PLpro inhibitor

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Chemical Structure| 1093070-14-4 同义名 : PLpro Inhibitor 6; KOM-70144; PLpro inhibitor, KOM70144
CAS号 : 1093070-14-4
货号 : A449583
分子式 : C22H22N2O2
纯度 : 99%+
分子量 : 346.42
MDL号 : MFCD12547684
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(303.1 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

生物活性
描述 The papain-like protease (PLpro) can process the viral polyprotein in a coordinated manner and strip ubiquitin and ISG15 from host-cell proteins to aid coronaviruses in their evasion of the host innate immune responses. Therefore, PLpro is an attractive antiviral drug target for its essential role for coronaviral replication[2]. PLpro inhibitor is a potent inhibitor against the PLpro from the coronavirus that causes severe acute respiratory syndrome (SARS-CoV). PLpro inhibitor was found to have an IC50 value of 2.6 ± 0.1 μM. PLpro inhibitor displayed significant antiviral activity with an EC50 value of 13.1 ± 0.7 uM, without toxicity up to the highest concentration tested. Notably, the increasing antiviral potency correlated with the in vitro inhibition of PLpro, suggesting that the compound works directly on the enzyme in cellshttp://www.google.com/patents/WO2010022355A1cl=en.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.89mL

0.58mL

0.29mL

14.43mL

2.89mL

1.44mL

28.87mL

5.77mL

2.89mL

参考文献

[1]Ratia, K., et al., A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication. Proc Natl Acad Sci U S A, 2008. 105(42): p. 16119-24.

[2]Báez-Santos YM, et al. The SARS-coronavirus papain-like protease: structure, function and inhibition by designed antiviral compounds. Antiviral Res. 2015 Mar;115:21-38