AP-1 Inhibitor

Lucidenic acid B is a triterpenoid compound. Lucidenic acid B inhibits the activities of ERK1/2, AP-1, NF-kB, and IKK, suppresses PMA (Phorbol 12-myristate 13-acetate) (HY-18739)-induced MMP-9 expression and cell invasion, and induces apoptosis in leukemia cells via the mitochondrial pathway. Lucidenic acid B inhibits the growth of various cancer cell lines without affecting normal lymphocytes and does not induce G1 phase arrest or necrosis. Lucidenic acid B can be used in research on hepatocellular carcinoma, human acute promyelocytic leukemia, and skin tumor promotion.

(R)-CSN5i-3 is the (R)-enantiomer of CSN5i-3. CSN5i-3 is a potent, selective and orally available inhibitor of CSN5.

Chloranthalactone B, a lindenane-type sesquiterpenoid, is a nature product that could be isolated from Chinese medicinal herb Sarcandra glabra. Chloranthalactone B inhibits the production of inflammatory mediators by inhibiting the AP-1 and p38 MAPK pathways.

Berberine (sulfate) (Standard) is the analytical standard of Berberine (sulfate). This product is intended for research and analytical applications. Berberine sulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine sulfate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine sulfate has antineoplastic properties. The sulfate form improves bioavailability[1][2].

Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC₅₀ value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice.

c-Fos-IN-1 (Compound P16) is a c-Jun inhibitor, and decreases mRNA levels and protein levels of c-Fos. c-Fos-IN-1 also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. c-Fos-IN-1 shows anticancer activity by inhibiting ERK/c-Fos/Jun pathway. c-Fos-IN-1 inhibits the proliferation and migration of gastric cancer cells (IC₅₀: 2.31 μM for MGC-803 cell). c-Fos-IN-1 arrests cell cycle at G2/M phase and induces cancer cell apoptosis. c-Fos-IN-1 inhibits gastric cancer tumor growth.

DL-Syringaresinol ((±)-Syringaresinol), a lignin, inhibits UVA-induced upregulation of MMP-1 by suppressing MAPK/AP-1 signaling in human HaCaT keratinocytes and dermal fibroblasts (HDFs). DL-Syringaresinol has antiphotoaging properties against UVA-induced skin aging. DL-Syringaresinol exhibits weak antimycobacterial activity against Mycobacterium tuberculosis H37Rv.

Atranorin (Standard) is the analytical standard of Atranorin (HY-N2907). This product is intended for research and analytical applications. Atranorin is a secondary metabolite of lichens and AKT inhibitor. Atranorin possesses multiple activities such as antibacterial, anti-inflammatory, antioxidant, anti-glycation, analgesic, and anti-tumor effects. Atranorin has IC₅₀ values for scavenging DPPH and ABTS free radicals of 117 μM and less than 10 μM, respectively. Additionally, Atranorin also exhibits effects in promoting wound healing. Atranorin can be used in the research of various diseases, including myelodysplastic syndromes, tumors, and inflammatory conditions.

Amorphigenin is a trothotenone compound. Amorphigenin inhibits osteoclast differentiation by suppressing the expression of c-Fos and NFATc1 in activated T cells. Amorphigenin degrades melanosome proteins by activating the AMPK-dependent autophagy pathway, but not in dependence of the mTOR pathway. Amorphigenin significantly protects bone mass and reduces bone erosion in a mouse model of inflammatory bone loss. Amorphigenin can be used to study inflammatory bone diseases, postmenopausal osteoporosis, and skin pigmentation disorders.

MJ-33 is a competitive phospholipase A₂ (PLA₂) inhibitor with an IC₅₀ of 0.3 μM. MJ-33 inhibits the activation of NOX2 by blocking the PLA₂ activity of Prdx6, thereby reducing the production of ROS. MJ-33 effectively inhibits the activity of acidic PLA₂ (pH 4.0), reduces the degradation of pulmonary surfactant phosphatidylcholine (PC), but has no effect on alkaline PLA₂ (pH 8.5). MJ-33 significantly alleviates lung oxidative damage induced by ischemia-reperfusion (I/R). MJ-33 significantly inhibits the invasive, migratory and adhesive abilities of prostate cancer cells by suppressing the MAPK, AKT, NF-κB and AP-1 signaling pathways. MJ-33 can be used to study ROS-related diseases and prostate cancer.

