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AP-1 site

" in MedChemExpress (MCE) Product Catalog:

5

Inhibitors & Agonists

2

Natural
Products

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N2593
    Isorhapontigenin
    4 Publications Verification

    		 Carnitine Palmitoyltransferase (CPT) Reactive Oxygen Species (ROS) Autophagy Apoptosis NF-κB PI3K Akt MMP Keap1-Nrf2 Metabolic Disease Inflammation/Immunology Cancer
    Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes .
    Isorhapontigenin
  • HY-129056
    Melagatran

    		Thrombin NF-κB AP-1 Cardiovascular Disease Neurological Disease
    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-119418
    Desketoraloxifene

    		Estrogen Receptor/ERR Cancer
    Desketoraloxifene is an estrogen receptors alpha (ERα) activator at an AP-1 site. Desketoraloxifene can be used for the research of osteoporosis and breast cancer .
    Desketoraloxifene
  • HY-N2593R
    Isorhapontigenin (Standard)

    		Reference Standards Carnitine Palmitoyltransferase (CPT) Reactive Oxygen Species (ROS) Autophagy Apoptosis NF-κB PI3K Akt MMP Keap1-Nrf2 Inflammation/Immunology Cancer
    Isorhapontigenin (Standard) is the analytical standard of Isorhapontigenin (HY-N2593). This product is intended for research and analytical applications. Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes.
    Isorhapontigenin (Standard)
  • HY-W471288
    JPC0661

    		AP-1 Neurological Disease
    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 .
    JPC0661

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