Home Cell Cycle PFKFB inhibitor 3PO For research use only.

3PO

Synonyms: 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one

3PO (3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one) is a small-molecule inhibitor of PFKFB3 with an IC50 of 22.9 μM for recombinant human PFKFB3 protein and does not inhibit PFK-1 activity. It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.

3PO Chemical Structure

3PO Chemical Structure

CAS No. 18550-98-6

Purity & Quality Control

3PO Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat Growth inhibition assay 48 hrs Growth inhibition of human Jurkat cells expressing inducible FLAG-tagged PFKFB incubated for 48 hrs by trypan blue dye exclusion assay, IC50=1.4μM ChEMBL
NHBE Growth inhibition assay 48 to 72 hrs Growth inhibition of human NHBE cells immortalized with human telomerase and large-T antigen and transformed with mutated Ras protein incubated for 48 to 72 hrs by trypan blue dye exclusion assay, IC50=1.5μM ChEMBL
K562 Growth inhibition assay 48 hrs Growth inhibition of human K562 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=3.2μM ChEMBL
HL60 Growth inhibition assay 48 hrs Growth inhibition of human HL60 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=4.5μM ChEMBL
MDA-MB-231 Growth inhibition assay 48 hrs Growth inhibition of human MDA-MB-231 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=4.7μM ChEMBL
Jurkat Growth inhibition assay 48 hrs Growth inhibition of human Jurkat cells expressing un-altered PFKFB expression incubated for 48 hrs by trypan blue dye exclusion assay, IC50=8.9μM ChEMBL
CRL11174 Growth inhibition assay 48 hrs Growth inhibition of human CRL11174 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=15μM ChEMBL
LLC Growth inhibition assay 48 hrs Growth inhibition of mouse LLC cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=19μM ChEMBL
Jurkat Growth inhibition assay 48 hrs Growth inhibition of human Jurkat cells expressing inducible FLAG-tagged PFKFB in presence of doxycycline incubated for 48 hrs by trypan blue dye exclusion assay, IC50=19.3μM ChEMBL
HeLa Growth inhibition assay 48 hrs Growth inhibition of human HeLa cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=24μM ChEMBL
Jurkat Growth inhibition assay 48 hrs Growth inhibition of PFKFB3+/-ht/LT/Ras human Jurkat cells and incubated for 48 hrs by trypan blue dye exclusion assay, IC50=26μM ChEMBL
A549 Growth inhibition assay 48 hrs Growth inhibition of human A549 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=48μM ChEMBL
Jurkat Growth inhibition assay 48 hrs Growth inhibition of PFKFB3+/+ht/LT/Ras human Jurkat cells and incubated for 48 hrs by trypan blue dye exclusion assay, IC50=49μM ChEMBL
Jurkat Cell proliferation assay 10 uM 36 hrs Inhibition of cell proliferation of human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM incubated for 36 hrs by trypan blue dye exclusion assay ChEMBL
Jurkat Cell cycle assay Inhibition of cell cycle arrest in human Jurkat cells expressing inducible FLAG-tagged PFKFB assessed as accumulation at G2/M phase by propidium iodide staining based flow cytometry ChEMBL
Jurkat Function assay 10 uM Reduction in 2-deoxy-glucose uptake in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM measured within 4 hrs using [14C]-2-deoxy-glucose by scintillation counting method ChEMBL
Jurkat Function assay 10 uM 4 hrs Reduction in Fru-2,6-BP production in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM measured within 4 hrs ChEMBL
Jurkat Function assay 10 uM 8 hrs Reduction in lactate secretion in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 8 hrs by lactate oxidase based colorimetric assay ChEMBL
Jurkat Function assay 10 uM 16 hrs Reduction in NADH level in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 16 hrs ChEMBL
Jurkat Function assay 10 uM 24 hrs Reduction in NAD+ level in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 24 hrs ChEMBL
Jurkat Function assay 10 uM 24 hrs Reduction in ATP level in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 24 hrs ChEMBL
Jurkat Function assay 10 uM 36 hrs Suppression of glycolytic flux into lactate in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 36 hrs by NMR spectroscopy ChEMBL
NHBE Growth inhibition assay 1 uM 48 to 72 hrs Growth inhibition of human NHBE cells immortalized with human telomerase and large-T antigen and transformed with mutated Ras protein at 1 uM incubated for 48 to 72 hrs by trypan blue dye exclusion assay ChEMBL
NHBE Growth inhibition assay 10 uM 48 to 72 hrs Growth inhibition of human NHBE cells immortalized with human telomerase and large-T antigen and transformed with mutated Ras protein at 10 uM incubated for 48 to 72 hrs by trypan blue dye exclusion assay ChEMBL
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Biological Activity

Description 3PO (3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one) is a small-molecule inhibitor of PFKFB3 with an IC50 of 22.9 μM for recombinant human PFKFB3 protein and does not inhibit PFK-1 activity. It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.
Targets
PFKFB3 [2]
22.9 μM
In vitro
In vitro 3PO is an inhibitor of the PFKFB3 isozyme primarily through competition with Fru-6-P and does not inhibit purified PFK-1 activity. 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μmol/L) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. 3PO can cause G2-M phase arrest[1].
Cell Research Cell lines Jurkat cells
Concentrations 10 μmol/L
Incubation Time 0, 4, 8, 16, 24, or 36 h
Method

Jurkat cells are plated at 1 × 105/mL in RPMI 1640 supplemented with 10% fetal bovine serum and 50 μg/mL gentamicin sulfate. Cells are immediately treated with vehicle or 10 μmol/L 3PO for 0, 4, 8, 16, 24, or 36 h. Cell cycle analysis is done.
In Vivo
In vivo i.p. administration of 3PO (0.07 mg/g) to tumor-bearing mice markedly reduces the intracellular concentration of Fru-2,6-BP, glucose uptake, and growth of established tumors in vivo. It suppresses tumorigenic growth of breast adenocarcinoma, leukemia, and lung adenocarcinoma cells in vivo[1]. The PK properties of 3PO are examined in C57Bl/6 mice intravenously administered 3PO: clearance CL=2312 mL/min/kg, T1/2=0.3 hr, Cmax=113 ng/ml, AUC0-inf=36 ng/hr/ml. 3PO is reported to have potent activity against a highly relevant mouse model of leukemia[2].
Animal Research Animal Models tumor bearing mice (BALB/c nude mice or C57Bl/6 female mice background)
Dosages 0.07 mg/g
Administration i.p.

Chemical Information & Solubility

Molecular Weight 210.23 Formula

C13H10N2O
CAS No. 18550-98-6 SDF Download 3PO SDF
Smiles C1=CC(=CN=C1)C=CC(=O)C2=CC=NC=C2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 42 mg/mL ( (199.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 11 mg/mL

Water : Insoluble


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In vivo
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