Lonidamine (Synonyms: AF 1890, DICA, Diclondazolic Acid) |
Catalog No.GC11532
One-Click Copy Product Info
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Lonidamine is an inhibitor of hexokinase, mitochondrial pyruvate carrier (with a Ki of 2.5μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporter, and also inhibits mitochondrial complex II.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 50264-69-2
Sample solution is provided at 25 µL, 10mM.
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Lonidamine is an inhibitor of hexokinase, mitochondrial pyruvate carrier (with a Ki of 2.5μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporter, and also inhibits mitochondrial complex II [1]. Lonidamine is an anti-tumor drug that can inhibit aerobic glycolysis in cancer cells [2]. Lonidamine can be used in the research of mitochondrial metabolism and inflammation [3].
In vitro, Lonidamine (3, 10, and 30μM; 24h) treatment of IL-4, IL-13, and TNF-α-induced human nasal mucosal epithelial cells significantly and dose-dependently reduced the expression of CXCL1 and PTN, confirming its direct anti-inflammatory and anti-resorptive effects on nasal epithelial cells [4]. Lonidamine (150μM; 45min and 3h) treatment of human melanoma DB-1 cells significantly reduced NADH levels, the Fp redox ratio (Fp/(NADH + Fp)) increased, and mitochondrial redox capacity significantly decreased [5].
In vivo, Lonidamine (100mg/kg; ip) treatment for 2 hours significantly reduced the βNTP level in nude mice with DB-1 human melanoma. At the same time, the NTP levels in DB-1, HCC1806, BT-474, A2780 and LNCaP also decreased respectively [6]. Lonidamine (1, 3, and 10mg/kg/day for 11 days; i.g.) treatment alleviated the symptoms of chronic sinusitis mice, reduced sneezing, cytokine release, inflammatory cell infiltration, and goblet cell hyperplasia. Lonidamine inhibits inflammation by inhibiting the differentiation of inflammatory epithelial cells and neutrophils through Cxcl1-Cxcr2 [4].
References:
[1] Shutkov IA, Okulova YN, Tyurin VY, et al. Ru(III) Complexes with Lonidamine-Modified Ligands. Int J Mol Sci. 2021;22(24):13468.
[2] Nancolas B, et al. The anti-tumour agent lonidamine is a potent inhibitor of the mitochondrial pyruvate carrier and plasma membrane monocarboxylate transporters. Biochem J. 2016 Apr 1;473(7):929-36.
[3] Xueqian Yin, et al. Hexokinase 2 couples glycolysis with the profibrotic actions of TGF-β. Sci Signal. 2019 Dec 17;12(612):eaax4067.
[4] Liu J, Wu L, Wei H, et al. Lonidamine alleviates inflammation and tissue remodeling in a mouse model of eosinophilic chronic sinusitis: A single-cell transcriptomics study[J]. International Immunopharmacology, 2025, 163: 115258.
[5] Xu H N, Feng M, Nath K, et al. Optical redox imaging of lonidamine treatment response of melanoma cells and xenografts[J]. Molecular Imaging and Biology, 2019, 21(3): 426-435.
[6] Nath K, Nelson D S, Heitjan D F, et al. Lonidamine induces intracellular tumor acidification and ATP depletion in breast, prostate and ovarian cancer xenografts and potentiates response to doxorubicin[J]. NMR in Biomedicine, 2015, 28(3): 281-290.
| Cell experiment [1]: | |
Cell lines | DB-1 cell |
Preparation Method | For testing Lonidamine treatment response of cultured cells, DB-1 cells were expanded in phenol-red free RPMI 1640 complete medium. Suspended DB-1 cells (4 × 104, 200μl) were transferred to a 35-mm glass bottom dish (MatTek, MA) and incubated for 4h to allow cells to attach to the glass surface. Fresh medium (1 ml) was then added, and the dish was incubated for 20h. Approximately 1h before imaging, the medium was removed and the dish were rinsed twice with PBS (with Ca2+ and Mg2+) followed by adding 1ml live cell imaging solution (LCIS) spiked with 11mM glucose and 2mM glutamine. For the Lonidamine-treated group, the cells were treated with 150μM Lonidamine for 45min (0.8% or 0.2% DMSO in the glucose and glutamine-spiked LCIS). The control group was treated with 0.8% or 0.2% DMSO for 45min. |
Reaction Conditions | 150μM; 45min |
Applications | Lonidamine significantly reduced the NADH level in the cells, and the Fp redox ratio (Fp/(NADH + Fp)) increased, while the mitochondrial redox capacity was significantly decreased. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | C57BL/6 mice were housed in ventilated cages. All animal experiments were approved by the institutional animal care and use committee at the Zhejiang University Laboratory Animal Center. A mouse model of eosinophilic chronic sinusitis (ECRS) was established using intranasal papain administration (20μg in 20μL PBS) on Days 0–2 and 7–10 for a total of 7 doses, with controls receiving PBS. Treatment groups included gavage with Lonidamine (1, 3, or 10mg/kg), or intraperitoneal DEX (1mg/kg) daily for 11 days. Seventy-two mice (balanced for sex) were divided into six groups (n = 12 per group): control, ECRS, ECRS+ Lonidamine (1, 3, or 10mg/kg), and ECRS+DEX. No adverse effects were noted. Mice were anesthetized with isoflurane and euthanized using CO2 (30% vol/min). This study followed ethical guidelines for humane animal treatment. |
Dosage form | 1, 3, and 10mg/kg/day for 11 days; i.g. |
Applications | Lonidamine alleviated ECRS symptoms, reducing sneezing, cytokine release, inflammatory cell infiltration, and goblet cell hyperplasia. |
References: | |
| Cas No. | 50264-69-2 | SDF | |
| Synonyms | AF 1890, DICA, Diclondazolic Acid | ||
| Chemical Name | 1-[(2,4-dichlorophenyl)methyl]indazole-3-carboxylic acid | ||
| Canonical SMILES | C1=CC=C2C(=C1)C(=NN2CC3=C(C=C(C=C3)Cl)Cl)C(=O)O | ||
| Formula | C15H10Cl2N2O2 | M.Wt | 321.16 |
| Solubility | ≥ 11.1mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1137 mL | 15.5686 mL | 31.1371 mL |
| 5 mM | 622.7 μL | 3.1137 mL | 6.2274 mL |
| 10 mM | 311.4 μL | 1.5569 mL | 3.1137 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)