NF-κB

Nuclear factor-κB; Nuclear factor-kappaB

NF-κB

NF-κB Isoform Specific Products:

NF-κB Isoform Comparison

NF-κB Related Products (1749)
Antibodies (32)
NF-κB Signaling Pathway
NF-κB Isoform Comparison

By Effects:	Inhibitors (1435)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-N0460R

1-Caffeoylquinic acid (Standard)	Inhibitor
1-Caffeoylquinic acid (Standard) is the analytical standard of 1-Caffeoylquinic acid. This product is intended for research and analytical applications. 1-Caffeoylquinic acid is an effective NF-κB inhibitor, shows significant binding affinity to the RH domain of p105 with K_i of 0.007 μM. 1-Caffeoylquinic acid has anti-oxidative stress ability. 1-Caffeoylquinic acid is the inhibitor for PD-1/PD-L1.

HY-170585

COX-2-IN-51	Inhibitor
COX-2-IN-51 (E25) is a potent COX-2 inhibitor, with an IC₅₀ of 70.7 nM. COX-2-IN-51 significantly inhibits LPS-induced release of NO and PGE2, expression of COX-2 and iNOS, and activation of NF-κB pathway. COX-2-IN-51 exhibits anti-inflammatory and analgesic effects in diverse murine models through inhibiting NF-κB pathway. COX-2-IN-51 has lower gastrointestinal side effects than Indomethacin (HY-14397).

HY-178983

SHP2-IN-45	Inhibitor
SHP2-IN-45 (Compound 6) is a potent, highly selective, and orally active SHP2 allosteric inhibitor. SHP2-IN-45 significantly reduces the expressions of IL-6, TNF-α, IL-1β, and iNOS. SHP2-IN-45 inhibits the polarization of M1-type macrophages. SHP2-IN-45 can inhibit the NF-κB pathway. SHP2-IN-45 can be used in the research of sepsis and acute lung injury.

HY-182236

JRN73958	Inhibitor
JRN73958 (Reduced scytonemin) is a PI3K/Akt, MAPK, and NF-κB inhibitor found in Nostoc commune. JRN73958 inhibits nitric oxide production, induce reactive oxygen species (ROS) generation, and lead to autophagy. JRN73958 decreases LPS (HY-D1056)/IFNγ-induced PI3K/Akt, MAPK, and NF-κB activity. JRN73958 can be used for the research of leukemia.

HY-N0589S

Dehydrodiisoeugenol-d₄	Inhibitor
Dehydrodiisoeugenol-d₄ is the deuterium labeled Dehydrodiisoeugenol (HY-N0589). Dehydrodiisoeugenol is an orally active anti-inflammatory and anti-tumor agent. Dehydrodiisoeugenol inhibits the proliferation of colorectal cancer cells, and induces apoptosis, autophagy, endoplasmic reticulum stress and cell cycle arrest. Dehydrodiisoeugenol also exerts anti-inflammatory effects by inhibiting the activation of NF-κB and the expression of COX-2. Dehydrodiisoeugenol can be used in the research related to colorectal cancer, inflammatory diseases and ulcerative colitis.

HY-172619

BS-153	Inhibitor
BS-153 is a novel synthetic oxazolidinone agent with anti-inflammatory activities by blocking the activation of the NF-κB/PKCθ pathway. BS-153 inhibits the expression levels of iNOS and COX-2 and pro-inflammatory cytokines (TNF-α, IL-1β, and IL-6) on LPS-stimulated RAW264.7 cells.

HY-N2497R

Isoliquiritin apioside (Standard)	Inhibitor
Isoliquiritin apioside (Standard) is the analytical standard of Isoliquiritin apioside. This product is intended for research and analytical applications. Isoliquiritin apioside significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis of cancer cells and endothelial cells.

HY-184001

LT-1339-553	Inhibitor
LT-1339-553 is a selective, orally active RIPK1 inhibitor with IC₅₀ values of 4.32, 95.74 and 84.33 nM against RIPK1, RIPK2 and RIPK3, respectively. LT-1339-553 exerts anti-necroptotic activity by inhibiting the AKT/PI3K/NF-κB pathway and the IL-17 pathway. LT-1339-553 reduces liver injury, inflammatory responses and collagen deposition. LT-1339-553 can be used in studies related to schistosomiasis-induced liver fibrosis.

HY-147129

cGAS-IN-9	Inhibitor
cGAS-IN-9 is a cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) inhibitor, with IC₅₀ values of 27.5 nM and 5.15 μM against human and murine cGAS, respectively. cGAS-IN-9 shows weak inhibitory activity against human soluble adenylate cyclase, with an IC₅₀ of 26.4 μM. cGAS-IN-9 inhibits dsDNA-induced expression of IFNB1 and CXCL10, as well as activation of the NF-κB pathway, in human immune cells. cGAS-IN-9 can be used in research related to cGAS-dependent inflammatory diseases.

HY-N0212R

Peimine (Standard)	Inhibitor
Peimine (Standard) is the analytical standard of Peimine. This product is intended for research and analytical applications. Peimine (Verticine; Dihydroisoimperialine) is an orally active natural product. Peimine has anti-inflammatory, analgesic and cough relieving effects. Peimine can be used in cancer and inflammation related research.

HY-N0043R

Ginsenoside Rd (Standard)	Inhibitor
Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.

HY-173410

iNOs-IN-6	Inhibitor
iNOs-IN-6 is an anti-inflammatory agent. iNOs-IN-6 inhibits NF-κB, iNOS, and MAPK expression(IC₅₀: 0.2-0.62 μM). iNOs-IN-6 reduces IL-6, TNF-α, and IL-1β pro-inflammatory mediators levels (IC₅₀: 0.4-0.69 μM).

HY-N15196

Andrographolide-lipoic acid	Inhibitor
Andrographolide-lipoic acid is an Andrographolide (HY-N0191) analogue, which is formed by the coupling of Andrographolide and Lipoic acid (HY-18733). Andrographolide-lipoic acid inhibits NF-κB and has anti-diabetic and β-cell protective activities.

HY-175257

Theophylline-platinum(IV) prodrug-1	Inhibitor
Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer.

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-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-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.

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 (1749)

Antibodies (32)

NF-κB Signaling Pathway

NF-κB Isoform Comparison

NF-κB Related Products (1749):