Glucocorticoid Receptor Inhibitor

Hydrocortisone hemisuccinate sodium is an orally active physiological glucocorticoid. Hydrocortisone hemisuccinate sodium inhibits proinflammatory cytokine activity, with IC₅₀s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate sodium can be used for the research of ulcerative colitis (UC).

Triamcinolone is a long-acting corticosteroid with anti-inflammatory, anti-oedematous, anti-proliferative, anti-angiogenetic, immunomodulatory and neuroprotective effects through binding to glucocorticoid receptors. Triamcinolone can relieve several dermatitis, immune diseases and ocular diseases.

Desonide is a non-fluorinated corticosteroid anti-inflammatory agent that acts on the glucocorticoid receptor. Desonide can also specifically bind to the mutant huntingtin protein (mHTT), reducing the level and toxicity of mHTT. Desonide can be used in the research of Huntington's disease and inflammatory diseases such as atopic dermatitis.

3,6-Dibromocarbazole is a glucocorticoid receptor (GR) inhibitor and Environmental pollutant. 3,6-Dibromocarbazole induces abnormal development of zebrafish embryos and disrupts the neurohormonal function of the hypothalamic-pituitary-adrenal axis in zebrafish larvae. 3,6-Dibromocarbazole increases the α-diversity of soil bacteria, alters community structure, enhances interspecific competition, regulates metabolic functions, and changes the abundance of genes related to nitrogen fixation, nitrification and carbon cycling. 3,6-Dibromocarbazole exerts endocrine-disrupting potential by interfering with the gluconeogenesis pathway.

GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC₅₀ values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo.

INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC₅₀ values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research.

BI 653048, a chemical probe, is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC₅₀ value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC₅₀>30 μM). BI 653048 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.

Triamcinolone (Standard) is the analytical standard of Triamcinolone. This product is intended for research and analytical applications.

(S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.

Glucocorticoid receptor-IN-1 (Compound WX002) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-1 exhibits very good transcriptional repressive activity with an IC₅₀ of 2.11 nM against hMMP1, and transcriptional activation activity with an EC₅₀ of 5.59 nM against MMTV.

JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC₅₀ of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC₅₀=0.50 nM) and the rat androgen receptor (AR) (IC₅₀=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC₅₀ >3000 nM).

Glucocorticoid receptor/IL-6-IN-2 (Compound 36) is a selective dual inhibitor targeting the glucocorticoid receptor (GR) and IL-6 signaling pathway (IC₅₀ values of 40 nM and 19 nM, respectively). Glucocorticoid receptor/IL-6-IN-2 is promising for research of inflammatory diseases like rheumatoid arthritis and asthma.

Glucocorticoid receptor/IL-6-IN-1 (Compound 35) is a selective dual inhibitor targeting the glucocorticoid receptor (GR) and IL-6 signaling pathway (IC₅₀ values of 120 nM and 59 nM, respectively). Glucocorticoid receptor/IL-6-IN-1 inhibits IL-6-induced JAK/STAT3 phosphorylation, blocking inflammatory cytokine transcription. Glucocorticoid receptor/IL-6-IN-1 is promising for research of inflammatory diseases like rheumatoid arthritis and asthma.

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.

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.

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.

KR-67607 is a selective 11β-HSD1 inhibitor, with an IC₅₀ value of 4.8 nM against h11β-HSD1 and 7.1 nM against mouse 11β-HSD1. KR-67607 inhibits stress-induced Glucocorticoid receptor nuclear translocation, reduces cortisol levels, suppresses the expression of ROS and proinflammatory cytokines, and enhances Nrf-2-mediated antioxidant gene transcription. KR-67607 maintains trabecular meshwork structure and reverses elevated intraocular pressure. KR-67607 improves ocular antioxidant activity and mucus secretion, reverses ocular surface damage, and prevents ischemia-reperfusion induced ocular injury. KR-67607 can be used in research related to glaucoma and dry eye disease.

Toripristone (RU-40555) is a cortisol receptor inhibitor. Toripristone combined with clarithromycin can increase the antibacterial activity of Mycobacterium avium complex infection.

Desonide (Standard) is the analytical standard of Desonide. This product is intended for research and analytical applications. Desonide is a non-fluorinated corticosteroid anti-inflammatory agent that acts on the glucocorticoid receptor. Desonide can also specifically bind to the mutant huntingtin protein (mHTT), reducing the level and toxicity of mHTT. Desonide can be used in the research of Huntington's disease and inflammatory diseases such as atopic dermatitis.

Collismycin B is a potent dexamethasone-glucocorticoid receptor inhibitor with an IC₅₀ value of 10 µM. Collismycin B shows antimicrobial activity. Collismycin B shows cytotoxicity.