PF-06446846 is an orally active proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PF-06446846 directly and selectively inhibits translation of PCSK9 by stalling 80S ribosomes near codon regions.
PF-06446846 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Huh7 cells
0.3 µM
Overnight
Inhibited PCSK9 secretion with an IC50 of 0.3 μM
PLoS Biol. 2017 Mar 21;15(3):e2001882
HEK293T cells
4 µM
20 hours
To test whether PF846 can selectively inhibit translation termination in cells
Nat Commun. 2020 Oct 2;11(1):4941
HeLa cells
0.1 mM
23 minutes
To investigate the mechanism of selective stalling of human ribosomes by PF846, results showed that PF846 selectively stalls translation of specific mRNAs.
Nat Struct Mol Biol. 2019 Jun;26(6):501-509
HeLa cells
50 µM
23 minutes
To assess the effects of mutations in the nascent-chain sequence on PF846-dependent inhibition of translation termination
Nat Commun. 2020 Oct 2;11(1):4941
HeLa cells
50 µM
45 minutes
Inhibited translation of PCSK9(1-35)-luciferase fusion constructs
PLoS Biol. 2017 Mar 21;15(3):e2001882
JHOS2 cells
100 µM
48 hours
Evaluate the effect of PF-06446846 on JHOS2 cell proliferation, showing 85% cell survival, indicating that PCSK9 plays a survival role in these cancer cells.
Cancers (Basel). 2021 Jul 24;13(15):3727
OVCAR3cis cells
100 µM
48 hours
Evaluate the effect of PF-06446846 on OVCAR3cis cell proliferation, showing significant inhibition at 100 μM concentration.
Cancers (Basel). 2021 Jul 24;13(15):3727
OVCAR3 cells
100 µM
48 hours
Evaluate the effect of PF-06446846 on OVCAR3 cell proliferation, showing significant inhibition at 100 μM concentration.
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