Lonidamine
Based on 18 publication(s) in Google Scholar
Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (Ki: 2.5 μM). Lonidamine also inhibits aerobic glycolysis in cancer cells. Lonidamine can be used in the research of mitochondrial metabolism and inflammation, such as pulmonary fibrosis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.91%
- No. CAS: 50264-69-2
- Fòrmula: C15H10Cl2N2O2
- Peso molecular:321.16
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Lonidamine
More- Signal Transduct Target Ther. 2025 Sep 26;10(1):310. [Abstract]
- Cell Metab. 2022 Dec 6;34(12):1999-2017.e10. [Abstract]
- Cell Metab. 2022 Sep 6;34(9):1312-1324.e6. [Abstract]
- Cell Res. 2021 Sep;31(9):980-997. [Abstract]
- Cancer Res. 2025 Apr 28:OF1-OF13. [Abstract]
- ACS Nano. 2022 Jan 25;16(1):1182-1197. [Abstract]
- Cell Discov. 2020 Aug 18:6:56. [Abstract]
- Mol Cell. 2025 Mar 19:S1097-2765(25)00186-8. [Abstract]
- Aggregate. 2024 Jun 26.
- Adv Sci (Weinh). 2025 Aug;12(30):e02146. [Abstract]
- Biomaterials. 2026 Jan:324:123544. [Abstract]
- Phytomedicine. 2024 Apr:126:155426. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Food Biosci. 2026 Apr 29;80:108975.
- Commun Biol. 2025 Jun 2;8(1):845. [Abstract]
- Int Immunopharmacol. 2025 Oct 10:163:115258. [Abstract]
- Cell Signal. 2024 Jun:118:111126. [Abstract]
- Hong Kong Polytechnic University. 2025.
Customer Validation & Images
-
WB
-
IHC
-
WB
-
IF
-
RT-PCR
Ver todos los productos específicos de isoformas Parasite
More
Actividad biológica
|
Hexokinase 2 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
152.9 μM
Compound: LND
|
Antiproliferative activity against mouse 4T1 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
Antiproliferative activity against mouse 4T1 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
|
[PMID: 37376788] |
| 786-0 | IC50 |
120.43 μM
Compound: LND
|
Antiproliferative activity against human 786-0 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
Antiproliferative activity against human 786-0 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
|
[PMID: 37376788] |
| HGC-27 | IC50 |
77.62 μM
Compound: LND
|
Antiproliferative activity against human HGC-27 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
Antiproliferative activity against human HGC-27 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
|
[PMID: 37376788] |
| MCF7 | IC50 |
197.45 μM
Compound: LND
|
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
|
[PMID: 37376788] |
| PANC-1 | IC50 |
164.51 μM
Compound: LND
|
Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay
|
[PMID: 37376788] |
Lonidamine (100 μM, 24 h) inhibits TGF-β-stimulated lactate production and oxygen consumption rate in AKR-2B and TIG-1 cells[3].
Lonidamine (100 μM, 24/48 h) inhibits H2030BrM3 and A549 cell proliferation[4].
Lonidamine (100-200 μM, 24 h) inhibits H2030BrM3 and A549 cell invasion[4].
Lonidamine (100-1000 μM, 24 h) inhibits mitochondrial complex I and II activities[4].
Lonidamine (200 μM, 24 h) increases ROS generation in H2030BrM3 lung cancer cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Lonidamine (oral administration, 10-100 mg/kg/day, d10 to d20) improves lung function by inhibiting hexokinase 2 (HK2) activity in BLM-induced pulmonary fibrosis murine model[3].
-
Dosage:10, 30, 100 mg/kg/day
-
Administration:Oral administration, daily, d10 to d20 after BLM treatment.
-
Result:Partially or completely reversed the increases in HK2 and lactate induced by BLM and reduced the expression of 10 profibrotic mediators.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 50264-69-2
-
Appearance Solid
-
Peso molecular 321.16
-
Fòrmula C15H10Cl2N2O2
-
Color White to off-white
-
SMILES
O=C(C1=NN(CC2=CC=C(Cl)C=C2Cl)C3=C1C=CC=C3)O
-
Synonyms
AF-1890; Diclondazolic Acid; DICA
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (18)
-
Journal Impact Factor
-
Most Recent
-
Signal Transduct Target Ther
Reprogramming of cancer metabolism via photoresponsive nano-PROTAC enhances pyroptosis-mediated immunotherapy. [Abstract]2025 Sep 26;10(1):310. PMID: 40998785
Lonidamine purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Sep 26;10(1):310. [Abstract]
Lonidamine (1 μM; 3-24 h) treatment led to an initial reduction of the HK2 level in TNBC cells followed by eventual regeneration.
-
Cell Metab
Cancer cells co-opt nociceptive nerves to thrive in nutrient-poor environments and upon nutrient-starvation therapies. [Abstract]2022 Dec 6;34(12):1999-2017.e10. PMID: 36395769
Lonidamine purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):1999-2017.e10. [Abstract]
Combination treatment with Rimegepant and Lonidamine, Anlotinib, or Bevacizumab led to a reduced proportion of Ki67+ cancer cells, reduce LC3B puncta, and the accumulation of p62 puncta in cancer cells, indicating impaired cell proliferation and autophagic flux.
Lonidamine purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):1999-2017.e10. [Abstract]
Lonidamine (100 μM; 24 h) in vitro significantly increased NGF and Calca levels in Cal27 cells.
