1. Anti-infection Membrane Transporter/Ion Channel
  2. HIV CRM1
  3. PKF050-638

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。

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PKF050-638 Chemical Structure

PKF050-638 Chemical Structure

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[1].

IC50 & Target

IC50: 0.04 μM (HIV-1 Rev)[1]

体外研究
(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[1].
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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

292.72

Formula

C13H13ClN4O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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产品名称:
PKF050-638
目录号:
HY-114597
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