2. Signaling Pathways
  3. Immunology/Inflammation
    Vitamin D Related/Nuclear Receptor
  4. Glucocorticoid Receptor

Glucocorticoid Receptor

Glucocorticoid Receptor

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Glucocorticoid Receptor (GR, or GCR) also known as NR3C1 (nuclear receptor subfamily 3, group C, member 1) is the receptor to which cortisol and other glucocorticoids bind. The GR is expressed in almost every cell in the body and regulates genes controlling the development, metabolism, and immune response. When the glucocorticoid receptor binds to glucocorticoids, its primary mechanism of action is the regulation of gene transcription. The unbound receptor resides in the cytosol of the cell. After the receptor is bound to glucocorticoid, the receptor-glucorticoid complex can take either of two paths. The activated GR complex up-regulates the expression of anti-inflammatory proteins in the nucleus or represses the expression of pro-inflammatory proteins in the cytosol by preventing the translocation of other transcription factors from the cytosol into the nucleus. Dexamethasone is an agonist, and RU486 and cyproterone acetate are antagonists of the GR. Also, progesterone and DHEA have antagonist effects on the GR.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-19653A
    Butixocort propionate
    		Agonist
    Butixocort propionate (JO 1222), a corticosteroid, is a potent Glucocorticoid Receptor agonist. Butixocort propionate exhibits anti-inflammatory activity. Butixocort propionate can be used for the researches of inflammation, immunology and metabolic disease, such as asthma and arthritis.
    Butixocort propionate
  • HY-114154
    AL-438
    		Modulator
    AL-438 is a potent, selective and orally active glucocorticoid receptor modulator with Kis of 2.5, 1786, 53, 1440, >1000 nM for glucocorticoid receptor, progesterone receptor, mineralocorticoid receptor, androgen receptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity.
    AL-438
  • HY-12946A
    BI 653048 phosphate
    		Inhibitor
    BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
    BI 653048 phosphate
  • HY-W657887
    GSK-3β/G9a-IN-1
    		Inhibitor
    GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective, blood-brain-barrier permeable, competitive G9a (substrate-competitive, IC50: 1.1 μM) and GSK-3β (ATP competitive, IC50: 0.8 μM) inhibitor. GSK-3β/G9a-IN-1 is a potent H3K9me2 inhibitor that reshapes chromatin landscape. GSK-3β/G9a-IN-1 lowers tau phosphorylation, reduces Aβ aggregation. GSK-3β/G9a-IN-1 displays inhibition toward glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor. GSK-3β/G9a-IN-1 also upregulates SAGA complex members such as Eny2 and Sgf29. GSK-3β/G9a-IN-1 markedly improves memory, restores social behaviors, and increases synaptic complexity in late-onset Alzheimer’s disease.
    GSK-3β/G9a-IN-1
  • HY-121062
    Betamethasone acibutate
    		Modulator
    Betamethasone acibutate, derives from Betamethasone, is an acetate ester. Betamethasone acibutate is a glucocorticoid.
    Betamethasone acibutate
  • HY-W777281
    Fluocinolone acetonide-13C3
    Fluocinolone acetonide-13C3 is the 13C-labeled Fluocinolone (Acetonide) (HY-B0415). Fluocinolone is a glucocorticoid glucocorticoid receptor agonist. Fluocinolone is effective in preventing both lipid accumulation and inflammation. Fluocinolone can promote the proliferation of DPCs and has the potential role in repairing injured pulp tissues. Fluocinolone can be used to study the prevention of chemotherapy-induced peripheral neuropathy caused by Paclitaxel (HY-B0015).
    Fluocinolone acetonide-<sup>13</sup>C<sub>3</sub>
  • HY-W744577
    Dexamethasone acetate-d5
