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)