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Galloflavin LDH inhibitor

Cat.No.S9606

Galloflavin (NSC 107022) is a novel inhibitor of lactate dehydrogenasee (LDH) with Ki values of 5.46 μM and 15.06 μM for LDH-A and LDH-B, respectively.
Galloflavin LDH inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 278.17

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Quality Control

Batch: S960601 DMSO]2 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.21%
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  • NMR
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99.21

Solubility

In vitro
Batch:

DMSO : 2 mg/mL (7.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
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In vivo Formulation Calculator (Clear solution)

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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 ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 278.17 Formula

C12H6O8

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 568-80-9 -- Storage of Stock Solutions

Synonyms N/A Smiles C1=C2C(=C3C(=CC(=C(O3)O)O)OC2=O)C(=C(C1=O)O)O

Mechanism of Action

Targets/IC50/Ki
LDH-A
(Cell-free assay)
5.46 µM(Ki)
LDH-B
(Cell-free assay)
15.06 µM(Ki)
In vitro

Galloflavin inhibits both human LDH isoforms by preferentially binding the free enzyme, without competing with the substrate or cofactor. The calculated Ki values for pyruvate are 5.46 mm (LDH-A) and 15.06 mm (LDH-B). In cultured tumor cells, galloflavin blocks aerobic glycolysis at micromolar concentrations,  not interferes with cell respiration, and induces cell death by triggering apoptosis.
Kinase Assay
LDH activity assay
Human LDH-A (from human liver) and LDH-B (from human heart) are added in scalar amounts (0– 500 mm final concentrations) to a reaction mix containing 100 mm phosphate buffer (pH 7.5), LDH (0.015 UmL-1), 1 mm pyruvate, and 150 mm NADH. The enzymatic activity is measured by monitoring NADH oxidation for a period of 3 min (lex= 340 nm, lem =460 nm).
In vivo

Galloflavin treatment attenuates the malignant and invasion abilities of colon cancer cells in tumor-bearing mice, which are inhibited by the knockout of NLRP3.
References

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