    Dexamethasone acetate-d5 (Dexamethasone 21-acetate-d5; Hexadecadrol acetate-d5) is the deuterium labeled Dexamethasone acetate (HY-14648A). Dexamethasone acetate (Dexamethasone 21-acetate) is the acetate form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone acetate has a longer duration of action than Dexamethasone. Dexamethasone acetate can accumulate at inflammatory sites, in mouse liver and mouse lung via nanostructured lipid carriers. Dexamethasone acetate can be used to prepare topical formulations for studies related to sensorineural hearing loss, γ-carrageenan-induced paw edema, chronic active hepatitis, pulmonary diseases, and inflammation after vitreoretinal surgery.
    Dexamethasone acetate-d<sub>5</sub>
  • HY-142942
    Glucocorticoid receptor-IN-2
    		Inhibitor
    Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV.
    Glucocorticoid receptor-IN-2
  • HY-B0260S2
    Methylprednisolone-d4
    		Agonist
    Methylprednisolone-d4 is deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.
    Methylprednisolone-d<sub>4</sub>
  • HY-13570S1
    Betamethasone-d5-1
    		Agonist
    Betamethasone-d5-1 is deuterium labeled Betamethasone. Betamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone accelerates fetal lung maturation and induces gene expression and apoptosis.
    Betamethasone-d<sub>5</sub>-1
  • HY-17463S1
    Prednisolone-d6
    Prednisolone-d6 is the deuterium labeled Prednisolone (HY-17463). Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research.
    Prednisolone-d<sub>6</sub>
  • HY-165370
    BMS-791826
    		Modulator
    BMS-791826 is a selective glucocorticoid receptor modulator. BMS-791826 effectively binds to glucocorticoid receptors and effectively inhibits AP-1 and NF-κB-dependent reporter. BMS-791826 can be used in the research of inflammatory diseases.
    BMS-791826
  • HY-13609S3
    Deflazacort-d3-1
    Deflazacort-d3-1 is the deuterium labeled Deflazacort (HY-13609). Deflazacort, a glucocorticoid, is an inactive proagent and is converted rapidly to the active metabolite 21-desacetyldeflazacort. Deflazacort is used as an anti-inflammatory and immunosuppressant.
    Deflazacort-d<sub>3</sub>-1
  • HY-17461S
    Cortisone-13C3
    		Agonist
    Cortisone-13C3 is the 13C-labeled Cortisone. Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.
    Cortisone-<sup>13</sup>C<sub>3</sub>
  • HY-B0636S1
    Triamcinolone acetonide-13C3
    Triamcinolone acetonide-13C3 is the 13C-labeled Triamcinolone acetonide (HY-B0636). Triamcinolone acetonide inhibits basic fibroblast growth factor (bFGF) induced proliferation of retinal endothelial cells. Triamcinolone acetonide reduces chondrocyte viability and leads to cartilage destruction. Triamcinolone acetonide activates macrophage with anti-inflammatory characteristics. Triamcinolone acetonide can be used in the study of diseases such as atopic dermatitis.
    Triamcinolone acetonide-<sup>13</sup>C<sub>3</sub>
  • HY-17461S3
    Cortisone-d2
    		Agonist
    Cortisone-d2 is the deuterium labeled Cortisone. Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations.
    Cortisone-d<sub>2</sub>
  • HY-17463S3
    Prednisolone-d4-1
    		Agonist
    Prednisolone-d4-1 is the deuterium labeled Prednisolone (HY-17463). Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research.
    Prednisolone-d<sub>4</sub>-1
  • HY-B1121A
    Flunisolide hemihydrate
    		Activator
    Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation.
    Flunisolide hemihydrate
  • HY-W653985
    Cortodoxone-d7
    Cortodoxone-d7 (11-Deoxycortisol-d7) is a deuterium labeled Cortodoxone (HY-77839). Cortodoxone (11-Deoxycortisol; cortexolone) is a glucocorticoid steroid hormone and also is a glucocorticoid antagonist. Cortodoxone increases tryptophan oxygenase (TO) activity and induces the secretion of corticosterone. Cortodoxone regulates T cell proliferation and activation.
    Cortodoxone-d<sub>7</sub>
  • HY-B0629S
    Mometasone-d5
    Mometasone-d5 is the deuterium labeled Mometasone.
    Mometasone-d<sub>5</sub>
Cat. No. Product Name / Synonyms Application Reactivity