Home Metabolism LDH inhibitor Galloflavin For research use only.

Galloflavin

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

Galloflavin Chemical Structure

CAS: 568-80-9

Selleck's Galloflavin has been cited by 1 publication

Purity & Quality Control

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

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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
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.[1]
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).
Cell Research Cell lines PLC/PRF/5 cell line
Concentrations 0.1–500 μM
Incubation Time 3 h
Method

PLC/PRF/5 cells (1.6 × 104 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.
In Vivo
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.[2]

Chemical Information & Solubility

Molecular Weight 278.17 Formula

C12H6O8
CAS No. 568-80-9 SDF --
Smiles C1=C2C(=C3C(=CC(=C(O3)O)O)OC2=O)C(=C(C1=O)O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 2 mg/mL ( (7.18 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

Handling Instructions

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