ap-1

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].

AP-1, a miniaturized proteolysis-targeting chimera (PROTAC) incorporating an anaplastic lymphoma kinase (ALK) ligand connected to (±)-thalidomide via an ultrashort linker, effectively degrades ALK fusion proteins such as NPM-ALK in Karpas-299 cells and EML4-ALK and ALKF1174L in SN-N-SH and NCI H3122 cells, respectively. Concentrations ranging from 10 to 300 nM are sufficient for its action, which is hindered by the proteasome inhibitor MG-132. Demonstrating selectivity, AP-1 exhibits cytotoxicity towards ALK-dependent Karpas-299 cells with an IC50 value of 0.1265 nM, while showing significantly less toxicity to non-ALK-dependent THP-1 cells (IC50 = 2,704 nM). Furthermore, it effectively reduces tumor volume in NCI H3122 mouse xenograft models at doses of 25, 50, and 100 mg/kg.

INI-43, an inhibitor of Nuclear Import-43, shows a significant cytotoxic effect on various cervical and oesophageal cancer cell lines by targeting Kpnβ1 and interferes with the nuclear localization of Kpnβ1 and known Kpnβ1 cargoes, NFAT, NFκB, AP-1 and NF

Farudodstat (ASLAN003) is an orally active and potent inhibitor of DHODH (Human Dihydroorotate Dehydrogenase) with antitumor activity, showing potential as a first-in-class candidate in AML [Acute Myeloid Leukemia].

Vaginatin, a compound isolated from Laserpitium zernyi, has anticancer activity, inhibits AP-1 pro-inflammatory factor, and can be used in cancer research.10 FTHF disodium (10) has been shown to be effective in the study of cancer.

SR 11302 is an inhibitor of activator protein-1 (AP-1).

SL327 is a selective inhibitor for MEK1/2 with IC50 of 0.18 μM/0.22 μM; able to transport through the blood-brain barrier.

15(S)-HpETE is a product of arachidonic acid formed in the 15-lipoxygenase pathway and inhibits angiogenesis. 15(S)-HpETE can upregulate the expression of CD31, E-selectin, and gene selectin in cells.

T-5224 is a transcription factor c-Fos/AP-1 inhibitor that specifically inhibits the DNA-binding activity of c-Fos/c-Jun without affecting other transcription factors.

E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

IMM-H007 is a novel lipid-lowering agent, increasing abca1 protein expression

Dehydroglyasperin D exhibits anticancer, anti-inflammatory, anti-obesity, antioxidant and anti-aldose reductase effects, it inhibits the proliferation of HT-29 human colorectal cancer cells through direct interaction with phosphatidylinositol 3-kinase; it also mediates suppression of both COX-2 expression and the MLK3 signalling pathway through direct binding and inhibition of MLK3. Dehydroglyasperin D shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.

Kukoamine A possesses anticancer, cytoprotective, antioxidant, and anti-inflammatory activities, it also has neuroprotective effects through inhibiting oxidative stress and apoptosis after whole-brain irradiation (WBI) in rats.

3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) reduces cell proliferation in Caco-2 cells (IC50 = 24.1 μM) more effectively than anthocyanins and may offer protection against colon cancer after its formation in the gut. It inhibits transcription factors NF-κB, AP-1, STAT-1, and OCT-1, which are known to be activated in colorectal cancer.

3'-Demethylnobiletin has chemopreventive effects on colon carcinogenesis, it can significantly inhibit the growth of human colon cancer cells, cause cell-cycle arrest, induce apoptosis, and profoundly modulate signaling proteins related with cell prolifer

Alpha-Chaconine has anti-inflammatory effect, associated with the suppression of AP-1, and supports its possible therapeutic role for the treatment of sepsis. Alpha-Chaconine also has cytotoxic effects.

Asperulosidic acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities. ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways.

Atranorin shows significant antinociceptive and antiinflammatory activities, it has a relevant redox-active action, acting as a pro-oxidant or antioxidant agent depending on the radical, also, it will exert cytoprotective effects on cells under oxidative

Ganoderic acid C1 has anti-inflammatory activity, has potential for treating TNF-α± mediated inflammation in asthma and other inflammatory diseases. Ganoderic acid C1 has anti-tumor-promoting activity. It is moderately active inhibitors against HIV-1 prot

Ganoderic acid H is a potent antitumour agent, it mediates its biological effects through the inhibition of transcription factors AP-1 and NF-kappaB, resulting in the down-regulation of expression of Cdk4.

Norathyriol is a potent PTP1B inhibitor with good cell permeability and oral availability.

Capillarisin is a novel blocker of STAT3 activation and thus may have a potential in negative regulation of growth, metastasis, and chemoresistance of tumor cells, it inhibits cancer cell growth of osteosarcoma cells by inducing apoptosis accompanied with

Communic acid has antibacterial activity, including against mycobacterial. trans-Communic acid has potential to be utilized as anti-wrinkling agents and cosmetic ingredients, as they suppress UVB-induced MMP-1 expression.

Dehydroglyasperin C is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C possesses potent antioxidant, cancer chemopreventive, and neuroprotective activities, it has protective effects against chronic diseases