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

目录号: HY-14585 纯度: 99.99%: FAQs
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摩尔计算器

Estrone O-sulfamate (Estrone 3-O-sulfamate) 是一种有效的类固醇硫酸酯酶 (STS) 抑制剂。Estrone O-sulfamate 对胎盘微粒体 (P.M.) 制剂和 MCF-7 细胞中的 STS 具有抑制活性，IC₅₀ 值分别为 18 nM 和 0.83 nM。Estrone O-sulfamate 可用于癌症的研究。

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Estrone O-sulfamate Chemical Structure

CAS No. : 148672-09-7

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生物活性
纯度 & 产品资料
参考文献

生物活性

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].

细胞效力
(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]

体外研究
(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].

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

分子量

349.44

Formula

C₁₈H₂₃NO₄S

CAS 号

148672-09-7

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

纯度 & 产品资料

纯度: 99.99%

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Data Sheet (530 KB) SDS (251 KB)

COA (196 KB) HNMR (236 KB) LCMS (137 KB)

产品使用指南 (1538 KB)

参考文献

[1]. L W Lawrence Woo, et al. Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors. Bioorg Med Chem. 2012 Apr 15;20(8):2506-19. [Content Brief]

Estrone O-sulfamate 相关分类

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Help & FAQs

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.

Keywords:

Estrone O-sulfamate148672-09-7Estrone 3-O-sulfamateSteroid Sulfatasesteroid sulfatase (STS)placental microsomes (P.M.)MCF-7 cellscancerInhibitorinhibitorinhibit

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

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

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Other Forms of Estrone O-sulfamate: