528893-52-9
528893-52-9 structure
- Name: PKF050-638
- Chemical Name: PKF050-638
- CAS Number: 528893-52-9
- Molecular Formula: C13H13ClN4O2
- Molecular Weight: 292.72
- Catalog: Signaling Pathways Anti-infection HIV
- Create Date: 2020-06-01 20:44:48
- Modify Date: 2024-01-15 20:23:13
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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].
| Name | PKF050-638 |
|---|
| 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]. |
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| Related Catalog | |
| 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]. |
| References |
| Molecular Formula | C13H13ClN4O2 |
|---|---|
| Molecular Weight | 292.72 |