2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
Irosustat, also known as STX64, BN83495 and 667 coumate, is a potent, irreversible inhibitor of steroid sulfatase. Inhibition of steroid sulfatase (STS), the enzyme responsible for the hydrolysis of steroid sulfates, represents a potential novel treatment for postmenopausal women with hormone-dependent breast cancer. Estrone and DHEA are formed by this sulfatase pathway and can be converted to steroids (estradiol and androstenediol, respectively), which have potent estrogenic properties. STX64 (667 coumate) is a potent tricylic coumarin-based sulfamate that irreversibly inhibits STS activity (IC50 = 8 nM in a placental microsomal assay system). Estrone sulfamate (EMATE) is also a potent STS inhibitor, but has estrogenic activity.