Estrone sulfate
Based on 3 publication(s) in Google Scholar
Estrone sulfate is an inactive endogenous estrogen that can be converted into Estrone (HY-B0234) and Estradiol (HY-B0141). Estrone sulfate is also a substrate of the OATP1B3 transporter. Estrone sulfate can be converted into Estrone and Estradiol in normal mammary parenchymal cells. Estrone sulfate stimulates the growth of nitrosomethylurea-induced mammary tumors in ovariectomized rats and the colony formation of dispersed nitrosomethylurea mammary cells, with conversion into Estrone and Estradiol occurring both in vivo and in vitro during this process. Estrone sulfate is applicable to breast cancer-related research.
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- CAS No.: 481-97-0
- Formule: C18H22O5S
- Masse moléculaire:350.43
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Stockage:
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Estrone sulfate
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Activité biologique
Description
IC50 & Target
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Human Endogenous Metabolite |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| JEG-3 | IC50 |
7600 nM
Compound: E1S (enzyme substrate)
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Estrone sulfatase activity against homogenized human JEG-3 cells was determined by measuring the [3H]E1 obtained from [3H]E1S
Estrone sulfatase activity against homogenized human JEG-3 cells was determined by measuring the [3H]E1 obtained from [3H]E1S
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[PMID: 9873454] |
| JEG-3 | IC50 |
7600 nM
Compound: Estrone sulfate (E1S)
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Inhibition of steroid sulfatase activity of JEG-3 cells
Inhibition of steroid sulfatase activity of JEG-3 cells
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[PMID: 11087571] |
| Sf9 | IC50 |
45 μM
Compound: Estrone-3-sulfate
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TP_TRANSPORTER: inhibition of E217betaG uptake in membrane vesicles from MRP4-expressing Sf9 cells
TP_TRANSPORTER: inhibition of E217betaG uptake in membrane vesicles from MRP4-expressing Sf9 cells
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[PMID: 12523936] |
| Sf9 | IC50 |
95 μM
Compound: Estrone-3-sulfate
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TP_TRANSPORTER: inhibition of DHEAS in membrane vesicles from MRP4-expressing Sf9 cells
TP_TRANSPORTER: inhibition of DHEAS in membrane vesicles from MRP4-expressing Sf9 cells
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[PMID: 12523936] |
In Vitro
Estrone sulfate (1.0 μM; 1-64 min) is taken up at a low rate by dispersed normal breast parenchymal cells, resulting in a cells/medium concentration ratio of 0.20-0.33 when incubated at 37°C[2].
Estrone sulfate (1.0 nM-100 μM) is converted to estrone by dispersed normal breast parenchymal cells with a mean half-time of 628 min per 106 cells (intact cells) or 246 min per 106 cells (homogenized cells)[2].
Estrone sulfate is not produced via conversion of estrone by dispersed normal breast parenchymal cells under conditions where MCF-7 breast cancer cells exhibit sulfotransferase activity[2].
Estrone sulfate stimulates colony formation in dispersed nitrosomethylurea mammary cells and is converted to estrone and estradiol by these cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Estrone sulfate (75 mg/kg; p.o; daily; for 5 days) reduces glucose-6-phosphatase activity and protein levels, and lowers blood glucose in ob/ob mice[4].
Estrone sulfate modulates glucose-6-phosphatase kinetic parameters in control mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (female, castrated, nitrosomethylurea-induced mammary tumor model)[3]
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Dosage:30 pmol/hr; 300 pmol/hr; 3000 pmol/hr; 400 pmol/hr; 1300 pmol/hr
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Administration:s.c.; continuous infusion; 14 days
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Result:Did not significantly alter castration-induced tumor regression at 30 pmol/hr; partially blunted castration-induced tumor regression at 300 pmol/hr; stimulated tumor growth at 3000 pmol/hr; Observed significantly different tumor growth slopes for 300 and 3000 pmol/hr doses; Detected 14%, 10%, and 13% conversion to estradiol, and 24%, 22%, and 28% conversion to estrone on days 7, 10, and 14, respectively, at 400 pmol/hr; Recorded similar conversion rates at 1300 pmol/hr; Measured serum estradiol levels of 17 pg/ml (400 pmol/hr), 56 pg/ml (1300 pmol/hr), 6.8 ± 1.2 pg/ml (300 pmol/hr, day 14), and 48 ± 10.2 pg/ml (3000 pmol/hr, day 14).
Chemical Information
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CAS No. 481-97-0
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Masse moléculaire 350.43
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Formule C18H22O5S
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SMILES
C[C@]1([C@](CC2)([H])[C@]3([H])CCC4=C(C=CC(OS(=O)(O)=O)=C4)[C@@]3([H])CC1)C2=O
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Res
2023 Dec;33(12):940-951. PMID: 37674011 -
Nat Commun
2025 Aug 30;16(1):8124. PMID: 40885756 -
ACS Omega
Association Study of OATP1B3 Polymorphisms on Hepatic Uptake and Drug-Drug Interaction In Vitro. [Abstract]2025 Oct 29;10(44):52562-52575. PMID: 41244417
Pureté et documentation
Références
[1]. Yang Z, et al. Association Study of OATP1B3 Polymorphisms on Hepatic Uptake and Drug-Drug Interaction In Vitro. ACS Omega. 2025;10(44):52562-52575. Published 2025 Oct 29. [Content Brief]
[2]. Chatterton RT Jr, et al. Formation of estrone and estradiol from estrone sulfate by normal breast parenchymal tissue. J Steroid Biochem Mol Biol. 2003;86(2):159-166. [Content Brief]
[3]. Santner SJ, et al. Estrone sulfate stimulates growth of nitrosomethylurea-induced breast carcinoma in vivo in the rat. Int J Cancer. 1990;46(1):73-78. [Content Brief]
[4]. Borthwick EB, et al. The antihyperglycemic effect of estrone sulfate in genetically obese-diabetic (ob/ob) mice is associated with reduced hepatic glucose-6-phosphatase. Horm Metab Res. 2001 Dec;33(12):721-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Estrone sulfate Related Classifications
HY-113293 Related Classifications
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