2 or
TAB3 TAK1 NEMO IKKα IKKβ p105 p50 p105 REL p50 p50 p50 REL p50 RELA p50 c-REL p50 p50 IκBα REL p50 REL p50 CREB TRIM25 RNF135 IPS1 TRAF3 TRAF2/6 Virus MKK3 or
MKK6 MKK4 or
MKK7 p38 JNK CREB AP1 AP1 LPS LBP CD14 TLR4 MD2 MD2 MD2 TLR4 MyD88 TIRAP TRAM TRIF IRAK1 IRAK4 TRAF6 RIP1 TRAF3 CD40L, RANKL CD40,
RANK LTα1β2, LIGHT,
BAFF LTβR,
BAFFR TRAF6 IKKε TBK1 IRF7 IRF3 IRF3 IRF7 BLC, ELC, SLC, SDF-1α, BAFF,
ICAM, CXCL12, CXCL13, CCL19, CCL21, etc. TRAF3 TRAF2 cIAP1/2 NIK TBK1 IKKα p100 RELB p52 RELB p52 RELB

Download NF-κB Signaling Pathway Map.

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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NF-κB

NF-κB

NF-κB Isoform Specific Products:

NF-κB Isoform Specific Products:

NF-κB Related Products (1746)

Antibodies (32)

NF-κB Signaling Pathway

NF-κB Isoform Comparison

NF-κB Related Products (1746):