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PKF050-638

CAS No. : 528893-52-9

MCE 站：PKF050-638

产品活性：PKF050-638 是一种有效且具有选择性的 HIV-1 Rev 抑制剂 (IC₅₀=0.04 μM)。 PKF050-638 通过破坏 CRM1-NES 相互作用抑制 CRM1 介导的 Rev 核输出。

研究领域：Anti-infection  |  Membrane Transporter/Ion Channel

作用靶点：HIV  |  CRM1

In Vitro: 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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