1. Signaling Pathways
  2. Immunology/Inflammation
  3. AP-1

AP-1

Activator Protein 1

Activator Protein 1 (AP-1) is not a single protein, but a collective term referring to dimeric transcription factors composed of Jun (c-Jun, JunB, JunD), Fos (c-Fos, FosB, Fra-1, Fra-2) ATF (activating transcription factor, ATF-2, ATF-3/LRF1, ATF-4, ATF-5, ATF-6B, ATF-7, BATF, BATF-2, BATF-3, JDP2) or MAF (c-MAF, MafA, MafB, MafF, MafG, MafK and Nrl) subunits that bind to a common DNA site, the AP-1-binding site. AP-1 is involved in a plethora of cellular and physiological functions. It is acknowledged as a master integrator of a myriad of extracellular signals allowing cells to adapt to changes in their environment. AP-1 has also been implicated in various severe diseases. These include transplant rejection, fibrosis, organ injury and a variety of inflammatory pathologies such as rheumatoid arthritis, asthma and psoriasis. In addition, cancer is undoubtedly the most documented pathology involving AP-1 where its activity is often dysregulated and contributes to cell transformation, tumor progression, aggressiveness and resistance to treatments.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W031757
    Anthraquinone-2-carboxylic acid
    Inhibitor 98.0%
    Anthraquinone-2-carboxylic acid is an orally active anthraquinone compound and Antibacterial agent. Anthraquinone-2-carboxylic acid can be isolated from Bajitian. Anthraquinone-2-carboxylic acid inhibits the activation of DPP-IV, COX-2, NF-κB and AP-1. Anthraquinone-2-carboxylic acid blocks IAV-induced activation of the RIG-I/STAT1 pathway, alleviates IAV-mediated weight loss, and protects against lethal IAV infection. Anthraquinone-2-carboxylic acid inhibits the growth of various Staphylococcus strains. It possesses potent anti-inflammatory, immunomodulatory, analgesic and antibacterial activities.\n



