(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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 193275-86-4
- 分子式: C27H31Br2ClN4O2
- 分子量:638.82
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
|
STAT1 |
Bcl-2 |
H-Ras |
Akt |
体外実験
Lonafarnib inhibits RSV A2 infection in HEp-2 cells via a farnesyltransferase-independent mechanism[2].
Lonafarnib (3.3 μM; pre (-2-0 h), during (0-2 h), and post (2-16 h) infection) blocks RSV A2 infection in HEp-2 cells primarily by inhibiting the viral entry process, with significant inhibitory effects observed during the 0-2 h entry window or over the full −2-22 h period[2].
Lonafarnib inhibits RSV entry into HEp-2 cells and suppresses RSV F-induced intercellular fusion in HEK293T cells, confirming that it targets the RSV membrane fusion process[2].
Lonafarnib (0.1-0.5 μM; 48 h) stimulates endosomal microautophagy in NIH3T3 mouse fibroblasts, promoting the transport of substrates to late endosomal compartments and their degradation[3].
Lonafarnib (10 μM; 9 days) reduces the level of phosphorylated tau (Thr181) in wild-type and MAPTR406W mutant human induced pluripotent stem cell-derived neurons[3].
Lonafarnib (5 μM; 48-72 h) combined with 4 μM Sorafenib (HY-10201) synergistically suppresses the proliferation of BLM, MV3, MEWO and SKMel1 human metastatic melanoma cell lines, strengthens growth inhibition on primary melanoma cells derived from human skin metastases and reduces BLM cell viability[4].
Lonafarnib (5 μM; 24 h) inhibits the mTOR pathway in human metastatic melanoma cells. When combined with Sorafenib, it significantly downregulates intracellular Bcl-2, completely eliminates Mcl-1, and only slightly alters Bcl-xL expression[4].
Lonafarnib (3 μM; 14 days) reduces the invasion and proliferation of BL melanoma cells in organotypic skin models, and the combination with 2 μM Sorafenib completely blocks the invasion and proliferation of these cells[4].
Lonafarnib (5 μM; 24 h) combined with Sorafenib triggers typical apoptotic morphological features such as cell fragmentation in human metastatic melanoma BLM cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
CAS 番号 193275-86-4
-
分子量 638.82
-
分子式 C27H31Br2ClN4O2
-
SMILES
O=C(N1CCC(CC(N2CCC(C3C4=C(Br)C=C(Cl)C=C4CCC5=CC(Br)=CN=C53)CC2)=O)CC1)N
-
別名
Sch66336 racemate
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
(Rac)-Lonafarnib 関連分類
HY-15136B 関連分類
Powered by Bioz
Keywords
- (Rac)-Lonafarnib
- 193275-86-4
- Sch66336
- Sch 66336
- Sch-66336
- Farnesyl Transferase
- Tau Protein
- RSV
- Akt
- Ras
- Bcl-2 Family
- STAT
- nAChR
- Apoptosis
- Autophagy
- Drug Isomer
- Ftase
- Respiratory syncytial virus
- PKB
- Protein kinase B
- Nicotinic acetylcholine receptors
- α7nAChR
- tau inclusions
- Hutchinson-Gilford progeria syndrome
- Alzheimer’s disease
- Aβ1-42 mice
- farnesyltransferase
- respiratory syncytial virus
- melanoma
- HEp-2 cells
- hippocampal BDNF
- Inhibitor
- inhibitor
- inhibit