2173005-10-0
Chemical Structure
R-IMPP hydrochloride
Synonym(s): PF-00932239 hydrochloride
- CAS No.: 2173005-10-0
- Formula:C24H28ClN3O2
- Molecular Weight:425.95
IUPAC Name: (R)-N-(isoquinolin-1-yl)-3-(4-methoxyphenyl)-N-(piperidin-3-yl)propanamide hydrochloride
InChIKey: OSIRDWNTKGVIOE-VEIFNGETSA-N
SMILES: COC(C=C1)=CC=C1CCC(N([C@@H]2CCCNC2)C3=NC=CC4=C3C=CC=C4)=O.Cl
Biological Activity: R-IMPP hydrochloride (PF-00932239 hydrochloride) is a PCSK9 translation inhibitor and a selective 80S ribosome binder. R-IMPP hydrochloride inhibits the KRAS/MEK/ERK signaling cascade. R-IMPP hydrochloride reduces LPS-induced nuclear translocation of NFkB P65. R-IMPP hydrochloride increases LDL-R levels in cells, promotes LDL-C uptake, and does not alter the secretion of transferrin or albumin. R-IMPP hydrochloride inhibits the growth of colorectal cancer (CRC) cells, organoids and xenografts carrying APC/KRAS mutations, as well as the number and burden of spontaneous mouse tumors. R-IMPP hydrochloride can be used in research related to colorectal cancer with APC/KRAS mutations, hepatic ischemia-reperfusion injury and hypercholesterolemia[1][2][3].
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R-IMPP hydrochloride | R-IMPP hydrochloride (PF-00932239 hydrochloride) is a PCSK9 translation inhibitor and a selective 80S ribosome binder. R-IMPP hydrochloride inhibits the KRAS/MEK/ERK signaling cascade. R-IMPP hydrochloride reduces LPS-induced nuclear translocation of NFkB P65. R-IMPP hydrochloride increases LDL-R levels in cells, promotes LDL-C uptake, and does not alter the secretion of transferrin or albumin. R-IMPP hydrochloride inhibits the growth of colorectal cancer (CRC) cells, organoids and xenografts carrying APC/KRAS mutations, as well as the number and burden of spontaneous mouse tumors. R-IMPP hydrochloride can be used in research related to colorectal cancer with APC/KRAS mutations, hepatic ischemia-reperfusion injury and hypercholesterolemia. | |||||||||||||||||||||
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References
- [1]. Wong CC, et al. The cholesterol uptake regulator PCSK9 promotes and is a therapeutic target in APC/KRAS-mutant colorectal cancer. Nature communications. 2022 Jul 08;13(1):3971.
- [2]. Zhang Y, et al. Blockade of Hepatocyte PCSK9 Ameliorates Hepatic Ischemia-Reperfusion Injury by Promoting Pink1-Parkin-Mediated Mitophagy. Cellular and molecular gastroenterology and hepatology. 2024;17(1):149-169. [Content Brief]
- [3]. 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. [Content Brief]
