Lonidamine - ≥99%, high purity , CAS No.50264-69-2, Inhibitor of mitochondrial pyruvate carrier 1 like;Inhibitor of mitochondrial pyruvate carrier 2

Item Number
L129342
Grouped product items
SKUSizeAvailabilityPrice Qty
L129342-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$64.90
L129342-25mg
25mg
In stock
$292.90
L129342-100mg
100mg
In stock
$1,053.90
L129342-250mg
250mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$2,369.90
L129342-1g
1g
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$8,529.90
L129342-5g
5g
In stock
$38,381.90

Hexokinase inhibitor

Basic Description

SynonymsAF-1890;Diclondazolic Acid;DICA | AM20060642 | CCG-204803 | A929099 | KN-228 | Lopac-L-4900 | Diclondazolic acid | HMS3412P05 | L 4900 | NCGC00015609-09 | Pharmakon1600-01503225 | WDRYRZXSPDWGEB-UHFFFAOYSA-N | 1-(2,4-dichlorobenzyl)indazole-3-carboxylic a
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsInhibits the energy metabolism of neoplastic cells by interfering with hexokinase and disrupting uncoupler-stimulated mitochondrial electron transport; damages cell and mitochondrial membranes.
Storage TempStore at -20°C,Argon charged
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of mitochondrial pyruvate carrier 1 like;Inhibitor of mitochondrial pyruvate carrier 2
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Product Describtion:

Lonidamine is an indazole compound that has been reported to inhibit angiogenic-related endothelial cell functions. This compound has been found to trigger apoptosis in endothelial cells and cause a decrease in proliferation, migration, invasion, and morphogenesis. The apoptotic effects of Lonidamine have been demonstrated to be due to Bax, Bid, caspase-3, and caspase-9 activation, as well as cytochrome c release. Futher studies show that Lonidamine prevents cellular energy metabolism via HXK (hexokinase) inhibition. This compound also blocks CFTR Cl- channels in vitro.
It elicits cell apoptosis and blocks CFTR Cl- channel.

Associated Targets(Human)

MPC2 Tbio Mitochondrial pyruvate carrier 2 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MPC1L Tdark Mitochondrial pyruvate carrier 1-like protein (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ESR1 Tclin Estrogen receptor alpha (17718 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NR3C1 Tclin Glucocorticoid receptor (14987 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PGR Tclin Progesterone receptor (8562 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AR Tclin Androgen Receptor (11781 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
VDR Tclin Vitamin D receptor (26531 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GABRA1 Tclin GABA receptor alpha-1 subunit (399 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TSHR Tclin Thyroid stimulating hormone receptor (29986 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AVPR2 Tclin Vasopressin V2 receptor (2912 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PPARG Tclin Peroxisome proliferator-activated receptor gamma (15191 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC29A1 Tclin Equilibrative nucleoside transporter 1 (1711 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2B Tclin Alpha-2b adrenergic receptor (4412 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2C Tclin Alpha-2c adrenergic receptor (4876 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EDNRA Tclin Endothelin receptor ET-A (5008 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA2A Tclin Adenosine A2a receptor (16305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA3 Tchem Adenosine A3 receptor (15931 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BDKRB2 Tclin Bradykinin B2 receptor (3970 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HRH3 Tclin Histamine H3 receptor (10389 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

ampC Beta-lactamase AmpC (62480 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Npy1r Neuropeptide Y receptor type 1 (8 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Cckar Cholecystokinin A receptor (90 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Pde4d Phosphodiesterase 4D (4 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Saccharomyces cerevisiae (19171 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Plasmodium falciparum (966862 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Leishmania donovani (89745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Trypanosoma cruzi (99888 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Trypanosoma brucei rhodesiense (7991 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Npsr1 Neuropeptide S receptor (260 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Luciferin 4-monooxygenase (66902 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Txnrd1 Thioredoxin reductase 1, cytoplasmic (45279 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Nfe2l2 Nuclear factor erythroid 2-related factor 2 (214 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rorc Nuclear receptor ROR-gamma (89407 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NS1 Nonstructural protein 1 (33327 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
LAP M17 leucyl aminopeptidase (931 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 1-[(2,4-dichlorophenyl)methyl]indazole-3-carboxylic acid
INCHI InChI=1S/C15H10Cl2N2O2/c16-10-6-5-9(12(17)7-10)8-19-13-4-2-1-3-11(13)14(18-19)15(20)21/h1-7H,8H2,(H,20,21)
InChi Key WDRYRZXSPDWGEB-UHFFFAOYSA-N
Canonical SMILES C1=CC=C2C(=C1)C(=NN2CC3=C(C=C(C=C3)Cl)Cl)C(=O)O
Isomeric SMILES C1=CC=C2C(=C1)C(=NN2CC3=C(C=C(C=C3)Cl)Cl)C(=O)O
WGK Germany 3
Alternate CAS 50264-69-2
PubChem CID 39562
NSC Number 741419
MeSH Entry Terms 1-(2,4-dichlorobenzyl)indazole-3-carboxylic acid;AF 1890;diclondazolic acid;lonidamine
Molecular Weight 321.16

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

11 results found

Lot NumberCertificate TypeDateItem
G2228751Certificate of AnalysisJun 11, 2024 L129342
H1808094Certificate of AnalysisJan 17, 2024 L129342
H1808092Certificate of AnalysisJan 17, 2024 L129342
C23211020Certificate of AnalysisJun 12, 2022 L129342
C23211021Certificate of AnalysisJun 12, 2022 L129342
C23241044Certificate of AnalysisJun 12, 2022 L129342
G2228358Certificate of AnalysisJun 12, 2022 L129342
G2228363Certificate of AnalysisJun 12, 2022 L129342
J2311063Certificate of AnalysisJun 12, 2022 L129342
J2327073Certificate of AnalysisJun 12, 2022 L129342
D1607152Certificate of AnalysisJan 19, 2022 L129342

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Chemical and Physical Properties

SolubilitySoluble in ethanol (5 mM), DMSO (100 mM), CHCl3/MeOH 1/1 (9.80-10.20 mg/ml), water (<1 mg/ml at 25° C), DMSO (64 mg/ml at 25° C), and ethanol (<1 mg/ml at 25° C).
SensitivityAir Sensitive
Melt Point(°C)210 °C

Safety and Hazards(GHS)

Pictogram(s) GHS08,   GHS07
Signal Danger
Hazard Statements

H351:Suspected of causing cancer

H302:Harmful if swallowed

H360:May damage fertility or the unborn child

Precautionary Statements

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P270:Do not eat, drink or smoke when using this product.

P330:Rinse mouth.

P203:Obtain, read and follow all safety instructions before use.

P301+P317:IF SWALLOWED: Get medical help.

P318:if exposed or concerned, get medical advice.

WGK Germany 3

Related Documents

Citations of This Product

1. 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]
2. 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]
3. 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]
4. 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]
5. 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,  (31): (11103-11118).  [PMID:28741634] [10.1039/C7NR02193C]

References

1. 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]
2. 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]
3. 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]
4. 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]
5. 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,  (31): (11103-11118).  [PMID:28741634] [10.1039/C7NR02193C]

Solution Calculators