NCGC00092410 是一种有效，选择性和非糖性葡萄糖脑苷脂酶 (glucocerebrosidase, GC) 抑制剂，IC50 值为 31 nM。NCGC00092410 对相关水解酶没有活性。NCGC00092410 是一种 GC 分子伴侣，可提高突变型细胞株中葡萄糖脑苷脂酶的活性和溶酶体定位。NCGC00092410可用于戈谢病的研究。
NCGC00092410 is a potent, selective, and nonsugar glucocerebrosidase (GC) inhibitor, with an IC50 of 31 nM. NCGC00092410 shows no activity against the related hydrolases at concentrations up to 77 μM. NCGC00092410, a GC chaperone, and increases the activity and lysosomal localization of glucocerebrosidase in mutant cell lines. NCGC00092410 can be used for the research of Gaucher disease[1].
NCGC00092410 (7.3-130 nM; 25 min) inhibits the GC activity at various substrate concentrations (10-150 μM) in a dose-dependent manner[1].NCGC00092410 (55-40 μM; 2 d) increases the GC activity in the N370S mutant fibroblasts[1].NCGC00092410 (40 μM; 60-72 h) increases the lysosomal localization of GC in gaucher fibroblasts[1].
[1]. Zheng W, et, al. Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease. Proc Natl Acad Sci U S A. 2007 Aug 7;104(32):13192-7.
动态评分
0.0