Irosustat (STX64)

A steroid sulfatase inhibitor

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5mg

￥1200.00

960.00

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10mg

￥1937.00

1550.00

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25mg

￥4062.00

3250.00

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50mg

￥6850.00

5480.00

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100mg

￥11762.00

9410.00

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Background

STX-64 is a steroid sulfatase inhibitor (IC₅₀ = 0.008 ?M in placental microsomes).¹ It also inhibits carbonic anhydrase II (CAII; IC₅₀ = 0.025 ?M).² STX-64 inhibits LPS-induced production of nitric oxide (NO) and prostaglandin E₂ in RAW 264.7 macrophages (IC₅₀s = 85.76 and 0.081 ?M, respectively).³ It reduces rat liver steroid sulfatase activity when administered at a dose of 1 mg/kg.¹ STX-64 (2 mg/kg) inhibits estrone sulfate-induced uterine growth and reduces the growth of N-nitroso-N-methylurea-induced, estrone sulfate-maintained mammary tumors in ovariectomized rats.⁴

1.Malini, B., Purohit, A., Ganeshapillai, D., et al.Inhibition of steroid sulphatase activity by tricyclic coumarin sulphamatesJ. Steroid Biochem. Mol. Biol.75(4-5)253-258(2000) 2.Ho, Y.T., Purohit, A., Vicker, N., et al.Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamatesBiochem. Biophys. Res. Commun.305(4)909-914(2003) 3.Jang, H.-L., El-Gamal, M.I., Choi, H.-E., et al.Synthesis of tricyclic fused coumarin sulfonates and their inhibitory effects on LPS-induced nitric oxide and PGE2 productions in RAW 264.7 macrophagesBioorg. Med. Chem. Lett.24(2)571-575(2014) 4.Purohit, A., Woo, L.W., Potter, B.V., et al.In vivo inhibition of estrone sulfatase activity and growth of nitrosomethylurea-induced mammary tumors by 667 COUMATECancer Res.60(13)3394-3396(2000)

Protocol

Cell experiment:

MCF-7 cells are cultured in growth medium (minimum essential medium (MEM) containing, phenol red, 10% foetal calf serum (FCS) and essential nutrients). When the cells reach 60% confluency, they are treated with Irosustat (0.001-10 μM) in growth medium. After 72 h of incubation, photographs are taken under normal conditions of light and the number of attached cells in each flask is determined using a Coulter cell counter[2].

Animal experiment:

Rats[1]Ludwig rats bearing mammary tumors are used in the assay. Tumor development is monitored, and animals are ovariectomized when tumors reach 0.8-1.5 cm in diameter. Tumors are allowed to regress over a 12- to 13-day period to confirm their hormone-dependent status. Regrowth of tumors is stimulated with oestrone sulfate (E1S; 50 μg/day, s.c.). When tumors have regrown, animals continue to receive either E1S alone or E1S plus Irosustat at 10 mg/kg/day or 2 mg/kg/day, p.o., until tumor regression has occurred. Tumor volumes are calculated from two measured diameters[1].

参考文献:

[1]. Purohit A, et al. In vivo inhibition of estrone sulfatase activity and growth of nitrosomethylurea-induced mammary tumors by 667 COUMATE. Cancer Res. 2000 Jul 1;60(13):3394-6.
[2]. Raobaikady B, et al. Inhibition of MCF-7 breast cancer cell proliferation and in vivo steroid sulphatase activity by 2-methoxyoestradiol-bis-sulphamate. J Steroid Biochem Mol Biol. 2003 Feb;84(2-3):351-8.