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编 号：F380474
分子式：C13H13ClN4O2
分子量：292.72
分子式：C13H13ClN4O2
分子量：292.72
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CAS No: 528893-52-9
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生物活性：
PKF050-638 is a potent and selective inhibitor of HIV-1 Rev (IC50=0.04 μM). PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disrupting CRM1-NES interaction.
体外研究：
Nuclear export of Rev is mediated by its leucine-rich nuclear export signal (NES) and is known to use the CRM1 export factor to export the viral RNA from the nucleus to the cytoplasm. CRM1 is a nuclear export receptor for proteins carrying the leucine-rich NES.PKF050-638 (5 μM; 2 hours) inhibits nuclear export of rev, in addition, the Rev14-GFP mutant accumulates in the nucleus indicating that the NES of Rev is a part of Rev required for export inhibition by PKF050-638.PKF050-638 (7.5 μM; 4 hours) restores the inhibition of export in pRev14-GFP-transfected cells. In cells incubated with PKF050-638, most of the Rev14-GFP is localized in the nucleus and nucleolus. Whereas in untreated cells, Rev14-GFP is still in the cytoplasm. This result shows that the majority of PKF050-638-treated cells are able to reverse completely the inhibitory effects of the agent.PKF050-638 (7.5 μM; 1 hour) is interfering with the CRM1-mediated nuclear export machinery. HeLa cells are cotransfected with the BFP-tagged Rev protein and the GFP-tagged hCRM1. Upon treatment with PKF050-638, this Rev-dependent hCRM1 nucleolar localization is abolished after 60 min, and PKF050-638 does not affect the Rev nucleolar distribution.
PKF050-638 is a potent and selective inhibitor of HIV-1 Rev (IC50=0.04 μM). PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disrupting CRM1-NES interaction.
体外研究：
Nuclear export of Rev is mediated by its leucine-rich nuclear export signal (NES) and is known to use the CRM1 export factor to export the viral RNA from the nucleus to the cytoplasm. CRM1 is a nuclear export receptor for proteins carrying the leucine-rich NES.PKF050-638 (5 μM; 2 hours) inhibits nuclear export of rev, in addition, the Rev14-GFP mutant accumulates in the nucleus indicating that the NES of Rev is a part of Rev required for export inhibition by PKF050-638.PKF050-638 (7.5 μM; 4 hours) restores the inhibition of export in pRev14-GFP-transfected cells. In cells incubated with PKF050-638, most of the Rev14-GFP is localized in the nucleus and nucleolus. Whereas in untreated cells, Rev14-GFP is still in the cytoplasm. This result shows that the majority of PKF050-638-treated cells are able to reverse completely the inhibitory effects of the agent.PKF050-638 (7.5 μM; 1 hour) is interfering with the CRM1-mediated nuclear export machinery. HeLa cells are cotransfected with the BFP-tagged Rev protein and the GFP-tagged hCRM1. Upon treatment with PKF050-638, this Rev-dependent hCRM1 nucleolar localization is abolished after 60 min, and PKF050-638 does not affect the Rev nucleolar distribution.
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