JPC0661 is a direct and allosteric ΔFOSB inhibitor. JPC0661 inhibits the binding of ΔFOSB/JUND and ΔFOsB to DNA with IC₅₀ values in the micromolar range (9-52 uM), directly inhibits ΔFOSB-mediated transcription with IC₅₀ of 0.82 μM in vitro. JPC0661 significantly reduces ΔFOSB occupancy at genomic AP1 sites in vivo. JPC0661 binds to a novel groove outside the DNA-binding cleft of ΔFOSB and disrupt the formation of the ΔFOSB/JUND-DNA complex. JPC0661 can be used for Alzheimer's disease research.

YL0441 is an inhibitor of ΔFOSB/JUND heterodimers and ΔFOSB homomultimers, with IC₅₀ values of 13.7 μM and 12.3 μM, respectively. YL0441 blocks the binding of ΔFOSB to DNA. YL0441 reduces ΔFOSB bound to genomic DNA in the hippocampal tissues of APP mice. YL0441 is applicable to the research of Alzheimer's disease.

Antcin K is a selective inhibitor targeting the PI3K/Akt, NF-κB, MEK1/2-ERK, p38 and AP-1 pathways. Antcin K upregulates IL-10 expression, thereby inhibiting the production of pro-inflammatory factors, blocking monocyte adhesion, reducing tissue damage, and promoting myogenesis. Antcin K has significant anti-inflammatory, anti-damage and tissue protective activities. Antcin K is mainly used in the research of inflammation-related diseases such as periodontitis, rheumatoid arthritis, and skeletal muscle injury.

CD666 is a selective retinoic acid receptor-γ (RAR-γ) agonist with a K_d of 68 nM. CD666 inhibits proliferation of cancer cells and shows synergistical effects and anti-AP-1 activity with IFN-γ. CD666 can be used for the research of breast cancer.

1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid (Standard) is the analytical standard of 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid (HY-N4226). This product is intended for research and analytical applications. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is an AP-1 inhibitor which can be found in Cordyceps bassiana. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid downregulates the expression of COX-2. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid can be used for the study of atopic dermatitis.

Dihydro-N-caffeoyltyramine is a new phenolic amide that can be isolated from the root bark of wolfberry and has strong antioxidant activity and antifungal effects. Dihydro-N-caffeoyltyramine downregulates the expression of cyclooxygenase-2 by inhibiting the activity of C/EBP and AP-1 transcription factors.

δ-Tocotrienol (Standard) is the analytical standard of δ-Tocotrienol. This product is intended for research and analytical applications. δ-Tocotrienol is a Vitamin E in vegetables, fruits, seeds, nuts, grains and oils. Vitamin E has become well known for its role as an antioxidant, in lowering cholesterol and other lipids, as a neuroprotective and anticancer agent, and in cardiovascular disease protection.

Norkurarinol is a prenylated flavonoid. Norkurarinol can be isolated from Sophora flavescens. Norkurarinol potently inhibits mushroom Tyrosinase DOPA oxidase activity with an IC₅₀ of 2.1 μM. Norkurarinol inhibits poly(I:C)-induced NF-κB/AP-1 activation. Norkurarinol inhibits pro-inflammatory cytokines (TNF-α, IL-6). Norkurarinol inhibits phosphorylation of p38, JNK, and ERK1/2. Norkurarinol increases phosphorylation of IRF3. Norkurarinol has antiviral activity against Rotavirus KJ56-1

Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases.

7-O-Galloyl-D-sedoheptulose is an orally effective polyphenolic compound. 7-O-Galloyl-D-sedoheptulose lowers the serum levels of glucose, leptin, insulin, C-peptide, resistin, TNF-α, IL-6, and increases the serum level of adiponectin. 7-O-Galloyl-D-sedoheptulose significantly reduces the levels of ROS and lipid peroxidation products (TBARS) by down-regulating the protein expression of NADPH oxidase subunit Nox-4 and p22phox. 7-O-Galloyl-D-sedoheptulose down-regulates NF-κB and related pro-inflammatory factors (COX-2, iNOS), inhibits the phosphorylation of JNK and the activity of its downstream AP-1. 7-O-Galloyl-D-sedoheptulose reduces the expression of TGF-β1 and fibronectin, indicating its potential in anti-tissue fibrosis. 7-O-Galloyl-D-sedoheptulose can be used for the study of type 2 diabetes and its hepatic and pancreatic complications.