Lonidamine (AF-1890) - Moligand™, 10mM in DMSO , Inhibitor of mitochondrial pyruvate carrier 1 like;Inhibitor of mitochondrial pyruvate carrier 2, CAS No.50264-69-2, Inhibitor of mitochondrial pyruvate carrier 1 like;Inhibitor of mitochondrial pyruvate carrier 2

CAS: 50264-69-2 Cat. No.: L409034 Peso molecular: 321.16 Número EC: 256-510-0

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Diclondazolic Acid, DICA | 1-​[(2,​4-​dichlorophenyl)​methyl]​-1H-​indazole-​3-​carboxylic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Lonidamine (AF-1890) Lonidamine (AF 1890, Diclondazolic Acid, DICA) is an orally administered small molecule hexokinase inactivator.
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. 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. 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. 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. Lonidamine has a stronger effect on glioblastoma cell proliferation and metabolism in vitro than did either agent used alone.

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.
Cell Data

cell lines：T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, LNCaP, etc.

Concentrations：

Incubation Time：

Powder Purity:≥97%

Specifications

Sinónimos

Diclondazolic Acid, DICA | 1-​[(2, ​4-​dichlorophenyl)​methyl]​-1H-​indazole-​3-​carboxylic acid

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Lonidamine (AF 1890, Diclondazolic Acid, DICA) is an orally administered small molecule hexokinase inactivator.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of mitochondrial pyruvate carrier 1 like;Inhibitor of mitochondrial pyruvate carrier 2

Nombres e identificadores

• Isómeros SMILES: C1=CC=C2C(=C1)C(=NN2CC3=C(C=C(C=C3)Cl)Cl)C(=O)O
• WGK Alemania: 3
• CAS alternativo: 50264-69-2
• Número NSC: 741419
• Términos de entrada MeSH: 1-(2,4-dichlorobenzyl)indazole-3-carboxylic acid;AF 1890;diclondazolic acid;lonidamine
• Peso molecular: 321.16
• Reaxy-Rn: 894483
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=894483&ln=

Objetivos asociados (humanos)

MPC2 Tbio Mitochondrial pyruvate carrier 2 (0 Activities)

Discover Target: MPC2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MPC1L Tdark Mitochondrial pyruvate carrier 1-like protein (0 Activities)

Discover Target: MPC1L

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro
• Punto de fusión (°C): 210 °C

Referencias

1. Junya Lu, Shuaipeng Feng, Zhu Liu, Yan Xiao, Hui Zhang, Siling Wang, Qinfu Zhao.  (2025)  Co-delivery of copper chelators and glycolytic inhibitors to disrupt glucose metabolism and inhibit tumor metastasis.  CHEMICAL ENGINEERING JOURNAL,      [PMID:] [10.1016/j.cej.2025.165899]

2. Yimei Zhang, Chen Yuan, Wenwen Yang, Dianyong Tang, Zhongzhu Chen, Zheng Huang.  (2025)  Lonidamine dimer-based nanomedicine for overcoming multidrug resistance by manipulating energy metabolism and disrupting redox homeostasis.  NEW JOURNAL OF CHEMISTRY,      [PMID:] [10.1039/D5NJ02765A]

3. Chen Huan, Li Ting, Liu Zhiyong, Tang Shuwan, Tong Jintao, Tao Yingfang, Zhao Zinan, Li Nan, Mao Chun, Shen Jian, Wan Mimi.  (2023)  A nitric-oxide driven chemotactic nanomotor for enhanced immunotherapy of glioblastoma.  Nature Communications,  14  (1): (1-21).  [PMID:36804924] [10.1038/s41467-022-35709-0]

4. Lu Yang, Junnan Li, Zhaoyuan Guan, Jingwen Zhang, Xin Wang, Rupei Tang.  (2022)  Carrier-free prodrug nanoparticles based on lonidamine and cisplatin for synergistic treatment of breast cancer.  JOURNAL OF BIOMATERIALS APPLICATIONS,      [PMID:35689328] [10.1177/08853282221107951]

5. Jia-Qi Huang, Lin-Ping Zhao, Xiang Zhou, Ling-Shan Liu, Rong-Rong Zheng, Fu-An Deng, Yi-Bin Liu, Xi-Yong Yu, Shi-Ying Li, Hong Cheng.  (2022)  Carrier Free O2-Economizer for Photodynamic Therapy Against Hypoxic Tumor by Inhibiting Cell Respiration.  Small,  18  (15): (2107467).  [PMID:35224854] [10.1002/smll.202107467]

