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Steroid sulfatase (STS) inhibitors block the enzyme that frees active steroids from their sulfate conjugates. STS hydrolyzes estrone sulfate to estrone and dehydroepiandrosterone sulfate (DHEAS) to dehydroepiandrosterone (DHEA). Both products can be converted into active estrogens and androgens, so the enzyme is studied in hormone-dependent breast, endometrial and prostate cancers. A 2005 review summarized the molecular biology, regulation and inhibition of this membrane-bound enzyme of the endoplasmic reticulum. Estrone O-sulfamate is an aryl sulfamate that inactivates the enzyme irreversibly, and estradiol 3-sulfamate carries the same sulfamate group. Irosustat, a tricyclic coumarin sulfamate described in 2000, is a nonsteroidal inhibitor, and KW-2581 is listed as a further STS inhibitor.
Synonyms: STX64; BN83495; 667-Coumate
Irosustat is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.
Protein Kinase Inhibitor 14 is a potent inhibitor of serine/threonine kinases as well as receptor and non-receptor tyrosine kinases. This compound is valuable for studying kinase signaling pathways and can be utilized in various cellular and molecular biology research applications. Its inhibitory effects on these kinases make it an important tool for exploring kinase-related mechanisms in disease models.
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Synonyms: Estrone 3-O-sulfamate
Estrone O-sulfamate is a potent inhibitor of steroid sulfatase (STS), a key enzyme involved in steroid hormone metabolism. It demonstrates significant inhibitory activity with IC50 values of 18 nM in placental microsomes and 0.83 nM in MCF-7 cells. This compound is valuable for research focused on cancer, as it helps elucidate the role of STS in tumorigenesis and hormone-driven malignancies.
Synonyms: BLE 00084; E2MATE; ES-J 995
Estradiol 3-sulfamate is a potent steroid sulfatase inhibitor, effectively targeting estrone sulfatase with an IC50 value of 251 nM and a Ki of 133 nM. This compound is recognized for its long-acting and orally active properties, making it a valuable reagent for research applications focused on hormone metabolism and endocrine signaling. Its ability to modulate sulfated steroid levels supports investigations into various biological processes, including cancer research and reproductive health studies.
KW-2581 is a selective steroid sulfatase (STS) inhibitor, exhibiting an IC50 of 4 nM. This compound effectively inhibits STS activity in ZR-75-1 cells with an IC50 of 13 nM, demonstrating significant impairment of E1S-stimulated cell growth at an IC50 of 0.18 nM. KW-2581 has shown the ability to inhibit sulfated estrogen-dependent proliferation of breast cancer cells both in vitro and in vivo, leading to tumor regression in E1S-induced models. This reagent is suitable for studies focused on hormone receptor-positive breast cancer and the role of steroid sulfatase in tumor biology.
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Synonyms: NSC 732011; HLX-801
SR-16157 is a dual-action steroid sulfatase (STS) inhibitor and selective estrogen receptor alpha (ERα) modulator, with an IC50 of 0.1 µM. This compound displays potent STS inhibitory and anti-estrogenic effects in breast cancer cells, making it a valuable tool for understanding the role of estrogen signaling in cancer progression. SR-16157 is applicable in breast cancer research, particularly in studies exploring therapeutic strategies targeting estrogen metabolism and receptor modulation.
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Steroid sulfatase-IN-10 is a potent inhibitor of steroid sulfatase, exhibiting an IC50 range of 0.03-0.27 µM. This compound is valuable for investigating its role in various inflammatory conditions, including rheumatoid arthritis, type 1 and type 2 diabetes, and systemic lupus erythematosus. Its selective inhibition of steroid sulfatase makes it a useful tool in exploring therapeutic avenues for these diseases.
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Steroid sulfatase/17β-HSD1-IN-3 is a potent dual inhibitor targeting steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). It irreversibly inhibits human STS activity with an IC50 of 27 nM, demonstrating significant efficacy. This compound is suitable for research focused on endometriosis and other estrogen-dependent diseases, facilitating the exploration of therapeutic strategies in these areas.
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Steroid Sulfatase-IN-2 is a potent steroid sulfatase (STS) inhibitor, exhibiting an IC50 value of 109.5 nM. This compound enables research into hormone-dependent cancers, particularly those driven by estrogen, such as breast and endometrial cancer. Its role as an STS inhibitor makes it a valuable tool for understanding the molecular mechanisms underlying these cancer types and exploring potential therapeutic strategies.
Steroid sulfatase-IN-8 is a potent steroid sulfatase (STS) inhibitor, demonstrating a pharmacological IC50 of 1 nM in PM models and 0.025 nM in JEG-3 cells. This compound effectively interferes with steroid metabolism, making it a valuable tool for investigating steroid-related pathways. Its application extends to studies on hormone-dependent cancers and other conditions linked to altered steroid levels.
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DU-14 is a potent inhibitor of steroid sulfatase, exhibiting an IC50 of 55.8 nM. It effectively reduces MCF-7 cell proliferation, with an IC50 value of 38.7 nM. Additionally, DU-14 demonstrates neuroprotective properties against neurotoxic amyloid-beta (Aβ), indicating its potential to up-regulate endogenous dehydroepiandrosterone sulfate (DHEAS) and alleviate Aβ-induced deficits in spatial memory and synaptic plasticity. This compound is valuable for research in cancer biology and neurodegenerative diseases.
Steroid sulfatase-IN-4 is an irreversible inhibitor of steroid sulfatase (STS), exhibiting an IC50 of 25 nM against human STS. This compound is primarily utilized in research focused on endometriosis, offering potential insights into the role of STS in disease progression and therapeutic interventions. Its selective inhibition of STS facilitates the exploration of hormonal pathways involved in reproductive health.
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Steroid sulfatase-IN-3 is a potent inhibitor of steroid sulfatase (STS) with an IC50 value of 25.8 nM. This compound exhibits significant antiproliferative activity against T-47D estrogen-dependent breast cancer cells, demonstrating an IC50 of 1.04 µM. Steroid sulfatase-IN-3 is primarily utilized in cancer research to explore the role of STS in hormone-dependent tumor progression and treatment resistance.
Steroid sulfatase-IN-1 is a highly effective inhibitor of steroid sulfatase, exhibiting an IC50 value of 1.71 nM. This compound demonstrates significant antitumor activity in vivo, indicating its potential utility in cancer research. Steroid sulfatase-IN-1 is particularly relevant for studies focused on breast cancer, providing insights into mechanisms of disease and potential therapeutic approaches.
Steroid sulfatase/17β-HSD1-IN-1 is a potent inhibitor of steroid sulfatase and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1), exhibiting an IC50 value of 28 nM for human steroid sulfatase in cellular assays. This compound is valuable for investigating estrogen-dependent diseases, making it an important tool for research in hormone-related therapeutic areas. Its specificity and potency support studies aiming to elucidate the role of these enzymes in disease mechanisms.
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Steroid sulfatase/17β-HSD1-IN-4 is a potent dual inhibitor of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1 (17β HSD1). It irreversibly inhibits hSTS activity, demonstrating an IC50 value of 63 nM. This compound is valuable for studying endometriosis and other estrogen-dependent diseases, providing insights into the role of steroid metabolism in these conditions.
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Steroid sulfatase-IN-11 is a potent inhibitor of steroid sulfatase, an enzyme that hydrolyzes steroid sulfates. By effectively reducing steroid sulfatase activity, this compound is instrumental in the study of hormone-dependent cancers. Its application in research provides valuable insights into the role of steroid metabolism in cancer progression and therapeutic resistance.
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