193275-86-4
Chemical Structure
(Rac)-Lonafarnib
Synonym(s): Sch66336 racemate
- CAS No.: 193275-86-4
- Formula:C27H31Br2ClN4O2
- Molecular Weight:638.82
IUPAC Name: 4-(2-(4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl)-2-oxoethyl)piperidine-1-carboxamide
InChIKey: DHMTURDWPRKSOA-UHFFFAOYSA-N
SMILES: O=C(N1CCC(CC(N2CCC(C3C4=C(Br)C=C(Cl)C=C4CCC5=CC(Br)=CN=C53)CC2)=O)CC1)N
Biological Activity: (Rac)-Lonafarnib (Sch66336 racemate) is an isomer of Lonafarnib (HY-15136). Lonafarnib (Sch66336) is an orally active, blood-brain barrier penetrant farnesyltransferase (FPTase) inhibitor. Lonafarnib increases the phosphorylation levels of Akt, CaMKII and CREB, upregulates BDNF expression in the hippocampus, elevates the content of α7nAChR on cell membranes, and blocks the isoprenylation of H-Ras. Lonafarnib repairs synapses and reverses spatial memory deficits in Aβ1-42 model mice. Lonafarnib inhibits RSV fusion and replication, and alleviates virus-induced lung injury. Lonafarnib activates the lysosomal and autophagic pathways, and reduces the phosphorylation and aggregation of tau. Lonafarnib acts synergistically with Sorafenib (HY-10201) to promote apoptosis, and inhibits the proliferation and invasion of melanoma cells. Lonafarnib inhibits the farnesylation of progerin, repairs nuclear membrane defects, and activates the cGAS-STING-STAT1 signaling pathway. Lonafarnib can be used in research related to diseases including Alzheimer's disease, viral infections, melanoma, and progeria[1][2][3][4][5].
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(Rac)-Lonafarnib | (Rac)-Lonafarnib (Sch66336 racemate) is an isomer of Lonafarnib (HY-15136). Lonafarnib (Sch66336) is an orally active, blood-brain barrier penetrant farnesyltransferase (FPTase) inhibitor. Lonafarnib increases the phosphorylation levels of Akt, CaMKII and CREB, upregulates BDNF expression in the hippocampus, elevates the content of α7nAChR on cell membranes, and blocks the isoprenylation of H-Ras. Lonafarnib repairs synapses and reverses spatial memory deficits in Aβ1-42 model mice. Lonafarnib inhibits RSV fusion and replication, and alleviates virus-induced lung injury. Lonafarnib activates the lysosomal and autophagic pathways, and reduces the phosphorylation and aggregation of tau. Lonafarnib acts synergistically with Sorafenib (HY-10201) to promote apoptosis, and inhibits the proliferation and invasion of melanoma cells. Lonafarnib inhibits the farnesylation of progerin, repairs nuclear membrane defects, and activates the cGAS-STING-STAT1 signaling pathway. Lonafarnib can be used in research related to diseases including Alzheimer's disease, viral infections, melanoma, and progeria. | |||||||||||||||||||||
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- [1]. Cai C, et al. Ras Inhibitor Lonafarnib Rescues Structural and Functional Impairments of Synapses of Aβ Mice via α7nAChR-Dependent BDNF Upregulation. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2022 Aug 03;42(31):6090-6107. [Content Brief]
- [2]. Yang Q, et al. Farnesyltransferase inhibitor lonafarnib suppresses respiratory syncytial virus infection by blocking conformational change of fusion glycoprotein. Signal transduction and targeted therapy. 2024 Jun 10;9(1):144.
- [3]. Hernandez I, et al. A farnesyltransferase inhibitor activates lysosomes and reduces tau pathology in mice with tauopathy. Science translational medicine. 2019 Mar 27;11(485):eaat3005. [Content Brief]
- [4]. Niessner H, et al. The farnesyl transferase inhibitor lonafarnib inhibits mTOR signaling and enforces sorafenib-induced apoptosis in melanoma cells. The Journal of investigative dermatology. 2011 Feb;131(2):468-79.
- [5]. Arnold R, et al. Baricitinib, a JAK-STAT Inhibitor, Reduces the Cellular Toxicity of the Farnesyltransferase Inhibitor Lonafarnib in Progeria Cells. International journal of molecular sciences. 2021 Jul 12;22(14):7474.
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