复合蛋白酶/复合酶/Compound proteinase

 Description
Biochem/physiol Actions SID 852843 is an inhibitor of West Nile Virus NS2B-NS3 proteinase. Flaviviruses, such as West Nile and Dengue, are a threat to humans from both public health and bioterrorism perspectives. The NS3 proteinase is essential for flaviviral maturation. Inhibitors of NS3 are sought for treatment and prophylactic therapeutics. The NIH molecular library was screened for activity against West Nile Virus NS3, resulting in the discovery of SID 852843. This compound inhibits the NS3 proteinase of West Nile, but not of Dengue type 2 virus. SID 852843 is a reversible, allosteric inhibitor of the formation of the functional conformation of the NS3 proteinase. This is the first flaviviral proteinase inhibitor with the potential to lead to a drug. Aprotinin is an efficient inhibitor of NS3, but it is not selective and has low penetration into cells, limiting its potential for therapeutic use.

Properties
assay ≥98% （HPLC）
form powder
color white to off-white
solubility DMSO: 10 mg/mL
storage temp. 2-8°C

Safety
WGK Germany NWG

References
reference Motlekar, N., et al., Evaluation of an orthogonal pooling strategy for rapid high-throughput screening of proteases. Assay Drug Dev. Technol. 6, 395-405, （2009）
  Johnston, P.A., et al., HTS identifies novel and specific uncompetitive inhibitors of the two-component NS2B-NS3 proteinase of West Nile Virus. Assay Drug Dev. Technol. 5, 737-750, （2007）

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