Home Cell Cycle PFKFB inhibitor KAN0438757 For research use only.

KAN0438757

KAN0438757 is a potent and selective inhibitor of the metabolic kinase PFKFB3 (6-Phosphofructo-2-Kinase/Fructose-2,6-Biphosphatase 3) with IC50 of 0.19 μM and 3.6 μM for PFKFB3 and PFKFB4, respectively.

KAN0438757 Chemical Structure

KAN0438757 Chemical Structure

CAS No. 1451255-59-6

Purity & Quality Control

Batch: S040001 DMSO]7 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.37%
99.37

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Biological Activity

Description KAN0438757 is a potent and selective inhibitor of the metabolic kinase PFKFB3 (6-Phosphofructo-2-Kinase/Fructose-2,6-Biphosphatase 3) with IC50 of 0.19 μM and 3.6 μM for PFKFB3 and PFKFB4, respectively.
Targets
PFKFB3 [1]
(Cell-free assay)		 PFKFB4 [1]
(Cell-free assay)
0.19 μM 3.6 μM
In vitro
In vitro

A PFKFB3 inhibitor, KAN0438757, which selectively inhibits proliferation of transformed cells while sparing non-transformed cells. Inhibition of PFKFB3 enzymatic activity by KAN0438757 impairs IR-induced recruitment of ribonucleotide reductase (RNR) M2 and deoxynucleotide incorporation upon DNA repair.[1]
Kinase Assay ADP-GloTM Kinase Assay
First, after the kinase reaction, an equal volume of ADP-GloTM Reagent was added to terminate the kinase reaction and deplete the remaining ATP. Second, the Kinase Detection Reagent was added to simultaneously convert ADP to ATP and allow the newly synthesized ATP to be measured using a luciferase/luciferin reaction. The light generated was measured. The assay was performed in white 384-well plates by consecutive additions of a test compound solution, enzyme solution and substrate. Controls in the absence of inhibitor, 100 nM of an in-house inhibitor, and 49.5 µM of an in-house inhibitor were included in the plate. The final concentrations of all reagents per well were 50 mM Tris HCl at pH 8.0, 10 mM MgCl2, 5 mM NaPi at pH 8.0, 81.48 nM PFKFB3 or 145 nM PFKFB4, 8 µM ATP, 100 µM F6P (acid treated and then neutralized to remove any contaminating F-2,6-P2), 0.005% Tween-20 and 1 mM dithiothreitol. Enzyme, compounds, and controls were pre-incubated at room temperature for 15 min before the addition of substrate solution. The enzymatic reaction was allowed to proceed for 20 min and the reaction was terminated by the addition of ADP-GloTM Reagent (10 µL) to all wells followed by 40 min incubation at room temperature. After addition of Kinase Detection Reagent (20 µL) to all wells, the plate was incubated for 30 min at room temperature, followed by measurement. All plates were centrifuged after each addition.
Cell Research Cell lines U2OS cells
Concentrations 10 μM
Incubation Time 6 h
Method

Confocal analysis of IR-induced foci of RAD51 or RPA32 in U2OS cells following treatment with DMSO or 10 μM KAN757 (6 h), subjected to IR (6 Gy, 2 h recovery), or left untreated. HR activity after treatment of U2OS DR-GFP cells with indicated inhibitors as assessed by FACS analysis.
In Vivo
In vivo

In vivo administration of KAN0438757 in mice is well tolerated and does not trigger major systemic or toxic alterations.[2]
Animal Research Animal Models C57BL6/N mice
Dosages 10, 25, 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 447.43 Formula

C21H18FNO7S
CAS No. 1451255-59-6 SDF --
Smiles C1=CC(=CC(=C1)S(=O)(=O)NC2=CC(=C(C=C2)C(=O)OCCO)O)C3=C(C=CC(=C3)F)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 7 mg/mL ( (15.64 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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