Verproside, a catalpol derivative iridoid glycoside isolated from the genus Pseudolysimachion, represses TNF-α -induced MUC5AC expression by inhibiting NF-κB activation via the IKK/IκB signaling cascade. Verproside has potent anti-inflammatory, antioxidant, antinociceptive and anti-asthmatic activities. Verproside has the potential for the study of chronic obstructive pulmonary disease (COPD).

MJ210 is a modulator of the NF-κB and MAPK pathways with oral activity and the ability to penetrate the blood-brain barrier, and it exhibits neuroprotective activity. In vitro, 5 μM of MJ210 can increase the survival rate of SH-SY5Y cells treated with Rotenone to 81.9% and reduce the level of ROS, etc. In vivo, 5 mg/kg of MJ210 can improve the motor impairment in a rat model of Parkinson's disease. MJ210 can be used in the research of neurological diseases, such as Parkinson's disease.

MAY0132 is a potent and selective EPAC2 inhibitor with an IC50 of 0.4 μM. MAY0132 significantly inhibits replication of HMPV, AdV and RSV, reduces viral infection-induced cytokine/chemokine production, and inhibits NF-κB activation. MAY0132 has antiviral activity and can be used in the study of respiratory virus infection.

DBMB is an inhibitor of spleen tyrosine kinase (Syk), capable of significantly inhibiting the activity of Syk kinase. DBMB exhibits anti-inflammatory activity by suppressing the signaling of NF-κB, which in turn reduces the production of inflammatory mediators such as nitric oxide (NO) and prostaglandin E2 (PGE2). DBMB can be utilized in research on inflammatory diseases.

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.

Bengamide B is an inhibitor for NF-κB with an IC50 of 85 nM. Bengamide B inhibits LPS-induced expression of TNF-α, IL-6 and MCP-1, exhibits anti-inflammatory activity. Bengamide B exhibits antitumor efficacy (IC50 for HCT-116 is 2 nM).

Amorfrutin A is the inhibition of NF-κB activation, that inhibits TNF-α-induced IκBα degradation, p65 nuclear translocation, and DNA-binding activity. Amorfrutin A promotes TNF-α-induced apoptosis in HeLa cell through promotion of caspase-3 and PARP proteolysis.

​​B022​​ represents a breakthrough in targeted kinase modulation as a highly potent and selective NF-κB-inducing kinase (NIK) antagonist.

DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.

IT 901 is a c-Rel inhibitor (IC50 = 3 μM). Inhibits IL-2 expression in activated T-cells in vitro.

Lipoic acid is a selective, small molecule large-conductance Ca(2+)-activated K(+) channel (BKCa, KCa1.1, MaxiK) positive modulator with EC50 of 11 uM. Lipoic acid shows a favorable selectivity profile on Nav, Cav, SK, and IK channels. Lipoic acid causes distinct activation from a concentration of 0.3 and 10 µM Lipoic acid left-shifted the voltage activation curve by 60 mV. Lipoic acid reduces spontaneous phasic contractions in guinea pig urinary bladder strips at 1 uM, while having only a modest effect on contractions evoked by electrical field stimulation (EFS) and no effect on high K+-induced contractions.

Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.

Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.

A small molecule that inhibits NFATc1 and NF-κB activity, inhibits RANKL-induced osteoclastogenesis in vivo.

NF-κΒ activator 1 is a potent NF-κΒ activator with an EC50 of 0.9 μM. NF-κΒ activator 1 induces superoxide dismutase (SOD) 2 mRNA expression.

SC75741 is a potent NF-κB inhibitor with EC50 of 200 nM.

JSH-23 is an inhibitor of NF-κB transcriptional activity with IC50 of 7.1 μM.

BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with an IC50 value of 10 μM.

BAY 11-7082 is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM. Also inhibiting components of the ubiquitin system.

