Art. -Nr.: HY-B0486

Lonidamine

(Synonyms: AF-1890; Diclondazolic Acid; DICA)

18 Cited Publications

Kundenbewertung

Based on 18 publication(s) in Google Scholar

Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (K_i: 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.

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Reinheit: 99.91%
CAS. Nr.: 50264-69-2
Formel: C₁₅H₁₀Cl₂N₂O₂
Molecular Weight:321.16

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Lonidamine Chemical Structure

CAS. Nr.: 50264-69-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (18)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Hexokinase 2

Alle Parasite Isoform-spezifische Produkte anzeigen :

Cellular Effect

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]

In Vitro

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.

In Vivo

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].

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 50264-69-2
Appearance Solid
Molecular Weight 321.16
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (18)

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Journal Impact Factor

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
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
ACS Nano

Self-Delivery Ternary Bioregulators for Photodynamic Amplified Immunotherapy by Tumor Microenvironment Reprogramming. [Abstract]

2022 Jan 25;16(1):1182-1197. PMID: 35023720
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 May 23:e02146. PMID: 40407216
Aggregate

2024 Jun 26.
Biomaterials

Disrupting tumor homeostasis with an autoamplificatory nanoinducer to augment pyroptosis for efficient immunotherapy. [Abstract]

2026 Jan:324:123544. PMID: 40652803
Cell Discov

A bioenergetic shift is required for spermatogonial differentiation. [Abstract]

2020 Aug 18;6:56. PMID: 32864161
Phytomedicine

Oridonin inhibits bladder cancer survival and immune escape by covalently targeting HK1. [Abstract]

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
Food Biosci

2026 Apr 29;80:108975.
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 Jul 22:163:115258. 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
Hong Kong Polytechnic University

2025.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1137 mL

15.5686 mL

31.1371 mL

5 mM

0.6227 mL

3.1137 mL

6.2274 mL

10 mM

0.3114 mL

1.5569 mL

3.1137 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (301 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

18 Cited Publications

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Lonidamine

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Publications Citing Use of MedChemExpress (MCE) Lonidamine

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lonidamine Related Classifications

HY-B0486 Related Classifications