GLCCI1 Inhibitors
Chemical inhibitors of the GLCCI1 protein operate through various mechanisms to impede the protein's function. Dexamethasone, a synthetic steroid, binds to glucocorticoid receptors, which can lead to a repression of transcription of certain genes, ultimately reducing GLCCI1 protein levels and activity. Similarly, RU486 (Mifepristone) and Cyproterone acetate serve as glucocorticoid receptor antagonists, directly competing with glucocorticoids for receptor binding sites, which prevents the receptor-mediated actions that are necessary for the transcription and synthesis of the GLCCI1 protein. Spironolactone, though primarily an anti-mineralocorticoid, can also exert a weak antagonistic effect on glucocorticoid receptors, potentially reducing the expression of GLCCI1 by limiting glucocorticoid receptor-mediated expression.
Additional inhibitors like Ketoconazole and Metyrapone disrupt glucocorticoid synthesis by inhibiting specific cytochrome P450 enzymes and 11β-hydroxylase, respectively. This results in lower levels of glucocorticoids, which in turn leads to reduced activation of glucocorticoid receptors and subsequent expression of the GLCCI1 protein. Trilostane and Aminoglutethimide inhibit enzymes crucial to the early stages of steroidogenesis, namely 3β-hydroxysteroid dehydrogenase and P450scc. This inhibition decreases the overall synthesis of glucocorticoids, thus diminishing the activation of glucocorticoid receptors required for the upregulation of GLCCI1. Mitotane directly affects the adrenal cortex, lowering glucocorticoid production and consequently the activation of glucocorticoid receptors that regulate GLCCI1. Similarly, Etomidate suppresses cortisol synthesis by selectively inhibiting 11β-hydroxylase, leading to a decrease in receptor-mediated GLCCI1 expression. Lastly, Hydrocortisone in high concentrations can saturate glucocorticoid receptors and initiate a negative feedback mechanism that reduces the expression of GLCCI1, thus functionally inhibiting the protein.
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Items 1 to 10 of 11 total
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Dexamethasone | 50-02-2 | sc-29059 sc-29059B sc-29059A | 100 mg 1 g 5 g | $76.00 $82.00 $367.00 | 36 | |
Dexamethasone binds to the glucocorticoid receptor, which then translocates to the nucleus and binds to glucocorticoid response elements in the promoter region of target genes. GLCCI1 is a glucocorticoid-induced transcript, and its protein product may be functionally inhibited as the glucocorticoid receptor complex can repress the transcription of certain genes, leading to reduced GLCCI1 protein levels and activity. | ||||||
Mifepristone | 84371-65-3 | sc-203134 | 100 mg | $60.00 | 17 | |
RU486 is a glucocorticoid receptor antagonist that competes with glucocorticoids for their receptor binding sites. By blocking glucocorticoid receptors, RU486 prevents the receptor-mediated actions that would normally lead to the transcription and synthesis of GLCCI1, thus functionally inhibiting GLCCI1 protein. | ||||||
Cyproterone Acetate | 427-51-0 | sc-204703 sc-204703A | 100 mg 250 mg | $60.00 $199.00 | 5 | |
Cyproterone acetate acts as a glucocorticoid receptor antagonist. It competes with glucocorticoids for binding to the receptor, thus impeding the receptor's ability to induce GLCCI1 expression and consequently inhibiting the function of the GLCCI1 protein. | ||||||
Spironolactone | 52-01-7 | sc-204294 | 50 mg | $107.00 | 3 | |
Spironolactone, through its anti-mineralocorticoid properties, exerts a weak antagonistic effect on glucocorticoid receptors. By competing for these receptor sites, it may indirectly inhibit the function of GLCCI1 by preventing glucocorticoid receptor-mediated expression of the protein. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $62.00 $260.00 | 21 | |
Ketoconazole inhibits cytochrome P450 enzymes, which are involved in the synthesis of glucocorticoids. By lowering glucocorticoid levels, ketoconazole indirectly inhibits the activation of glucocorticoid receptors, thus reducing the expression and function of GLCCI1 protein. | ||||||
Metyrapone | 54-36-4 | sc-200597 sc-200597A sc-200597B | 200 mg 500 mg 1 g | $25.00 $56.00 $86.00 | 4 | |
Metyrapone inhibits 11β-hydroxylase, an enzyme crucial in the final step of glucocorticoid synthesis. Reduced synthesis of glucocorticoids leads to decreased activation of glucocorticoid receptors, which in turn functionally inhibits GLCCI1 by reducing its expression mediated by glucocorticoid receptors. | ||||||
Trilostane | 13647-35-3 | sc-208469 sc-208469A | 10 mg 100 mg | $224.00 $1193.00 | 2 | |
Trilostane inhibits 3β-hydroxysteroid dehydrogenase, which is involved in the biosynthesis of glucocorticoids. The consequent reduction in glucocorticoid synthesis leads to decreased glucocorticoid receptor activation, which indirectly inhibits the function of GLCCI1. | ||||||
Aminoglutethimide | 125-84-8 | sc-207280 sc-207280A sc-207280B sc-207280C | 1 g 5 g 25 g 100 g | $41.00 $143.00 $530.00 $2020.00 | 2 | |
Aminoglutethimide inhibits the enzyme P450scc, which converts cholesterol to pregnenolone in the initial step of steroidogenesis, thereby reducing glucocorticoid levels. This diminishes the activation of glucocorticoid receptors and indirectly inhibits the function of GLCCI1. | ||||||
Mitotane | 53-19-0 | sc-205754 sc-205754A | 100 mg 1 g | $71.00 $163.00 | 1 | |
Mitotane directly affects the adrenal cortex and reduces the synthesis of glucocorticoids. By lowering glucocorticoid levels, it indirectly inhibits the function of GLCCI1 by reducing the activation of glucocorticoid receptors that would otherwise upregulate GLCCI1 expression. | ||||||
Etomidate | 33125-97-2 | sc-203577 | 10 mg | $124.00 | ||
Etomidate selectively inhibits 11β-hydroxylase, an enzyme involved in cortisol synthesis. By inhibiting cortisol synthesis, etomidate indirectly inhibits the function of GLCCI1 by decreasing the activation of glucocorticoid receptors that regulate GLCCI1 expression. | ||||||