NF-κB Pathway

(R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen and inhibits NF-κB activation. (R)-(-)-Ibuprofen has anti-inflammatory and antinociceptive effects.

Obtusifolin has antioxidant properties and improves chemically induced diabetes and its complications by modulation of oxidative stress. Obtusifolin suppresses phthalate esters-mediated bone resorption, thus may be a novel anti-breast-cancer bone metastasis agent. Obtusifolin has beneficial effects on the development of diabetic retinopathy via inhibition of accumulation of oxidatively modified DNA and nitrotyrosine in the retina, can help prevent vision loss in diabetic patients. Obtusifolin and gluco-Obtusifolin produce significant antinociceptive action in rodent behavioral models of inflammatory/neuropathic pain, and that this activity is associated with modulation of neuroinflammation in spinal cord. Gluco-Obtusifolin and its aglycone may be useful for the treatment of cognitive impairment, and that its beneficial effects are mediated, in part, by the enhancement of cholinergic signaling.

1-Caffeoylquinic acid is an important intermediate in lignin biosynthesis. 1-Caffeoylquinic acid has anti-influenza, and antioxidant activities, it also slows the release of glucose into the bloodstream after a meal.

4-Hydroxychalcone attenuates hyperaldosteronism, inflammation, and renal injury in cryptochrome-null mice.

Analgesic activity.

Bay 65-1942 hydrochloride is an inhibitor of ATP-competitive and selective IKKβ.

BI605906 is an inhibitor of IKKβ. When assayed at 0.1 mM ATP, the IC50 value is 380 nM.

BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor. With IC50s of 9 nM and 72 nM, respectively.

Chrysotoxine inhibits 6-hydroxydopamine induced apoptosis in SH-SY5Y cells via NF-κB modulation and mitochondria protection.

CID-2858522 is an effective and specific antigen receptor-mediated NF-κB activation inhibitor (IC50: 70 nM).

CLEFMA has anti-proliferative activity. CLEFMA inhibits tumor growth associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects.

Deoxyelephantopin has anti-inflammatory, hepatoprotective, and wound healing activities; it also has antitumor activity.Deoxyelephantopin inhibits NF-κB, MAPK, PI3K/Akt, and β-catenin signaling

DHMEQ racemate is an NF-κB inhibitor. The activity of DHMEQ racemate is lower than (-)-DHMEQ.

DMAPT is a water-soluble analogue of Parthenolide (PTL). It is an orally active NF-κB inhibitor with an LD50 of 1.7 μM on primary acute myeloid leukemia cells.

Dri-c21045 showed concentration-dependent inhibition of NF-kB activation and all CD40L induced by B cell proliferation with IC50 of 17.1 μM and 4.5 μM, respectively. Dri-c21045 is an effective selective inhibitor of CD40-CD40L synergistic stimulator protein-protein interaction (PPI) with IC50 of 0.17 μM.

Edasalonexent is an orally bioavailable inhibitor of NF-κB.

GSK319347A is a TBK1 and IKKε dual inhibitor (IC50s: 93 nM and 469 nM, respectively). GSK319347A inhibits IKK2 (IC50: 790 nM).

Hesperidin methylchalcone is the Citrus original products with powerful antioxidant activity. It can suppresse experimental gout arthritis in mice by inhibiting NF-κB activation.

Icariside F2 shows modest α-glucosidase inhibitory (4.60±1.74% to 11.97±3.30%) and antioxidant activities. It also displays potent NF-κB inhibitory effects, with the IC50 value of 16.25 ± 2.19 uM.

IMD-0560 is a novel inhibitor of IκB kinase β.