Lonidamine purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):1999-2017.e10. [Abstract]
Lonidamine (100 μM; 24 h) activated the JNK-c-Jun pathway in Cal27 cells.
-
Cell Metab
Aerobic glycolysis promotes tumor immune evasion by hexokinase2-mediated phosphorylation of IκBα. [Abstract]2022 Sep 6;34(9):1312-1324.e6. PMID: 36007522
Lonidamine purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Sep 6;34(9):1312-1324.e6. [Abstract]
Lonidamine (100 mg/kg; i.p.; every two days) treatment reduced HK2-mediated IkBα T291 phosphorylation and PD-L1 expression, accompanied by increased CD8+ T cell tumor infiltration and enhanced granzyme B expression in C57BL/6 mice.
Lonidamine purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Sep 6;34(9):1312-1324.e6. [Abstract]
Lonidamine (200 μM; 12 h) partially blocked the increase in PD-L1 expression induced by expression of activated EGFR variant III (EGFRvIII) mutant in LN229 GBM cells.
-
Cell Res
The metabolite α-KG induces GSDMC-dependent pyroptosis through death receptor 6-activated caspase-8. [Abstract]2021 Sep;31(9):980-997. PMID: 34012073 -
Cancer Res
Blocking the TCA Cycle in Cancer Cells Potentiates CD36+ T-cell-Mediated Antitumor Immunity by Suppressing ER Stress-Associated THBS2 Signaling. [Abstract]2025 Apr 28:OF1-OF13. PMID: 40293258 -
ACS Nano
Self-Delivery Ternary Bioregulators for Photodynamic Amplified Immunotherapy by Tumor Microenvironment Reprogramming. [Abstract]2022 Jan 25;16(1):1182-1197. PMID: 35023720 -
Cell Discov
2020 Aug 18:6:56. PMID: 32864161 -
Mol Cell
PI3Kβ functions as a protein kinase to promote cellular protein O-GlcNAcylation and acetyl-CoA production for tumor growth. [Abstract]2025 Mar 19:S1097-2765(25)00186-8. PMID: 40132583 -
-
Adv Sci (Weinh)
Inhibiting FAT1 Blocks Metabolic Bypass to Enhance Antitumor Efficacy of TCA Cycle Inhibition through Suppressing CPT1A-Dependent Fatty Acid Oxidation. [Abstract]2025 Aug;12(30):e02146. PMID: 40407216 -
Biomaterials
Disrupting tumor homeostasis with an autoamplificatory nanoinducer to augment pyroptosis for efficient immunotherapy. [Abstract]2026 Jan:324:123544. PMID: 40652803 -
Phytomedicine
2024 Apr:126:155426. PMID: 38367425 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
-
Commun Biol
Cathepsin B-dependent glycolysis contributes to reduced renal uric acid excretion in hyperuricemia. [Abstract]2025 Jun 2;8(1):845. PMID: 40457023 -
Int Immunopharmacol
Lonidamine alleviates inflammation and tissue remodeling in a mouse model of eosinophilic chronic sinusitis: A single-cell transcriptomics study. [Abstract]2025 Oct 10:163:115258. PMID: 40700828 -
Cell Signal
HK2 promotes migration and invasion of intrahepatic cholangiocarcinoma via enhancing cancer stem-like cells' resistance to anoikis. [Abstract]2024 Jun:118:111126. PMID: 38453126 -
Solvente y solubilidad
DMSO : 50 mg/mL (155.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (281 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. 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. [Content Brief]
[2]. Ilya A Shutkov, et al. Ru(III) Complexes with Lonidamine-Modified Ligands. Int J Mol Sci. 2021 Dec 15;22(24):13468. [Content Brief]
[3]. Xueqian Yin, et al. Hexokinase 2 couples glycolysis with the profibrotic actions of TGF-β. Sci Signal. 2019 Dec 17;12(612):eaax4067. [Content Brief]
[4]. Gang Cheng, et al. Targeting lonidamine to mitochondria mitigates lung tumorigenesis and brain metastasis. Nat Commun. 2019 May 17;10(1):2205. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1137 mL | 15.5686 mL | 31.1371 mL | 77.8428 mL |
| 5 mM | 0.6227 mL | 3.1137 mL | 6.2274 mL | 15.5686 mL | |
| 10 mM | 0.3114 mL | 1.5569 mL | 3.1137 mL | 7.7843 mL | |
| 15 mM | 0.2076 mL | 1.0379 mL | 2.0758 mL | 5.1895 mL | |
| 20 mM | 0.1557 mL | 0.7784 mL | 1.5569 mL | 3.8921 mL | |
| 25 mM | 0.1245 mL | 0.6227 mL | 1.2455 mL | 3.1137 mL | |
| 30 mM | 0.1038 mL | 0.5190 mL | 1.0379 mL | 2.5948 mL | |
| 40 mM | 0.0778 mL | 0.3892 mL | 0.7784 mL | 1.9461 mL | |
| 50 mM | 0.0623 mL | 0.3114 mL | 0.6227 mL | 1.5569 mL | |
| 60 mM | 0.0519 mL | 0.2595 mL | 0.5190 mL | 1.2974 mL | |
| 80 mM | 0.0389 mL | 0.1946 mL | 0.3892 mL | 0.9730 mL | |
| 100 mM | 0.0311 mL | 0.1557 mL | 0.3114 mL | 0.7784 mL |
Lonidamine Related Classifications
HY-B0486 Related Classifications
Powered by Bioz