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

PKF050-638 

Cat. No.: HY-114597
Handling Instructions

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.

For research use only. We do not sell to patients.

PKF050-638 Chemical Structure

PKF050-638 Chemical Structure

CAS No. : 528893-52-9

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Description

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]

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].

Molecular Weight

292.72

Formula

C₁₃H₁₃ClN₄O₂

CAS No.

528893-52-9

SMILES

O=C(OCC)/C=C\N1N=CN=C1C2=CC(Cl)=CC=C2N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

PKF050-638HIVCRM1Human immunodeficiency virusChromosomal Maintenance 1Exportin 1XPO1RevHeLacellsnucleolarlocalizationtumorInhibitorinhibitorinhibit

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PKF050-638
Cat. No.:
HY-114597
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