Description
(R)-IMPP is a cell-permeable inhibitor of the secretion of proprotein convertase subtilisin/kexin type 9 (PCSK9; IC
50 = 4.8 μM). It promotes the uptake of LDL cholesterol in hepatoma cells by increasing LDL receptor levels. (R)-IMPP apparently impairs PCSK9 secretion by causing transcript-dependent inhibition of PCSK9 translation.
Uses
R-IMPP (PF-00932239) is an anti-secretagogue of PCSK9 (IC50=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation[1].
References
[1] Petersen DN, et al. A Small-Molecule Anti-secretagogue of PCSK9 Targets the 80S Ribosome to Inhibit PCSK9 Protein Translation. Cell Chem Biol. 2016 Nov 17;23(11):1362-1371 DOI:
10.1016/j.chembiol.2016.08.016
