| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Galloflavin targets lactate dehydrogenase (LDH), a key enzyme in glycolysis that catalyzes the conversion of pyruvate to lactate. By inhibiting LDH, galloflavin blocks glycolysis and reduces ATP production in cancer cells, which are highly dependent on glycolysis for energy (Warburg effect). The compound inhibits both LDH-A and LDH-B isoforms, with higher potency against LDH-A. This mechanism makes galloflavin a potential anticancer agent, particularly for cancers with high glycolytic activity.
|
|---|---|
| ln Vitro |
Pentaflavin participates in several signaling pathways that control metabolism, cell cycle, apoptosis, cell stress, and metastasis, hence successfully inhibiting cell growth in endometrial cancer cell lines and human endometrial cancer primary cultures [3].
In vitro, galloflavin has been shown to inhibit cell growth in endometrial cancer cell lines and primary cultures of human endometrial cancer. The compound inhibits LDH activity and reduces ATP production in cancer cells, leading to cell death. Galloflavin also inhibits SW480 cell viability and migration in inflammatory microenvironments. In B16 and A375 melanoma cells, galloflavin induces cell death through involvement in multiple signaling pathways that regulate metabolism, cell cycle, apoptosis, cell stress, and metastasis. |
| ln Vivo |
In vivo, galloflavin has been shown to significantly inhibit tumor growth in tumor xenograft-bearing mice. Administration of galloflavin at 5 or 15 mg/kg for 15 days resulted in time-dependent inhibition of tumor growth and tumor volume. Protein analysis revealed that galloflavin inhibits NLRP3 expression, as well as c-Myc and P21 expression. These in vivo studies support the potential of galloflavin as an anticancer agent.
|
| Enzyme Assay |
The in vitro enzyme inhibition assay for galloflavin measures its ability to inhibit LDH enzymatic activity. The assay is performed using purified LDH-A or LDH-B enzymes and substrates (pyruvate and NADH). The reaction is monitored by measuring the decrease in absorbance at 340 nm due to NADH oxidation. Ki values are calculated from dose-response curves and Lineweaver-Burk plots. Selectivity is assessed by testing the compound against other dehydrogenases or related enzymes.
|
| Cell Assay |
In vitro cellular studies are conducted using various cancer cell lines including endometrial cancer, melanoma, and SW480 cells. Cells are treated with galloflavin at various concentrations (typically 5-15 μM) for defined time periods. Cell viability is assessed using MTT or CellTiter-Glo assays. Cell migration and invasion are measured by wound healing and transwell assays. LDH activity is measured in cell lysates. ATP levels are measured using luminescence-based assays. Apoptosis is assessed by measuring caspase activity or Annexin V staining.
|
| Animal Protocol |
In vivo animal experiments are performed using tumor xenograft models in mice. Tumor-bearing mice are administered galloflavin at doses of 5 or 15 mg/kg for 15 days via intraperitoneal injection. Tumor volume is measured over time, and tumors are excised for analysis. Protein expression (NLRP3, c-Myc, P21) is measured by Western blot in tumor tissues. Body weight and general health are monitored throughout the study.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of galloflavin include solubility in DMSO. The compound has a molecular weight of 278.17 g/mol, molecular formula C12H6O8, and density of 2.10 g/cm³ (predicted). Storage at -20°C for powder is recommended. The compound should be protected from light and moisture. It appears as a yellow solid. Purity is typically ≥98%.
|
| Toxicity/Toxicokinetics |
Toxicological data for galloflavin are derived from preclinical studies. The compound is for research use only and not intended for human therapeutic applications. No significant toxicity has been reported at effective doses in animal studies. Standard safety precautions should be followed when handling the compound. Long-term toxicity and carcinogenicity studies have not been conducted.
|
| References |
|
| Additional Infomation |
Galloflavin is also known as NSC 107022 and 培黄素 (Chinese name). It is a lactate dehydrogenase inhibitor that inhibits both LDH-A and LDH-B isoforms with Ki values of 5.46 μM and 15.06 μM, respectively. Galloflavin hinders cancer cell proliferation by blocking glycolysis and ATP production. The compound has shown efficacy in endometrial cancer, melanoma, and other cancer models. It is used in cancer research to study the role of glycolysis in tumor metabolism and to develop novel anticancer therapies.
|
| Molecular Formula |
C12H6O8
|
|---|---|
| Molecular Weight |
278.1712
|
| Exact Mass |
278.006
|
| CAS # |
568-80-9
|
| Related CAS # |
568-80-9 (free acid);1780260-20-9 (potassium) |
| PubChem CID |
135483971
|
| Appearance |
Brown to breen solid powder
|
| Density |
2.1g/cm3
|
| Boiling Point |
159.8ºC at 760 mmHg
|
| Flash Point |
37.4ºC
|
| Index of Refraction |
1.848
|
| LogP |
0.721
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
20
|
| Complexity |
729
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O1C(C2=C([H])C(C(=C(C2=C2C1=C([H])C(=C(O[H])O2)O[H])O[H])O[H])=O)=O
|
| InChi Key |
UXHISTVMLJLECY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H6O8/c13-4-1-3-7(9(16)8(4)15)10-6(19-11(3)17)2-5(14)12(18)20-10/h1-2,14-16,18H
|
| Chemical Name |
2,3,9,10-tetrahydroxypyrano[3,2-c]isochromene-6,8-dione
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~35.95 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5949 mL | 17.9746 mL | 35.9492 mL | |
| 5 mM | 0.7190 mL | 3.5949 mL | 7.1898 mL | |
| 10 mM | 0.3595 mL | 1.7975 mL | 3.5949 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
