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Technical Data
| Formula | C15H10Cl2N2O2 |
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| Molecular Weight | 321.16 | CAS No. | 50264-69-2 | |
| Solubility (25°C)* | In vitro | DMSO | 64 mg/mL (199.27 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Lonidamine is an orally administered small molecule hexokinase inactivator. | |
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| In vitro | Lonidamine reduces the oxygen consumption in both normal and neoplastic cells, while it increases the aerobic glycolysis of normal cells but inhibited that of tumor cells. [1] Lonidamine induces the permeabilization of ANT proteoliposomes in a cell-free system, yet has no effect on protein-free liposomes. Lonidamine adds to synthetic planar lipid bilayers containing ANT, eliciting ANT channel activities with clearly distinct conductance levels. [2] Lonidamine provokes a disruption of the mitochondrial transmembrane potential which precedes signs of nuclear apoptosis and cytolysis. Lonidamine causes the dissipation of the mitochondrial inner transmembrane potential and the release of apoptogenic factors capable of inducing nuclear apoptosis in vitro. [3] Lonidamine (50 mg/mL) induces apoptosis in adriamycin and nitrosourea-resistant cells (MCF-7 ADR(r) human breast cancer cell line, and LB9 glioblastoma multiform cell line), as demonstrated by sub-G1 peaks in DNA content histograms, condensation of nuclear chromatin, and internucleosomal DNA fragmentation. [4] Lonidamine has a stronger effect on glioblastoma cell proliferation and metabolism in vitro than did either agent used alone. [5] |
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| In vivo | Lonidamine (160 mg/kg) combined with Diazepam is significantly more effective in reducing glioblastoma tumor growth than either drug alone in mice, this tumor growth retardation is maintained as long as treatment is given. [5] |
Protocol (from reference)
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References
Selleck's Lonidamine has been cited by 15 publications
| Targeting tumor-intrinsic SLC16A3 to enhance anti-PD-1 efficacy via tumor immune microenvironment reprogramming [ Cancer Lett, 2024, 589:216824] | PubMed: 38522774 |
| Targeting mitochondrial energetics reverses panobinostat- and marizomib-induced resistance in pediatric and adult high-grade gliomas [ Mol Oncol, 2023, 17(9):1821-1843] | PubMed: 37014128 |
| Targeting mitochondrial energetics reverses panobinostat- and marizomib-induced resistance in pediatric and adult high-grade gliomas [ Mol Oncol, 2023, 17(9):1821-1843] | PubMed: 37014128 |
| Metabolic Reprogramming by Ribitol Expands the Therapeutic Window of BETi JQ1 against Breast Cancer [ Cancers (Basel), 2023, 15(17)4356] | PubMed: 37686632 |
| Metabolic Reprogramming by Ribitol Expands the Therapeutic Window of BETi JQ1 against Breast Cancer [ Cancers (Basel), 2023, 15(17)4356] | PubMed: 37686632 |
| Microglial hexokinase 2 deficiency increases ATP generation through lipid metabolism leading to β-amyloid clearance [ Nat Metab, 2022, 4(10):1287-1305] | PubMed: 36203054 |
| Deregulation and epigenetic modification of BCL2-family genes cause resistance to venetoclax in hematologic malignancies [ Blood, 2022, blood.2021014304] | PubMed: 35704690 |
| Directly targeting ASC by lonidamine alleviates inflammasome-driven diseases [ J Neuroinflammation, 2022, 19(1):315] | PubMed: 36577999 |
| Membrane-associated RING-CH protein (MARCH8) is a novel glycolysis repressor targeted by miR-32 in colorectal cancer [ J Transl Med, 2022, 20(1):402] | PubMed: 36064706 |
| Hexokinase 2-mediated glycolysis promotes receptor activator of NF-κB ligand expression in Porphyromonas gingivalis lipopolysaccharide-treated osteoblasts [ J Periodontol, 2021, 10.1002/JPER.21-0227] | PubMed: 34585393 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.