1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. Endogenous Metabolite Estrogen Receptor/ERR
  3. Estrone sulfate

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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Estrone sulfate

Estrone sulfate Chemical Structure

CAS No. : 481-97-0

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Based on 3 publication(s) in Google Scholar

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Description

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[1][2][3][4].

IC50 & Target

Human Endogenous Metabolite

 

Cellular Effect
Cell Line Type Value Description References
JEG-3 IC50
7600 nM
Compound: E1S (enzyme substrate)
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
[PMID: 9873454]
JEG-3 IC50
7600 nM
Compound: Estrone sulfate (E1S)
Inhibition of steroid sulfatase activity of JEG-3 cells
Inhibition of steroid sulfatase activity of JEG-3 cells
[PMID: 11087571]
Sf9 IC50
45 μM
Compound: Estrone-3-sulfate
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
[PMID: 12523936]
Sf9 IC50
95 μM
Compound: Estrone-3-sulfate
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
[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 (30-3000 pmol/hr; 400-1300 pmol/hr; s.c.; continuous infusion; 14 days) exerts dose-related stimulatory effects on nitrosomethylurea-induced hormone-responsive mammary tumor growth in castrate rats, with significant conversion to estrone and estradiol[3].
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.

Animal Model: Sprague-Dawley (female, castrated, nitrosomethylurea-induced mammary tumor model)[3]
Dosage: 30 pmol/hr; 300 pmol/hr; 3000 pmol/hr; 400 pmol/hr; 1300 pmol/hr
Administration: s.c.; continuous infusion; 14 days
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).
Molecular Weight

350.43

Formula

C18H22O5S

CAS No.
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

Structure Classification
Initial Source
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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Estrone sulfate
Cat. No.:
HY-113293
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