PKF050-638

Category	Human immunodeficiency Virus (HIV)
CAS	528893-52-9
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.

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Product Information

Synonyms	PKF050-638\|528893-52-9\|(2Z)-3-[5-(2-Amino-5-chlorophenyl)-1H-1,2,4-triazol-1-yl]-2-propenoic acid ethyl ester\|SCHEMBL12127035\|ethyl (Z)-3-[5-(2-amino-5-chlorophenyl)-1,2,4-triazol-1-yl]prop-2-enoate\|HY-114597\|CS-0063505\|ethyl (Z)-3-[5-(2-amino-5-chloro-phenyl)-1,2,4-triazol-1-yl]prop-2-enoate\|2-Propenoic acid, 3-[5-(2-amino-5-chlorophenyl)-1H-1,2,4-triazol-1-yl]-, ethyl ester, (2Z)-
Molecular Weight	292.72
Molecular Formula	C13H13ClN4O2
Canonical SMILES	CCOC(=O)C=CN1C(=NC=N1)C2=C(C=CC(=C2)Cl)N
Purity	≥98% (HPLC)
Solubility	Soluble in DMSO
Appearance	Solid powder
Storage	Store at -20°C
Complexity	366
Exact Mass	292.0727034
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.
Target	IC50: 0.04 μM (HIV-1 Rev)
XLogP3-AA	2.1