Dehydromiltirone (1,2-Didehydromiltirone) is a diterpenoid quinone with an anti-inflammatory effect. Dehydromiltirone prevents liver injury by modifying the MAPK and NF-κB signaling pathways, reducing neuroinflammatory responses, and inhibiting platelet aggregation. Dehydromiltirone can be used for osteoporosis research.

Laurotetanine ((+)-Laurotetanine) is an potent and orally active isoquinoline alkaloid and could be extracted from the roots of Litsea cubeba (Lour.) Pers. Laurotetanine exerts an anti-asthmatic effect by inhibition of IgE, histamine, and inflammatory reactions via down-regulating MUC5AC and NF-κB signaling pathways.

HSR1304 (Compound 5d) is a potent inhibitor of NFκB. The multifunctional transcription factor, nuclear factor-κB (NF-κB), is broadly involved in multiple human diseases, such as cancer and chronic inflammation. HSR1304 has the potential for the research of cancer diseases.

R-HP210 acts on the NF-κB mediated tethered transrepression function (IC50=3.80 μM). R-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. R-HP210 does not induce the transactivation functions of Glucocorticoids (GCs).

AS2690168 is a novel orally available, selective RANKL signal transduction inhibitor, reduces TRAP staining of sRANKL-stimulated RAW264 cells with IC50 of 0.28 uM, suppresses RANKL-induced osteoclastogenesis.AS2690168 suppressed soluble RANKL (sRANKL)-induced NFATc1 mRNA expression in RAW264 cells with 37.1% and 98.9% inhibiyion at 0.3 and 3.0 uM, respectively.AS2690168 also suppressed calcium release from parathyroid hormone-stimulated mouse calvaria with an IC50 value of 0.46 uM.AS2690168 (3 mg/kg, p.o.) completely suppressed the decrease in femoral bone mineral content in an sRANKL-induced osteopenic mice model, also significantly suppressed the decrease in femoral bone mineral density and increase in serum tartrate-resistant acid phosphatase-5b levels in ovariectomized rats at doses of 0.3, 1 and 3 mg/kg.AS260168 suppressed the increase in urine deoxypyridinoline in a rat prednisolone-induced osteoporosis model at 10 mg/kg.

AS2690168 is a novel orally available, selective RANKL signal transduction inhibitor, reduces TRAP staining of sRANKL-stimulated RAW264 cells with IC50 of 0.28 uM, suppresses RANKL-induced osteoclastogenesis.AS2690168 suppressed soluble RANKL (sRANKL)-induced NFATc1 mRNA expression in RAW264 cells with 37.1% and 98.9% inhibiyion at 0.3 and 3.0 uM, respectively.AS2690168 also suppressed calcium release from parathyroid hormone-stimulated mouse calvaria with an IC50 value of 0.46 uM.AS2690168 (3 mg/kg, p.o.) completely suppressed the decrease in femoral bone mineral content in an sRANKL-induced osteopenic mice model, also significantly suppressed the decrease in femoral bone mineral density and increase in serum tartrate-resistant acid phosphatase-5b levels in ovariectomized rats at doses of 0.3, 1 and 3 mg/kg.AS260168 suppressed the increase in urine deoxypyridinoline in a rat prednisolone-induced osteoporosis model at 10 mg/kg.

IMD-biphenylB is a potent imidazoquinolinone-NF-κB immunomodulator dimer that inhibits tumor proliferation while induces low systemic inflammation and reduces adjuvant toxicity.

Iguratimod is one of a series of 4H-1-benzopyran-4-ones which has potent anti-inflammatory, analgesic and antipyretic activity.

Ro 106-9920 is a potent inhibitor of NF-kappaB. Ro 106-9920 has the potential for the research of tumor and cancer diseases.

Didox is a simple, synthetic antioxidant that has been found to reduce the levels of oxidative injury markers.

TCEP (Tris(2-carboxyethyl)phosphine) hydrochloride, a non-thiol reducing agent, promotes NF-κB-DNA binding in a dose-related manner.