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3PO

Catalog No. T22223 CAS 18550-98-6

3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.

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3PO, CAS 18550-98-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 52.00
10 mg	In stock	$ 74.00
25 mg	In stock	$ 129.00
50 mg	In stock	$ 198.00
100 mg	In stock	$ 358.00
200 mg	In stock	$ 533.00
500 mg	In stock	$ 849.00
1 mL * 10 mM (in DMSO)	In stock	$ 58.00

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Purity: 99.67%

Purity: 97.76%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.
Targets&IC50	PFKFB3:22.9 μM
In vitro	3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. Compared with the wild-type PFKFB3+/+transformed cells (IC50, 49 μM), the PFKFB3+/- fibroblasts were more sensitive to compound 3PO treatment (IC50, 26 μM). 3PO Causes G2-M phase arrest, which Is preceded by decreased Fru-2,6-BP and glucose uptake. 3PO slows growth through inhibition of PFK-2 activity, then ectopic expression of the PFKFB3 isozyme may thwart the cytostatic activity of 3PO. [1] 3PO inhibits the glycolytic regulator PFKFB3 in endothelial cells (ECs). 3PO decreases glycolysis in ECs and impairs vessel sprouting. 3PO also suppresses vascular hyperbranching induced by inhibition of Notch or VEGF receptor 1 (VEGFR1) and amplified the antiangiogenic effect of VEGF blockade[2].
In vivo	Compared with vehicle control, compound 3PO treatment significantly reduced Fru-2,6-BP in tumor xenografts (vehicle: 13.1 ± 1.9 pmol/mg, 3PO: 8.5 ± 1.7 pmol/mg). [1] 3PO also impairs (pathological) angiogenesis.

Molecular Weight	210.23
Formula	C13H10N2O
CAS No.	18550-98-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 113mg/ml（537.51mM）

Ethanol: 11 mg/mL (52.32 mM)

References and Literature

1. Clem B, et al. Small-molecule inhibition of 6-phosphofructo-2-kinase activity suppresses glycolytic flux and tumor growth. Mol Cancer Ther. 2008 Jan;7(1):110-20. 2. Schoors S, et al. Partial and transient reduction of glycolysis by PFKFB3 blockade reduces pathological angiogenesis. Cell Metab. 2014 Jan 7;19(1):37-48. 3. Lea MA, Inhibition of Growth of Bladder Cancer Cells by 3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one in Combination with Other Compounds Affecting Glucose Metabolism. Anticancer Res. 2015 Nov;35(11):5889-99.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Autophagy Compound Library Metabolism Compound Library Apoptosis Compound Library Kinase Inhibitor Library Glycolysis Compound Library Anti-Cancer Metabolism Compound Library NO PAINS Compound Library Preclinical Compound Library

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Related compounds with same targets

PF-04991532 Tangshenoside I ARRY-403 PFK-015 Palmitelaidic Acid AMG-1694 PFK-158 Globalagliatin

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Keywords

3PO 18550-98-6 Autophagy Metabolism Glucokinase isozyme inhibit adenocarcinoma cell human malignant hematopoietic chemotherapeutic agents small-molecule Inhibitor inhibitor

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