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[High-throughput Screening of Human Soluble Protein Tyrosine Phosphatase 1B Inhibitors]

[High-throughput Screening of Human Soluble Protein Tyrosine Phosphatase 1B Inhibitors]

Xiao-bin Pang, Xin-mei Xie, Shou-bao Wang, Guan-hua Du

Yao Xue Xue Bao. 2011 Sep;46(9):1058-64.

PMID: 22121775

Abstract:

To screen potential human soluble protein tyrosine phosphatase 1B (PTP1B) inhibitors, a high-throughput screening (HTS) model in 384-well microplate with total volume of 50 microL was established. Recombinant PTP1B was cloned and expressed in E. coli. with its specific substrate 4-nitrophenyl phosphate disodium salt hexahydrate (PNPP). The HTS model was based on enzyme reaction rate with enhanced sensitivity and specificity (Z' = 0.78). A total of 24,240 samples were screened, among them 80 samples with inhibition greater than 70% were selected for further rescreening. Finally, six compounds with high inhibitory activity were identified, whose IC50 values were 21.58, 18.39, 15.37, 11.92, 37.27, and 36.61 microg x mL(-1), separately. The results indicated that the method was stable, sensitive, reproducible and also suitable for high-throughput screening.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP333338184-A	4-Nitrophenyl phosphate disodium salt hexahydrate		333338-18-4	Price

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