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.
Product information
CAS Number: 528893-52-9
Molecular Weight: 292.72
Formula: C13H13ClN4O2
Chemical Name: ethyl (2Z)-3-[5-(2-amino-5-chlorophenyl)-1H-1,2,4-triazol-1-yl]prop-2-enoate
Smiles: CCOC(=O)/C=C\N1N=CN=C1C1=CC(Cl)=CC=C1N
InChiKey: QWVNYBWNXRRADG-WAYWQWQTSA-N
InChi: InChI=1S/C13H13ClN4O2/c1-2-20-12(19)5-6-18-13(16-8-17-18)10-7-9(14)3-4-11(10)15/h3-8H,2,15H2,1H3/b6-5-
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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. 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.
Products are for research use only. Not for human use.
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