For research use only. Not for therapeutic Use.
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].
R-IMPP stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. R-IMPP does not decrease PCSK9 transcription or increase PCSK9 degradation, but causes transcript-dependent inhibition of PCSK9 translation. R-IMPP is able to selectively bind to human, but not E. coli, ribosomes[1].
| Catalog Number | I046334 |
| CAS Number | 2133832-83-2 |
| Synonyms | N-isoquinolin-1-yl-3-(4-methoxyphenyl)-N-[(3R)-piperidin-3-yl]propanamide |
| Molecular Formula | C24H27N3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H27N3O2/c1-29-21-11-8-18(9-12-21)10-13-23(28)27(20-6-4-15-25-17-20)24-22-7-3-2-5-19(22)14-16-26-24/h2-3,5,7-9,11-12,14,16,20,25H,4,6,10,13,15,17H2,1H3/t20-/m1/s1 |
| InChIKey | OKTGXQMSOIQCTJ-HXUWFJFHSA-N |
| SMILES | COC1=CC=C(C=C1)CCC(=O)N(C2CCCNC2)C3=NC=CC4=CC=CC=C43 |
| Reference | [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 |
