NF-κB

Nuclear factor-κB; Nuclear factor-kappaB

NF-κB

NF-κB Isoform Specific Products:

NF-κB Isoform Comparison

NF-κB Related Products (1743)
Antibodies (32)
NF-κB Signaling Pathway
NF-κB Isoform Comparison

By Effects:	Inhibitors (1428) Agonists (6) Degraders (3) Controls (7) Ligands (2) Antagonist (1) Activators (131) Modulators (33) Inducers (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-183934

Anti-inflammatory agent 99	Inhibitor
Anti-inflammatory agent 99 is a chalcone derivative. Anti-inflammatory agent 99 inhibits LPS (HY-D1056)-induced NF-κB nuclear translocation and suppress the phosphorylation of JNK, ERK, and p38. Anti-inflammatory agent 99 inhibits the expression of cytoinflammatory factors such as *TNF-α* and IL-6 induced by LPS. Anti-inflammatory agent 99 can be used for the research of LPS-induced septic shock.

HY-111165

SNX-7081	Inhibitor
SNX-7081 is an Hsp90 inhibitor with K_i and IC₅₀ values of 26 nM and 44 nM, respectively. SNX-7081 blocks the nuclear translocation of NF-κB, inhibits the production of pro-inflammatory cytokines, attenuates the ERK/JNK and PDGF signaling pathways, and suppresses LPS (HY-D1056)-induced nitric oxide production. SNX-7081 inhibits DNA repair, induces G₂/M cell cycle arrest, and triggers apoptosis via downregulation of MYC/nucleolin and activation of Fas. SNX-7081 can be used in research related to rheumatoid arthritis and cancer.

HY-142119

Penehyclidine	Activator
Penehyclidine, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation.

HY-P11489

RN-0001	Inhibitor
RN-0001 is a cyclophilin (Cyp) inhibitor with K_i values of 4.1 nM and 12.0 nM against CypA and CypD, respectively, and an EC₅₀ of 916 nM for CypD. RN-0001 binds directly to CypD, inhibits the peptidyl-prolyl cis-trans isomerase activities of CypD and CypA, and prevents CypD-dependent mitochondrial permeability transition pore opening. RN-0001 improves mitochondrial function, reduces ROS production, inhibits the expression of lipogenic markers, blocks the nuclear translocation of NF-κB p65, and decreases the release of activated caspase-3 and cytochrome c. RN-0001 can be used in the research of alcohol-associated liver disease.

HY-100507A

Avadomide hydrochloride	Inhibitor
Avadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active cereblon modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities.

HY-B1272AS1

Desipramine-d₃
Desipramine-d₃ is the deuterium labeled Desipramine (HY-B1272A). Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases.

HY-N0176S

Dihydroartemisinin-d₃	Inhibitor
Dihydroartemisinin-d₃ is the deuterium labeled Dihydroartemisinin. Dihydroartemisinin is a potent anti-malaria agent.

HY-170692

Hypoglycemic agent 3	Inhibitor
Hypoglycemic agent 3 (Compound H26), a derivative of corosolic acid, exhibits lipid-lowering and significant hypoglycemic effects and can be used as a hypoglycemic agent. Hypoglycemic agent 3 inhibits insulin resistance by targeting MCCC1 and can be used in the study of type 2 diabetes.

HY-170579

Antioxidant agent-20	Inhibitor
Antioxidant agent-20 (Compound 3d) has potent anti-inflammatory and antioxidant activity. Antioxidant agent-20 reduces reactive oxygen species (ROS) and apoptosis in a dose-dependent manner. Antioxidant agent-20 exhibits photoprotective effect against UVB-irradiated human skin keratinocytes (HaCaT) (IC₅₀=5.13 µM) via activation of Nrf2/HO-1 signaling and inhibition of NF-κB pathway.

HY-N2381R

Menthone (Standard)
Menthone (Standard) is the analytical standard of Menthone. This product is intended for research and analytical applications. Menthone, an orally active monoterpene that can be isolated from plants and Mentha oil with antibacterial, antitumor, antioxidation, and antivirus properties. Menthone is a main volatile component of the essential oil, and has anti-Inflammatory properties in Schistosoma mansoni infection and rheumatoid arthritis.

HY-W012732R

Isoquinoline (Standard)	Inhibitor
Isoquinoline (Standard) is the analytical standard of Isoquinoline. This product is intended for research and analytical applications. Isoquinoline is an analog of pyridine. Isoquinoline structural-based alkaloids, such as tropoloisoquinoline, phthalideisoquinoline, and naphthylisoquinoline has anti-cancer activities.

