Steroid sulfatase/17β-HSD1-IN-1 是一种有效的类固醇硫酸酯酶 (steroid sulfatase) 和 17β-羟甾类固醇脱氢酶 1 型 (17β-HSD1) 抑制剂,对胞内人类固醇硫酸酯酶的IC50为 28 nM。Steroid sulfatase/17β-HSD1-IN-1 可用于雌激素依赖性疾病的研究。
产品描述
Steroid sulfatase/17β-HSD1-IN-1 is a potent steroid sulfatase and 17β-hydroxysteroid dehydrogenase type 1 ( 17β-HSD1 ) inhibitor with an IC 50 value of 28 nM for cellular human steroid sulfatase. Steroid sulfatase/17β-HSD1-IN-1 can be used to research estrogen-dependent diseases [1].
体外活性
Steroid sulfatase/17β-HSD1-IN-1 (compound 13) (20 μM; 48 h) has a low cytotoxicity in HEK-293 cells [1]. Steroid sulfatase/17β-HSD1-IN-1 (50-750 nM; 0-25 min) can inhibit T47D cells growth and 17β-HSD1 in a time-dependent manner [1]. Cell Cytotoxicity Assay [1] Cell Line: HEK-293 cells Concentration: 20 μM Incubation Time: 48 h Result: Exhibited a low cytotoxicity with the cell growth inhibition of 12.8%. Cell Proliferation Assay [1] Cell Line: T47D Concentration: 50, 100, 250, 500 and 750 nM Incubation Time: 0-25 min Result: Inhibited cell growth and 17β-HSD1 in a time-dependent manner.
体内活性
Steroid sulfatase/17β-HSD1-IN-1 shows good metabolic stability in human hepatic S9 fraction (t 1/2 =47 min) and low intrinsic clearance Clint (15 μL/min/mg protein) [1].
分子式
C19H18N2O5S
分子量
386.42
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years