17β-HSD Inhibitors
17β-Hydroxysteroid dehydrogenases (17β-HSDs) are enzymes that play a crucial role in the regulation of steroid metabolism, particularly in the interconversion of active and inactive forms of sex steroids such as estrogens and androgens. Inhibitors of 17β-HSDs target these enzymes, modulating the balance between various steroid hormones at the molecular level. These enzymes are classified into different isoforms, each of which catalyzes specific reactions involving hydroxylation and dehydrogenation at the 17β position of steroid molecules. By influencing the conversion processes, 17β-HSD inhibitors can modulate the intracellular concentrations of active steroid hormones, thus altering cellular responses that depend on hormone signaling. For example, 17β-HSD inhibitors might act on the conversion of estrone (E1) to the more biologically active estradiol (E2) or similarly alter the balance between testosterone and its less active derivative, androstenedione.
The inhibition of 17β-HSDs involves a range of chemical compounds, many of which display selectivity for specific isoforms of the enzyme. These inhibitors may interact directly with the enzyme's active site, often by mimicking the natural substrates of the enzyme, such as steroid molecules. In some cases, inhibitors form covalent or non-covalent bonds with key residues in the enzyme, preventing the proper binding or conversion of the endogenous substrate. The molecular design of 17β-HSD inhibitors is generally guided by a detailed understanding of enzyme structure, including the active site topology and substrate recognition patterns. This allows for the rational design of molecules with high specificity and potency in targeting particular 17β-HSD isoforms, which are implicated in the regulation of diverse biological processes.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Trilostane | 13647-35-3 | sc-208469 sc-208469A | 10 mg 100 mg | $228.00 $1217.00 | 2 | |
Trilostane is a competitive inhibitor of 3β-hydroxysteroid dehydrogenase, which is upstream of HSD17B1 in the steroidogenesis pathway. By inhibiting this enzyme, trilostane reduces the overall pool of steroids available for subsequent conversion by HSD17B1, thus indirectly diminishing the enzyme's activity by limiting its substrate availability. | ||||||
Epostane | 80471-63-2 | sc-207627 | 1 mg | $379.00 | 1 | |
Epostane directly inhibits HSD17B1 by binding to the enzyme's active site, preventing it from catalyzing the conversion of estrone to estradiol. This inhibition is a result of epostane's structural similarity to the enzyme's natural substrates, leading to competitive inhibition. | ||||||
Finasteride | 98319-26-7 | sc-203954 | 50 mg | $105.00 | 3 | |
Finasteride is a specific inhibitor of 5α-reductase, an enzyme involved in the steroidogenesis pathway. By decreasing the production of dihydrotestosterone, finasteride indirectly affects HSD17B1 activity by altering the balance of steroids and potentially reducing the availability of substrates for HSD17B1. | ||||||
Dutasteride | 164656-23-9 | sc-207600 | 10 mg | $167.00 | 2 | |
Dutasteride inhibits both isoforms of 5α-reductase, and although its primary action is not on HSD17B1, the reduction in dihydrotestosterone levels can lead to decreased substrate availability for HSD17B1, thereby indirectly lowering its activity. | ||||||
Aminoglutethimide | 125-84-8 | sc-207280 sc-207280A sc-207280B sc-207280C | 1 g 5 g 25 g 100 g | $42.00 $146.00 $541.00 $2060.00 | 2 | |
Aminoglutethimide inhibits the enzyme P450scc, which is crucial in the early steps of steroid biosynthesis. This inhibition leads to reduced production of all steroid hormones, including those that serve as substrates for HSD17B1, hence indirectly decreasing HSD17B1 activity. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $63.00 $265.00 | 21 | |
Ketoconazole is known for its broad inhibition of cytochrome P450 enzymes, which are involved in steroid synthesis. By inhibiting these enzymes, ketoconazole can decrease the levels of substrates required by HSD17B1, thereby indirectly inhibiting its activity. | ||||||
Letrozole | 112809-51-5 | sc-204791 sc-204791A | 25 mg 50 mg | $87.00 $147.00 | 5 | |
Although letrozole is typically an activator of HSD17B1 by increasing androgen substrate levels through aromatase inhibition, it can also lead to reduced estrogen levels. As estradiol can upregulate HSD17B1 expression in some tissues, the net effect of letrozole in certain contexts could paradoxically result in decreased HSD17B1 activity by diminishing the positive feedback loop provided by estradiol. | ||||||
2-Methoxyestradiol | 362-07-2 | sc-201371 sc-201371A | 10 mg 50 mg | $71.00 $288.00 | 6 | |
2-Methoxyestradiol is a natural metabolite of estradiol with lower affinity for the estrogen receptor and can compete with substrates for HSD17B1, acting as a competitive inhibitor. This metabolite can bind to the active site of HSD17B1 and prevent the enzyme from converting estrone to the more active estradiol. | ||||||
Danazol | 17230-88-5 | sc-203021 sc-203021A | 100 mg 250 mg | $92.00 $238.00 | 3 | |
Danazol is a synthetic steroid that can downregulate the expression of several enzymes in the steroidogenesis pathway, including HSD17B1. By altering gene expression, danazol indirectly decreases the activity of HSD17B1. | ||||||
Chlormadinone Acetate | 302-22-7 | sc-211070 | 10 mg | $136.00 | ||
Chlormadinone acetate is a synthetic progestin that can act as an inhibitor of several enzymes in the steroidogenesis pathway, potentially including HSD17B1. By mimicking the action of progesterone, it may influence the regulation of enzymes involved in steroid metabolism, leading to decreased HSD17B1 activity. | ||||||