1. Metabolic Enzyme/Protease
  2. Steroid Sulfatase
  3. Estrone O-sulfamate

Estrone O-sulfamate  (Synonyms: Estrone 3-O-sulfamate)

Cat. No.: HY-14585 Purity: 99.99%
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Estrone O-sulfamate (Estrone 3-O-sulfamate) is a potent steroid sulfatase (STS) inhibitor. Estrone O-sulfamate has inhibitory activity for STS in a placental microsomes (P.M.) preparation and in MCF-7 cells with IC50 values of 18 nM and 0.83 nM, respectively. Estrone O-sulfamate can be used for the research of cancer.

For research use only. We do not sell to patients.

Estrone O-sulfamate Chemical Structure

Estrone O-sulfamate Chemical Structure

CAS No. : 148672-09-7

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Based on 1 publication(s) in Google Scholar

Other Forms of Estrone O-sulfamate:

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Description

Estrone O-sulfamate (Estrone 3-O-sulfamate) is a potent steroid sulfatase (STS) inhibitor. Estrone O-sulfamate has inhibitory activity for STS in a placental microsomes (P.M.) preparation and in MCF-7 cells with IC50 values of 18 nM and 0.83 nM, respectively. Estrone O-sulfamate can be used for the research of cancer[1].

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.9 μM
Compound: 1; EMATE
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
[PMID: 34458740]
HEK293 IC50
0.9 nM
Compound: 1
Inhibition of human placental steroid sulfatase expressed in HEK293 cells using [3H] E1S as substrate after 2 hrs by liquid scintillation counting method
Inhibition of human placental steroid sulfatase expressed in HEK293 cells using [3H] E1S as substrate after 2 hrs by liquid scintillation counting method
[PMID: 31255926]
HEK293 IC50
0.9 nM
Compound: 10; EMATE
Inhibition of human placental estrone sulfatase expressed in HEK293 cells using [3H]E1S as substrate incubated for 2 hrs by liquid scintillation counting method
Inhibition of human placental estrone sulfatase expressed in HEK293 cells using [3H]E1S as substrate incubated for 2 hrs by liquid scintillation counting method
[PMID: 26974384]
HEK293 IC50
1.6 nM
Compound: 10; EMATE
Inhibition of estrone sulfatase (unknown origin) transfected in HEK293 cells using [3H]E1S as substrate incubated for 2 hrs by liquid scintillation counting method
Inhibition of estrone sulfatase (unknown origin) transfected in HEK293 cells using [3H]E1S as substrate incubated for 2 hrs by liquid scintillation counting method
[PMID: 26974384]
HEK293 IC50
1.6 nM
Compound: 3-Sulfamoylestrone (EMATE)
Inhibition of steroid sulfatase activity by the compound was determined in human embryonic kidney (HEK)-293 cells transfected with a sulfatase expression vector (pCMV-sulfa) using 100 uM of [3H]E1S
Inhibition of steroid sulfatase activity by the compound was determined in human embryonic kidney (HEK)-293 cells transfected with a sulfatase expression vector (pCMV-sulfa) using 100 uM of [3H]E1S
[PMID: 11087571]
HEK293 IC50
2.4 nM
Compound: 3-Sulfamoylestrone (EMATE)
Inhibition of steroid sulfatase activity by the compound was determined in human embryonic kidney (HEK)-293 cells transfected with a sulfatase expression vector (pCMV-sulfa) using 100 uM of [14C]-DHEAS
Inhibition of steroid sulfatase activity by the compound was determined in human embryonic kidney (HEK)-293 cells transfected with a sulfatase expression vector (pCMV-sulfa) using 100 uM of [14C]-DHEAS
[PMID: 11087571]
HeLa IC50
0.63 μM
Compound: 1; EMATE
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
[PMID: 34458740]
HepG2 IC50
0.85 μM
Compound: 1; EMATE
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
[PMID: 34458740]
JEG-3 IC50
3.2 nM
Compound: 10; EMATE
Inhibition of estrone sulfatase in human JEG-3 cells using [3H]-estrone sulphate as substrate incubated for 4 hrs by liquid scintillation counting method
Inhibition of estrone sulfatase in human JEG-3 cells using [3H]-estrone sulphate as substrate incubated for 4 hrs by liquid scintillation counting method
[PMID: 26974384]
JEG-3 IC50
7600 nM
Compound: EIS
Reversible inhibition of steroid sulfatase in human JEG3 cells using [3H] E1S as substrate by scintillation counting method
Reversible inhibition of steroid sulfatase in human JEG3 cells using [3H] E1S as substrate by scintillation counting method
[PMID: 32122754]
MCF7 IC50
0.07 μM
Compound: 1; EMATE
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
[PMID: 34458740]
MCF7 IC50
0.83 nM
Compound: EMATE
Inhibition of steroid sulfatase in human MCF7 cells using [3H]E1S as substrate after 20 hrs by scintillation spectrometry
Inhibition of steroid sulfatase in human MCF7 cells using [3H]E1S as substrate after 20 hrs by scintillation spectrometry
[PMID: 22455789]
MCF7 IC50
22.8 μM
Compound: 13 (EMATE)
Anti-proliferative activity against MCF-7 human breast cancer cells was determined by using MCF-7 plate assay
Anti-proliferative activity against MCF-7 human breast cancer cells was determined by using MCF-7 plate assay
[PMID: 15149660]
MCF7 IC50
65 pM
Compound: 1; EMATE
Irreversible inhibition of estrone sulfatase in human MCF7 cells using [3H]estrone sulfate as substrate preincubated for 2 hrs followed by substrate addition measured after 20 hrs
Irreversible inhibition of estrone sulfatase in human MCF7 cells using [3H]estrone sulfate as substrate preincubated for 2 hrs followed by substrate addition measured after 20 hrs
10.1039/C6MD00113K
MGC-803 IC50
0.48 μM
Compound: 1; EMATE
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
[PMID: 34458740]
MKN-45 IC50
0.54 μM
Compound: 1; EMATE
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
[PMID: 34458740]
In Vitro

Estrone O-sulfamate (Estrone 3-O-sulfamate) has inhibitory activity for STS in a placental microsomes (P.M.) preparation and in MCF-7 cells with IC50 values of 18 nM and 0.83 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

349.44

Formula

C18H23NO4S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@](CCC2=O)([H])[C@@]3([H])[C@@](CC1)([H])C4=CC=C(OS(N)(=O)=O)C=C4CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Purity & Documentation
References
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    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 O-sulfamate
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