Galloflavin

Catalog No.S9606

For research use only.

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 Chemical Structure

CAS No. 568-80-9

Purity & Quality Control

Choose Selective LDH Inhibitors

Biological Activity

Description 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.
Targets
LDH-A [1]
(Cell-free assay)
LDH-B [1]
(Cell-free assay)
5.46 µM(Ki) 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.<sup><a class="sref" href="#s_ref">[1]</a></sup>

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.<sup><a class="sref" href="#s_ref">[2]</a></sup>

Protocol (from reference)

Kinase Assay:

<sup><a class="sref" href="#s_ref">[1]</a></sup>

  • 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).

Cell Research:

<sup><a class="sref" href="#s_ref">[1]</a></sup>

  • Cell lines: PLC/PRF/5 cell line
  • Concentrations: 0.1–500 μM
  • Incubation Time: 3 h
  • Method:

    PLC/PRF/5 cells (1.6 × 10<sup>4 </sup>per well) are seeded in 24-well plates, allowed to adhere overnight, and treated for 72 h at 37 ℃ with  0–500 μM dose of Galloflavin. After the treatments, cells are used for assay of lactic acid production, cellular respiration and cell proliferation.

Animal Research:

<sup><a class="sref" href="#s_ref">[2]</a></sup>

  • Animal Models: Colon cancer model Balb/c nude mice inoculated with SW480 Cells
  • Dosages: 5 mg/kg, 15 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 278.17
Formula

C12H6O8

CAS No. 568-80-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=C2C(=C3C(=CC(=C(O3)O)O)OC2=O)C(=C(C1=O)O)O

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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