nfκb

AP-1/NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB mediated transcriptional activation (IC50 = 1 μM), without blocking basal transcription driven by the β-actin promoter. It has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells [1].

The NF-κB Activation Inhibitor III, controls the biological activity of NF-κB. It is primarily used for Inflammation/Immunology applications.

NF-κB/MAPK-IN-1 is a potent dual inhibitor of the NF-κB and MAPK pathways with potential anti-inflammatory activity, inhibition of NO production, and inhibition of LPS-induced activation of iNOS, COX-2, ERΚ and P38. NF-κB/MAPK-IN-1 is used for the prevention and treatment of rheumatoid arthritis (RA).

NF-κB-IN-8 is a competitive antagonist of LPS for MD-2 binding, and it impedes the expression of inflammatory factors by engaging MD-2. Additionally, it inhibits ALP activity and is usable in inflammation research, including acute lung injury (ALI) [1].

NF-κB-IN-10 (compound E1) is an NF-κB inhibitor that mitigates heart failure symptoms by modulating the Nrf2/NF-κB signaling pathway, alleviating oxidative stress and inflammation. It suppresses LPS-induced NO production and downregulates iNOS and COX-2 expression in RAW264.7 cells, showing potential for cardiovascular disease research [1].

NF-κB-IN-12 (compound 3h) is a potent NF-κB inhibitor with an IC50 of 1.02 μM, suitable for research in acute lung injury [1].

NF-κB-IN-11 (Compound 3i) is an inhibitor of NF-κB, effectively blocking TNF-α-induced NF-κB pathway activation and nuclear translocation of NF-κB, alongside reducing expression levels of phospho-IKK, IκBα, and NF-κB p65. Demonstrating anti-inflammatory properties, it mitigates dextran sulfate sodium-induced colitis in mice and exhibits a maximum tolerated dose (MTD) exceeding 1852 mg/kg in acute toxicity assays when administered orally (p.o.) [1].

NF-κB-IN-13 (compound 12) significantly inhibits LPS-induced NF-κB activation and NO synthesis in RAW264.7 macrophages, demonstrating anti-inflammatory properties [1].

NF-κB-IN-1 (1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)-) is a potent NF-κB signaling pathway inhibitor. It is a 4-arylidene crucumin analogue. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.

Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.

5-Aminosalicylic Acid (5-ASA) is a specific PPARγ agonist and also inhibits P21-activated kinase 1(PAK1) and NF-Κb. 5-Aminosalicylic Acid has anti-cancer and anti-inflammatory activities. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

Nimbolide suppresses CDK4/CDK6 kinase activity. Nimbolide inhibits the NF-κB, Wnt, PI3K-Akt, MAPK, and JAK-STAT signaling pathways. Nimbolide causes apoptosis through the inactivation of NF-κB. Nimbolide is a triterpene derived from the leaves and flowers

JSH-23 is an NF-κB inhibitor that inhibits NF-κB transcriptional activity (IC50=7.1 μM) but does not affect IκBα degradation. JSH-23 is an antioxidant with anti-inflammatory activity.

NF-κΒ activator 1 can activate the nf-kappa Β gene activator, EC50 of 0.9 microns. NF-κΒ is widely used in eukaryotic cells as a gene regulating cell proliferation and cell survival. NF-κΒ activator 1 induces superoxide dismutase (SOD) 2 1 mRNA expression.

CBL0137 hydrochloride (Curaxin-137 hydrochloride) is an inhibitor of the histone chaperone FACT, which also activates p53 and inhibits NF-κB with EC50 values ​​of 0.37 and 0.47 μM, respectively. CBL0137 hydrochloride functionally inactivates the complex that promotes chromatin transcription (FACT), thereby driving effects on p53 and NF-κB and promoting cancer cell death, and when used in combination with cisplatin, CBL0137 hydrochloride has potent anticancer activity against SCLC.

Sakuranetin, a flavanone phytoalexin from ultraviolet-irradiated rice leaves, it has antifungal, antimutagenic, anti-inflammatory and antioxidant effects

Rocaglamide (Roc-A), isolated from the genus Aglaia, can be used to treat coughs, injuries, asthma, and inflammatory skin diseases. It is a potent inhibitor of NF-κB activation in T-cells.

Phorbol 12-myristate 13-acetate (PMA) is a natural phorbol ester that acts as an activator of PKC, SphK, and NF-κB, and is commonly used to induce differentiation of THP-1 cells and establish dermatitis models.

CHPG sodium salt is a selective agonist of mGluR5 that activates ERK and Akt signaling pathways and is utilized in studies on traumatic brain injury.

CHPG hydrochloride is a selective agonist of mGluR5.

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

DMAPT (Dimethylamino Parthenolide) is an orally active NF-κB inhibitor and a Parthenolide (PTL) analogue with an LD50 value of 1.7 μM for primary acute myeloid leukemia cells. It has potential anti-tumor and anti-metastatic effects.

LTβR-IN-1 is a potent and selective lymphin β receptor (LTβR) inhibitor with a selective inhibitory effect on the nuclear translocation of p52 of TNF12A, without affecting the nuclear translocation of p65 mediated by the TNF-α receptor. It inhibits p52 nuclear translocation stimulated by TWEAK or Anti-LTβR with an IC50 of 10 μM and regulates the NF-kB signaling pathway in a ligand-independent manner.

Edasalonexent (CAT-1004) is an orally available NF-κB inhibitor designed to improve Duchenne muscular dystrophy.