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Nuclear Receptors

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  • 20(S)-Hydroxycholesterol | Smoothened activator
    20-(S)-Hydroxycholesterol (516-72-3) is an endogenous ligand for the LXR receptor.1 It has anti-adipogenic and pro-osteogenic effects in mesenchymal stem cells mediated via a non-LXR dependent pathway.2 The osteogenic...

  • 24(S),25-Epoxycholesterol | 77058-74-3 | Structure | Supplier
    24(S),25-Epoxycholesterol (77058-74-3) is a cholesterol metabolite that acts as an endogenous agonist for nuclear receptor LXR.1 Controls cellular cholesterol homeostasis.2 24(S),25-Epoxycholesterol promotes neural...

  • 24(S)-Hydroxycholesterol | Endogenous cholesterol metabolite
    24S Hydroxycholesterol (474-73-7) is an important cholesterol metabolite (cholesterol 24-hydroxylase) found in the brain.1 It is an endogenous agonist of the nuclear receptor LXR.2 It has been shown to induce cell death in...

  • 27-Hydroxycholesterol | Cholesterol oxidation metabolite
    27-Hydroxycholesterol (20380-11-4) is a metabolite resulting from the action of sterol 27-hydroxylase on cholesterol. Concentrations of 27-hydroxycholesterol are elevated in patients with Alzheimers disease and mild...

  • 5alpha,6alpha-Epoxycholesterol | LXR ligand
    5α,6α-Epoxycholesterol (1250-95-9) is a naturally occurring metabolite of cholesterol.  It is a major oxysterol found in processed food1 and has been implicated in atherosclerosis2,3...

  • 6-Formylindolo[3,2-b]carbazole | 172922-91-7 | Structure | Supplier
    6-Formylindolo(3,2-b)carbazole (172922-91-7) is a very potent (Kd = 0.07 nM) endogenous ligand for the aryl hydrocarbon receptor (AhR).1,2 References/Citations1) Rannung et al. (1987) Certain photooxidized derivatives of...

  • Adapalene | 106685-40-9 | Structure | Supplier
    Adapalene (106685-40-9) is a stable analog of retinoic acid that acts as a selective agonist for RARβ and RARγ. Adapalene also inhibits proliferation and induces apoptosis in colorectal cancer cells in culture...

  • BADGE | PPAR gamma antagonist
    BADGE (1675-54-3) is a PPARγ antagonist with μM affinity in 3T3-L1 and 3T3-F442A preadipocyte cells. Selective over PPARδ and PPARα. Antagonizes the ability of rosiglitazone to stimulate transcriptional...

  • Bexarotene | Retinoid RXR agonist
    Bexarotene (153559-49-0) is a highly potent and selective retinoid X receptor (RXR) agonist (EC50=28, 25, 20 nM for RXRα, β, γ respectively).1 Clinically useful antineoplastic agent for cutaneous T-cell...

  • Ciglitazone | 74772-77-3 | Structure | Supplier
    Ciglitazone (74772-77-3) is a PPARγ agonist (EC50=3 μM). Stimulates adipogenesis in human mesenchymal stem cells. Ciglitazone inhibits HUVEC differentiation and angiogenesis. Cell permeable. References/Citations1)...

  • Cinnabarinic acid | Endogenous AhR ligand
    Cinnabarinic acid (606-59-7) is a novel endogenous tryptophan metabolite which acts as an aryl hydrocarbon receptor (AHR) agonist.1 It drives IL-22 production by stimulating the differentiation of human and mouse T cells...

  • Dexamethasone | 50-02-2 | Structure | Supplier
    Dexamethasone (50-02-2) is a synthetic glucocorticoid used clinically in the treatment of a variety of inflammatory and autoimmune conditions. References/Citations1) Merck Index 14...

  • DiMNF | AhR modulator (SAhRM)
    DiMNF (14756-24-2) is a selective aryl hydrocarbon receptor (AHR) modulator (SAhRM). It exhibits antiinflammatory activity including suppression of cytokine-mediated acute phase genes through dissociation of...

  • DPN |ER beta agonist
    DPN (1428-67-7) is a potent estrogen ERβ receptor agonist. Displays a 70-fold selectivity over ERα, EC50 = 0.85 and 66 nM, respectively.1 Regulates expression of GluR1, 2 and 3 in rat hippocampus.2 Ameliorates...

  • FH-535 | 108409-83-2 | Structure | Supplier
    FH-535 (108409-83-2) suppresses Wnt/β-catenin signaling. It antagonizes PPARγ and PPARδ ligand-dependent activation which is mediated by inhibition of recruitment of the coactivators β-catenin and GRIP1...

  • GE-501516 | PPAR delta agonist
    GW-501516 (317318-70-0) is a potent and selective PPARδ (NR1C2) agonist, EC50=1.2 nM and 1000-fold selective over other PPAR subtypes.1  Induces apolipoprotein A1-mediated cholesterol efflux in vitro.1 Improves...

  • Genistein | Tyrosine kinase inhibitor
    Genistein (446-72-0) is a naturally occurring flavonoid with a wide range of biological actions. Inhibits protein tyrosine kinases including epidermal growth factor receptor kinase.1,2 Phytoestrogen3 and agonist at GPR304...

  • Genistin | Genistein glycoside
    Genistin (529-59-9) is a novel selective inhibitor of terminal deoxyribonucleotidyl-transferase.1 Disrupts cell cycle and induces apoptosis in human ovarian cancer SK-OV-3 cells.2 Inhibits UV light-induced plasmid DNA damage...

  • GSK-3787 | 188591-46-0 | Supplier | Structure
    GSK-3787 (188591-46-0) is a selective and irreversible antagonist of the peroxisome proliferator-activated receptor delta (PPARδ) plC50 = 6.6. It covalently binds to Cys 249 in the PPARδ binding site...

  • GW-9662 | PPAR gamma antagonist
    GW-9662 (22978-25-2) is a selective PPARγ antagonist (IC50 = 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively)1. Blocks the inhibition of osteoclast formation induced by IL-4 (1-2 μM)2...

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