6. Can Wu, Chunlu Wang, Yaoyao Zheng, Yaxin Zheng, Ziqi Liu, Keming Xu, Wenying Zhong.  (2021)  Triple Enzyme-Regulated Molecular Hydrogels for Carrier-Free Delivery of Lonidamine.  ADVANCED FUNCTIONAL MATERIALS,  31  (42): (2104418).  [PMID:] [10.1002/adfm.202104418]

7. Caixia Yue, Yuming Yang, Jie Song, Gabriel Alfranca, Chunlei Zhang, Qian Zhang, Ting Yin, Fei Pan, Jesús M. de la Fuente, Daxiang Cui.  (2017)  Mitochondria-targeting near-infrared light-triggered thermosensitive liposomes for localized photothermal and photodynamic ablation of tumors combined with chemotherapy.  Nanoscale,  9  (31): (11103-11118).  [PMID:28741634] [10.1039/C7NR02193C]

8. Weiguo Song, Hekai Yang, Ying Wang, Shuzhen Chen, Wenda Zhong, Qian Wang, Wenshuo Ding, Guangzhao Xu, Chen Meng, Ying Liang, Zhe-Sheng Chen, Shuhua Cao, Liuya Wei, Fahui Li.  (2024)  Glutathione-Sensitive Photosensitizer–Drug Conjugates Target the Mitochondria to Overcome Multi-Drug Resistance in Cancer.  Advanced Science,      [PMID:38898730] [10.1002/advs.202307765]

9. Haibin Lu, Weifang Tong, Meixu Jiang, Huimin Liu, Chen Meng, Kai Wang, Xupeng Mu.  (2024)  Mitochondria-Targeted Multifunctional Nanoprodrugs by Inhibiting Metabolic Reprogramming for Combating Cisplatin-Resistant Lung Cancer.  ACS Nano,      [PMID:39088743] [10.1021/acsnano.4c04024]

10. Yimei Zhang, Shiyi Xiang, Yayi Wu, Can Yang, Dianyong Tang, Zhongzhu Chen, Zheng Huang.  (2024)  Novel co-delivery nanomedicine for photodynamic enlarged immunotherapy by cascade immune activation and efficient Immunosuppression reversion.  BIOORGANIC CHEMISTRY,      [PMID:39577155] [10.1016/j.bioorg.2024.107978]

11. Jinchao Zhao, Lei Lei, Wenbin Dai, Angfeng Jiang, Qiao Jin, Zhe Tang.  (2024)  Simultaneous inhibition of heat shock proteins and autophagy enhances radiofrequency ablation of hepatocellular carcinoma.  Biomaterials Science,      [PMID:39429155] [10.1039/D4BM01190B]

12. Yingying Zhao, Beibei Zhang, Shaobo Duan, Yaqiong Li, Yuzhou Wang, Yongchao Wang, Juan Zhang, Rong Huang, Ru Jiang, Rui Zhang, Qi Zhou, Linlin Zhang, Xiaoxia Xu, Zesheng Li, Si Chen, Lianfeng Mo, Xu Zhang, Siyi Yang, Xiguo Cai, Lianzhong Zhang.  (2025)  An ultrasound-visualized methionine partitioning nano-modulator for enhanced immunotherapy against anti-PD-1 resistant tumors.  CHEMICAL ENGINEERING JOURNAL,      [PMID:] [10.1016/j.cej.2025.165409]

13. Fangrong Tan, Yuandong Zeng, Donghua Dong, Yan Deng, Zhe Tang, LinGe Wang, Qianqian Yu.  (2025)  GSH-Responsive Prodrug Polymersomes for Copper-Free Cuproptosis and Synergistic Photothermal Cancer Therapy.  BIOMACROMOLECULES,      [PMID:41412815] [10.1021/acs.biomac.5c01893]

14. Jing Zuo, Yichun Huang, Hailong Tian, Siyuan Qin, Yonghao Yan, Han Yan, Yining Jiang, Lei Li, Shiqi Wang, Yongfeng Jia, Yuan Zhao, Canhua Huang.  (2026)  H-ferritin engineered nanoplatform reprograms metabolism and immunity for glioblastoma immunotherapy.  JOURNAL OF CONTROLLED RELEASE,      [PMID:41506381] [10.1016/j.jconrel.2026.114613]

15. Qianhua Feng, Yiwei Li, Liying Sun, Jia Zhang, Lisha Shou, Jieyu Zhu, Huimin Zhou, Bingqian Si, Xinyu Gu, Chunlei Du, Zhenzhong Zhang, Lei Wang.  (2026)  Probiotic Spore-Based Oral Biotherapeutics Promote Brain Targeting toward Gut-Brain Dual-Regulation for Parkinson’s Disease Treatment.  ACS Nano,      [PMID:41757540] [10.1021/acsnano.5c17340]