CAS NO: | 528893-52-9 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | PKF050-638 is a potent and selective inhibitor ofHIV-1Rev(IC50=0.04 μM). PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disruptingCRM1-NESinteraction[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]. |
分子量 | 292.72 |
Formula | C13H13ClN4O2 |
CAS 号 | 528893-52-9 |
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. |