Galloflavin (Synonyms: NSC 107022) |
Catalog No.GC16816
One-Click Copy Product Info
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Galloflavin is a Lactate Dehydrogenase (LDH) inhibitor with IC50 values of 201µM and 200µM for LDH-A and LDH-B, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 568-80-9
Sample solution is provided at 25 µL, 10mM.
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Galloflavin is a Lactate Dehydrogenase (LDH) inhibitor with IC50 values of 201µM and 200µM for LDH-A and LDH-B, respectively[1]. Galloflavin induces the deacetylation of Sirtuin 6 and activates the activity of Sirtuin 6, with an EC50 value is 79µM[2]. Ascomycin inhibits the enzymatic activity of LDH-A by occupying the NADH site, prevents the binding of LDH-A to single-stranded DNA, and impairs RNA synthesis in cultured cells[3]. Galloflavin has been widely used in tumor research to inhibit lactate production and to suppress the growth of cancer cells[4].
In vitro, Galloflavin treatment for 72 hours markedly suppressed the proliferation of ECC-1 and Ishikawa cells, with IC50 values of 25µM and 43µM, respectively[5]. Treatment with 150µM Galloflavin for24 hours significantly reduced the viability of MCF-7 cells, decreased ATP production, and down-regulated the expression of ERα mRNA[6]. The 6-hour pre-treatment with 16µM Galloflavin inhibited the glycolytic activity in RAW264.7 cells stimulated by 200ng/ml lipopolysaccharide (LPS) and reduced the expression of IL-6, TNF-α, MCP-1, iNOS, and CD86[7].
In vivo, Galloflavin treatment via intraperitoneal injection at a dose of 80mg/kg/day dose for 5 days alleviated liver injury in the acute liver failure mouse model and increased survival rate[8]. Intraperitoneal injection of Galloflavin at a dose of 15mg/kg/day daily for 15 consecutive days inhibited tumor growth and reduced the expression of NLRP3, c-Myc, and P21 within tumors in the SW480 xenograft mouse model[9].
References:[1] Manerba M, Vettraino M, Fiume L, et al. Galloflavin (CAS 568‐80‐9): a novel inhibitor of lactate dehydrogenase[J]. ChemMedChem, 2012, 7(2): 311-317.
[2] Rahnasto-Rilla M, Järvenpää J, Huovinen M, et al. Effects of galloflavin and ellagic acid on sirtuin 6 and its anti-tumorigenic activities[J]. Biomedicine & Pharmacotherapy, 2020, 131: 110701.
[3] Fiume L, Vettraino M, Carnicelli D, et al. Galloflavin prevents the binding of lactate dehydrogenase A to single stranded DNA and inhibits RNA synthesis in cultured cells[J]. Biochemical and biophysical research communications, 2013, 430(2): 466-469.
[4] Vettraino M, Manerba M, Govoni M, et al. Galloflavin suppresses lactate dehydrogenase activity and causes MYC downregulation in Burkitt lymphoma cells through NAD/NADH-dependent inhibition of sirtuin-1[J]. Anti-cancer drugs, 2013, 24(8): 862-870.
[5] Han X, Sheng X, Jones H M, et al. Evaluation of the anti-tumor effects of lactate dehydrogenase inhibitor galloflavin in endometrial cancer cells[J]. Journal of hematology & oncology, 2015, 8(1): 2.
[6] Farabegoli F, Vettraino M, Manerba M, et al. Galloflavin, a new lactate dehydrogenase inhibitor, induces the death of human breast cancer cells with different glycolytic attitude by affecting distinct signaling pathways[J]. European Journal of Pharmaceutical Sciences, 2012, 47(4): 729-738.
[7] Wei J, Chen X, Wang Z, et al. Galloflavin mitigates acute kidney injury by suppressing LDHA-dependent macrophage glycolysis[J]. International Immunopharmacology, 2025, 150: 114265.
[8] Ferriero R, Nusco E, De Cegli R, et al. Pyruvate dehydrogenase complex and lactate dehydrogenase are targets for therapy of acute liver failure[J]. Journal of Hepatology, 2018, 69(2): 325-335.
[9] Guo L, Yang Y, Sheng Y, et al. Galloflavin relieves the Malignant behavior of colorectal cancer cells in the inflammatory tumor microenvironment[J]. Frontiers in Pharmacology, 2021, 12: 752118.
| Cell experiment [1]: | |
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Cell lines |
MCF-7 cells |
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Preparation Method |
MCF-7 cells were cultured in DMEM medium, supplemented with 10% fetal bovine serum (FBS), 100U/ml penicillin, 100μg/ml streptomycin, 2mM glutamine, and 1mM sodium pyruvate at 37°C in an incubator with 5% CO2. Cells (1×104/well) were seeded in 96-well plates, allowed to adhere overnight, and treated for 24h at 37°C with different concentrations of Galloflavin (0, 5, 10, 50, 100, 150, 200, and 150µM), the cell proliferation was tested. |
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Reaction Conditions |
0, 5, 10, 50, 100, 150, 200, and 150µM; 24h |
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Applications |
Galloflavin treatment reduced cell proliferation of MCF-7 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Nude mice |
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Preparation Method |
Nude mice (5 weeks old; 19-23g) were housed in SPF conditions with an automatic 12h/12h light-dark cycle at a constant temperature (21±1°C). SW480 cells were cultured to the logarithmic phase and digested, followed by the adjustment of cell concentration to 3×107/ml. Afterward, 0.2ml cell suspension (6×106 cells) was injected into the right hind limb after disinfection. Nodules appeared at the injection site within 3-4 days. Mice were subsequently divided into control and Galloflavin groups. Mice in the Galloflavin group were administered 15mg/kg Galloflavin (i.p.) once daily. Mice were kept for 15 days and sacrificed by carbon dioxide asphyxiation, followed by tumor resection and measurement of tumor volume. |
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Dosage form |
15mg/kg/day; 15 days; i.p. |
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Applications |
Galloflavin treatment reduced tumor growth in the SW480 xenograft mouse model. |
| References: [1] Farabegoli F, Vettraino M, Manerba M, et al. Galloflavin, a new lactate dehydrogenase inhibitor, induces the death of human breast cancer cells with different glycolytic attitude by affecting distinct signaling pathways[J]. European Journal of Pharmaceutical Sciences, 2012, 47(4): 729-738. [2] Guo L, Yang Y, Sheng Y, et al. Galloflavin relieves the Malignant behavior of colorectal cancer cells in the inflammatory tumor microenvironment[J]. Frontiers in Pharmacology, 2021, 12: 752118. | |
| Cas No. | 568-80-9 | SDF | |
| Synonyms | NSC 107022 | ||
| Formula | C12H6O8 | M.Wt | 278.2 |
| Solubility | DMSO: 5 mg/mL | 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 | 3.5945 mL | 17.9727 mL | 35.9454 mL |
| 5 mM | 718.9 μL | 3.5945 mL | 7.1891 mL |
| 10 mM | 359.5 μL | 1.7973 mL | 3.5945 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)