    Anthraquinone-2-carboxylic acid
  • HY-P10927
    BRP
    Activator
    BRP is a 12-peptide derived from BRINP2 that can cross the blood-brain barrier. BRP induces the central activation of FOS in neuronal cells via the cAMP-PKA-CREB signaling pathway. BRP exerts anorectic and anti-obesity effects without triggering nausea or aversive responses. The action of BRP is independent of the leptin, GLP-1 receptor and melanocortin 4 receptor pathways. BRP is applicable to obesity-related research.
    BRP
  • HY-110398
    5,6,7-Trimethoxyflavone
    Inhibitor 98.76%
    5,6,7-Trimethoxyflavone is a flavonoid compound that can be isolated from plants Callicarpa japonica. 5,6,7-Trimethoxyflavone exhibits antiviral and anti-inflammatory activities through inhibition of NF-κB/AP-1/STAT signaling pathway.
    5,6,7-Trimethoxyflavone
  • HY-165126
    Schizophyllan
    Inhibitor
    Schizophyllan (SPG) is an orally active extracellular β-glucan produced by the fungus Schizophyllum commune. Schizophyllan improves mitochondrial function and protects against metabolic liver injury by activating the SIRT3 pathway. Schizophyllan inhibits osteoclastogenesis and promotes osteoblast differentiation by suppressing the phosphorylation of JNK/p38, as well as downregulating PGC1β/PPARγ, c-Fos and NFATc1. Recognized via Dectin-1, schizophyllan enables precise delivery of oligonucleotide drugs and antigens to antigen-presenting cells, thus holding great potential in the treatment of inflammatory diseases and vaccine development.
    Schizophyllan
  • HY-N6857
    Armepavine
    Inhibitor 99.53%
    Armepavine, found in Nelumbo nucifera, is an orally active NF-κB inhibitor. Armepavine attenuates expression of p-p65, α-SMA, p-JNK1/2, p-ERK1/2, p-p38α stimulated by TNF-α and LPS. Armepavine suppresses NF-κB nuclear translocation, IκBα phosphorylation, and collagen deposition. Armepavine can be used for the research of hepatic fibrosis and leukemia.
    Armepavine
  • HY-N4225
    Aaptamine
    Activator 99.71%
    Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects.
    Aaptamine
  • HY-N0719
    Fargesin
    99.52%
    Fargesin is a bioactive neolignan isolated from magnolia plants, with antihypertensive and anti-inflammatory effects.
    Fargesin
  • HY-13703A
    Nimustine hydrochloride
    Activator 99.00%
    Nimustine hydrochloride (ACNU) is the hydrochloride salt form of Nimustine (HY-13703). Nimustine hydrochloride is an alkylating agent, which induces DNA double-strand breaks (DSBs) and inter-strand crosslinks (ICLs), thereby activating the DNA damage response (DDR) signaling pathway. Nimustine hydrochloride activates p38 MAPK/JNK signaling pathway, and exhibits antitumor activity.
    Nimustine hydrochloride
  • HY-141645
    IMM-H007
    Inhibitor
    IMM-H007 (WS070117) is an orally active and potent AMPK (AMP-activated protein kinase) activator and TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis.
    IMM-H007
  • HY-B0327
    Irsogladine
    Inhibitor 99.88%
    Irsogladine (Dicloguamine) is an orally active gastric mucosal protective agent. Irsogladine inhibits breast cancer recurrence and lung metastasis in nude mice. Irsogladine inhibits the transcriptional activities of NF-κB and AP-1, suppresses the activities of PDE and PDE4 to elevate intracellular cAMP levels, and activates TRPV1 and KATP channels. Irsogladine enhances iNOS expression, NO production, and the activation of cAMP-responsive elements. Irsogladine inhibits the development and progression of intestinal polyps in Apc-mutant mice. Irsogladine alleviates oxidative stress, increases gastric mucosal blood flow, and stimulates the production of endogenous prostaglandins. Irsogladine promotes insulin secretion in MIN6 cells. Irsogladine inhibits tumor angiogenesis, cancer cell proliferation, and the production of proinflammatory cytokines. Irsogladine exerts protective effects on astrocytes in ethanol/hydrochloric acid-induced gastric ulcers in mice. Irsogladine prevents colitis in IL-10 gene-deficient mice by reducing the production of IL-12 and IL-23. Irsogladine upregulates gap junction intercellular communication in pancreatic cancer cells via the PKA pathway. Irsogladine is applicable to research related to breast cancer, intestinal polyposis, gastric ulcer, spontaneous colitis, glioma, liver cancer, and pancreatic cancer[5][6].
    Irsogladine
  • HY-N1513
    Ganoderic acid H
    Inhibitor 99.68%
    Ganoderic acid H is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderic acid H suppresses growth and invasive behavior of breast cancer cells through the inhibition of transcription factors AP-1 and NF-kappaB signaling.
    Ganoderic acid H
  • HY-122808
    (-)-Camphoric acid
    Inducer 99.91%
    (-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid induces glutamate receptor expression. Camphoric acid also significantly induces the activation of NF-κB and AP-1. Camphoric acid significantly stimulates the differentiation of mouse osteoblastic MC3T3-E1 subclone 4 cells. Camphoric acid has weak regulatory function towards glutamate receptors. Camphoric acid can induce mRNA expression of glutamate signaling molecules and activate transcription factors, thereby stimulating osteoblast differentiation.
    (-)-Camphoric acid
  • HY-129056
    Melagatran
    Inhibitor 99.31%
    Melagatran is a reversible, selective, orally active direct inhibitor of thrombin with a Ki of 2 nM. Melagatran binds directly to the active site of thrombin, inhibiting thrombin-mediated conversion of fibrinogen to fibrin. Melagatran reduces the DNA binding activity of NF-κB and AP-1. Melagatran reduces fibrin deposition in organs, alleviates ischemic brain damage, and reduces the size of advanced atherosclerotic lesions. Melagatran can be used in the study of cardiovascular disease (coronary thrombosis, atherosclerosis) and ischemic brain damage.
    Melagatran
  • HY-B1272AS
    Desipramine-d4
    98.93%
    Desipramine-d4 is the deuterium labeled Desipramine (HY-B1272A). 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.
    Desipramine-d<sub>4</sub>
  • HY-P10927A
    BRP TFA
    Activator
    BRP (BRINP2-related peptide) TFA is a 12-peptide derived from BRINP2 that can cross the blood-brain barrier. BRP TFA induces the central activation of FOS in neuronal cells via the cAMP-PKA-CREB signaling pathway. BRP TFA exerts anorectic and anti-obesity effects without triggering nausea or aversive responses. The action of BRP TFA is independent of the leptin, GLP-1 receptor and melanocortin 4 receptor pathways. BRP TFA is applicable to obesity-related research.
    BRP TFA
  • HY-15870A
    (6E)-SR 11302
    99.68%
    (6E)-SR 11302 is a E-isomer of SR 11302. SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE).
    (6E)-SR 11302
  • HY-112134A
    (R)-CSN5i-3
    Inhibitor 99.87%
    (R)-CSN5i-3 is the (R)-enantiomer of CSN5i-3. CSN5i-3 is a potent, selective and orally available inhibitor of CSN5.
    (R)-CSN5i-3
  • HY-N10913
    Chloranthalactone B
    Inhibitor
    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.
    Chloranthalactone B
  • HY-151876
    Glucocorticoid receptor modulator 1
    Inhibitor 99.79%
    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.
    Glucocorticoid receptor modulator 1
  • HY-168895
    c-Fos-IN-1
    Inhibitor
    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.
    c-Fos-IN-1
Cat. No. Product Name / Synonyms Application Reactivity

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