3PO

Catalog No.S7639 Batch:S763901

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Technical Data

Formula

C13H10N2O
Molecular Weight 210.23 CAS No. 18550-98-6
Solubility (25°C)* In vitro DMSO 42 mg/mL (199.78 mM)
Ethanol 42 mg/mL (199.78 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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].
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].

Protocol (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    tumor bearing mice (BALB/c nude mice or C57Bl/6 female mice background)

  • Dosages

    0.07 mg/g

  • Administration

    i.p.

Selleck's 3PO has been cited by 8 publications

Short isoform thymic stromal lymphopoietin reduces inflammation and aerobic glycolysis of asthmatic airway epithelium by antagonizing long isoform thymic stromal lymphopoietin [ Respir Res, 2022, 23(1):75] PubMed: 35351157
STAT3 signaling mediates peritoneal fibrosis by activating hyperglycolysis [ Am J Transl Res, 2022, 14(10):7552-7565] PubMed: 36398234
Hypoxic postconditioning promotes neurogenesis by modulating the metabolism of neural stem cells after cerebral ischemia [ Exp Neurol, 2021, 347:113871] PubMed: 34563509
The role of macrophage-fibroblast interaction in lipopolysaccharide-induced pulmonary fibrosis: an acceleration in lung fibroblast aerobic glycolysis [ Lab Invest, 2021, 10.1038/s41374-021-00701-7] PubMed: 34775492
HMGB1-activated fibroblasts promote breast cancer cells metastasis via RAGE/aerobic glycolysis [ Neoplasma, 2021, 68(1):71-78] PubMed: 33030958
PI3K-Akt-mTOR/PFKFB3 pathway mediated lung fibroblast aerobic glycolysis and collagen synthesis in lipopolysaccharide-induced pulmonary fibrosis [ Lab Invest, 2020, 100(6):801-811] PubMed: 32051533
PI3K-Akt-mTOR/PFKFB3 pathway mediated lung fibroblast aerobic glycolysis and collagen synthesis in lipopolysaccharide-induced pulmonary fibrosis. [ Lab Invest, 2020, 10.1038/s41374-020-0404-9] PubMed: 32051533
Targeting PFKFB3 sensitizes chronic myelogenous leukemia cells to tyrosine kinase inhibitor [ Oncogene, 2018, 37(21):2837-2849] PubMed: 29511345

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.