HY-14654B

Aspirin DL-lysine	Inhibitor
Aspirin DL-lysine (ASA DL-lysine) is a lysine-containing aspirin derivative. Aspirin DL-lysine inhibits cyclooxygenase (COX) in platelets, blocks the synthesis of thromboxane A2 (TXA2), and thus inhibits platelet aggregation and activation. Aspirin DL-lysine can be used to study thrombin generation in patients with unstable angina pectoris.

HY-B0130AR

Perindopril erbumine (Standard)
Perindopril (erbumine) (Standard) is the analytical standard of Perindopril (erbumine). This product is intended for research and analytical applications. Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NF-κB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure.

HY-162092

Multi-target Pt	Inhibitor
Multi-target Pt (IV), an antitumor agent, suppresses the IKKβ phosphorylation, IκBα phosphorylation and NF-κB p65 phosphorylation and nuclear translocation, leading to blocked the NF-kB signal pathway.

HY-121012

(rac)-AG-205
(rac)-AG-205 is a potent inhibitor of progesterone receptor membrane component 1 (Pgrmc1) that induces genes involved in sterol synthesis, including the INSIG1 protein, which forms a complex with PGRMC1. (rac)-AG-205 prevents neuronal resistance to hypoxic ischaemia by blocking NF-kB signalling and activation of the BDNF/PI3K/AKT pathway.

HY-16362

Omtriptolide sodium	Inhibitor
Omtriptolide sodium (PG490-88Na) is a derivative of Triptolide (HY-32735). Omtriptolide sodium exhibits significant immunosuppressive, anti-fibrotic and anti-inflammatory properties. The mechanism of action of Omtriptolide sodium is diverse, including inhibiting T cell activation and proliferation, inducing T cell apoptosis (apoptosis), blocking fibroblast maturation/proliferation, inhibiting TGF-β mRNA expression, and suppressing pro-inflammatory cytokines (such as IL-2, IFN-γ, TNF-α) by blocking transcription factors such as NF-κB. Omtriptolide sodium can be used for research on obstructive airway diseases, pulmonary fibrosis and graft-versus-host disease.

HY-178132

Apoptosis inducer 46	Inhibitor
Apoptosis inducer 46 is an apoptosis inducer. Apoptosis inducer 46 exhibits potent and selective growth inhibitory effects on metastatic triple-negative breast cancer (TNBC) cells. Apoptosis inducer 46 induces G2/M phase cell cycle arrest and apoptotic cell death in MDA-MB-231 cells, and blocks NF-κB nuclear translocation. Apoptosis inducer 46 can be used for the study of TNBC.

HY-P2496

Endothelin 1 (swine, human), Alexa Fluor 488-labeled	Activator
Endothelin 1 (swine, human), Alexa Fluor 488-labeled is an Endothelin-1 conjugated with Alexa Fluor 488 (HY-D1304). Endothelin-1 is an endogenous vasoconstrictor and agonist of ETA/ETB receptor. Endothelin 1 (swine, human) exerts effects including promoting mitosis, angiogenesis, tumor invasion and metastasis, and inhibiting apoptosis. Endothelin 1 (swine, human) induces inflammation and oxidative stress by activating the NF-κB pathway. Endothelin 1 (swine, human), Alexa Fluor 488-labeled is specifically designed for fluorescence imaging, flow cytometry or receptor localization studies, and can be used in research related to sepsis, atherosclerosis, systemic inflammatory response syndrome, cancer and congestive heart failure.

HY-B1014S1

Acenocoumarol-d₄	Inhibitor
Acenocoumarol-d₄ is deuterium labeled Acenocoumarol (HY-B1014). Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist. Acenocoumarol inhibits MAPK/ERK/JNK signaling pathway, reduces the nuclear translocation of NF-κB p65, activates Akt/GSK3β signaling pathway. Acenocoumarol induces apoptosis in cell A549, arrests cell cycle at S phase.

HY-N1333

Rubioncolin C	Inhibitor
Rubioncolin C exerts anti-tumor activity by inducing apoptotic and autophagic Cell Death and inhibiting the NF-κB and Akt/mTOR/P70S6K Pathway in Human Cancer Cells.

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 (1743)

Antibodies (32)

NF-κB Signaling Pathway

NF-κB Isoform Comparison

NF-κB Related Products (1743):