| Description | PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disrupting CRM1-NES interaction. PKF050-638 is an effective and selective inhibitor of HIV-1 Rev (IC50=0.04 μM). |
| In vitro | 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 (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 displays that the majority of PKF050-638-treated cells are able to reverse completely the inhibitory effects of the agent. 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]. |
| Target activity | HIV-1 Rev:0.04 μM |
| molecular weight | 292.72 |
| Molecular formula | C13H13ClN4O2 |
| CAS | 528893-52-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Daelemans D, et al. A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14440-5. Epub 2002 Oct 9. |