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Chemical Structure| 18550-98-6 Chemical Structure| 18550-98-6

Structure of 3PO
CAS No.: 18550-98-6

Chemical Structure| 18550-98-6

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3PO is an inhibitor of PFKFB3. It inhibits the proliferation of various human cancer cells with IC50s ranging from 1.4-24 μmol/L. 3PO can inhibit glucose uptake, reduce intracellular concentrations of Fru-2,6-BP, lactate, ATP, NAD+, and NADH. It can be used in cancer research.

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

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Product Details of 3PO

CAS No. :18550-98-6
Formula : C13H10N2O
M.W : 210.23
SMILES Code : O=C(C1=CC=NC=C1)/C=C/C2=CC=CN=C2
Synonyms :
3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
MDL No. :MFCD00224002

Safety of 3PO

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
THP-1 monocytes 2.5, 5, or 10 μM 30 minutes To evaluate the effect of the PFKFB3 inhibitor 3PO on the chemotaxis of THP-1 monocytes, results showed that 3PO inhibited MCP-1-induced chemotaxis of THP-1 cells. Br J Pharmacol. 2022 Nov;179(21):4974-4991.
Idiopathic pulmonary fibrosis (IPF) lung myofibroblasts 10 μM 24 hours Inhibition of glycolysis, reversal of the differentiated state of IPF myofibroblasts Am J Respir Crit Care Med. 2015 Dec 15;192(12):1462-74.
Human normal lung fibroblasts MRC-5 10 μM 24 hours Inhibition of glycolysis, reduction of TGF-β1-induced myofibroblast differentiation Am J Respir Crit Care Med. 2015 Dec 15;192(12):1462-74.
Human umbilical vein endothelial cells (HUVECs) 0.20 μM 24 hours To evaluate the effect of 3PO on PFKFB3 expression in HUVECs, results showed that 3PO effectively inhibited BEV-induced PFKFB3 expression. Theranostics. 2020 Jun 5;10(16):7245-7259.
Human liver sinusoidal endothelial cells (LSEC) 15μM Inhibition of glycolysis attenuated stress fiber and focal adhesion formation in LSEC on stiff substrates, and decreased nuclear pore size J Hepatol. 2022 Sep;77(3):723-734.
C2C12 myotubes 10µM 1 hour To investigate the inhibitory effect of 3PO on glycolysis and its impact on trans-plasma membrane electron transport (tPMET). Results showed that 3PO did not affect WST-1 reduction, indicating glycolysis is not involved in tPMET. Redox Biol. 2019 Oct;27:101075.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Bleomycin and TGF-β1-induced lung fibrosis models Intraperitoneal injection 50 mg/kg Seven times within 2 weeks Inhibition of glycolysis, attenuation of bleomycin and TGF-β1-induced lung fibrosis Am J Respir Crit Care Med. 2015 Dec 15;192(12):1462-74.
NOD-SCID mice Patient-derived orthotopic GBM xenograft models Intraperitoneal injection 25 mg/kg Three times a week, until mice became moribund or displayed severe neurological symptoms To evaluate the effect of 3PO combined with BEV on tumor vascular normalization, hypoxia alleviation, lactate production reduction, and chemotherapy efficacy. Results showed that dual therapy significantly extended survival, delayed tumor growth, and enhanced the delivery of chemotherapeutic drugs. Theranostics. 2020 Jun 5;10(16):7245-7259.
Rats Sugen 5416/hypoxia-induced pulmonary hypertension model Intraperitoneal injection 50 mg/kg/d Once daily for 5 weeks 3PO almost completely prevented Su/Hx-induced pulmonary hypertension, reduced right ventricular systolic pressure and mean pulmonary arterial pressure, and improved pulmonary artery diastolic function Proc Natl Acad Sci U S A. 2019 Jul 2;116(27):13394-13403

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.76mL

0.95mL

0.48mL

23.78mL

4.76mL

2.38mL

47.57mL

9.51mL

4.76mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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