PFKFB3-IN-3
PFKFB3-IN-3 is a selective PFKFB3 inhibitor with a Ki value of 0.09 μM. PFKFB3-IN-3 reduces cancer cell viability, inhibits tumor growth in xenograft models, and acts as a chemosensitizer to exert synergistic effects with chemotherapeutic agents. The limited cellular activity of PFKFB3-IN-3 restricts its application as a chemical probe, but it demonstrates that the Cys154 residue of PFKFB3 is druggable. PFKFB3-IN-3 can be used for the research of pancreatic ductal adenocarcinoma.
For research use only. We do not sell to patients.
- Formula: C27H28ClN5O3
- Molecular Weight:506.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
PFKFB3-IN-3 (Compound 6) (1-50 μM; 48 h) reduces the viability of pancreatic ductal adenocarcinoma (PDAC) cell lines (PANC-1, MIA PaCa-2, Suit2, AsPC1, PaCa3, Hs776T), whereas its cytotoxicity against NHDF and HPDE cells is negligible[1].
PFKFB3-IN-3 (25 μM; 15 min-4 h) induces sustained cytotoxicity in PANC-1 and MIA PaCa-2 PDAC cells following transient exposure (1 h and longer)[1].
PFKFB3-IN-3 (1-50 μM; 48 h) reduces the viability of human cancer cell lines with high PFKFB3 expression (A549, ACHN, U251, SH-SY5Y) derived from non-pancreatic ductal adenocarcinoma (non-PDAC), while exerting minimal effects on PFKFB3-negative non-transformed fibroblasts (BJ, WI-38)[1].
PFKFB3-IN-3 (25 μM; 2 h) reduces PFK activity in lysates of MIA PaCa-2 PDAC cells, confirming that it continuously inhibits glycolytic flux via covalent targeting of PFKFB3[1].
PFKFB3-IN-3 (25 μM; 1-2 h) rapidly and potently blocks glycolytic ATP production in MIA PaCa-2 pancreatic ductal adenocarcinoma cells[1].
PFKFB3-IN-3 (25 μM; 2-6 h) reduces the glycolysis rate, glycolytic capacity, and glycolytic reserve of PANC-1 and MIA PaCa-2 PDAC cells, and its inhibitory effect on glycolytic function is time-dependent[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Normal human dermal fibroblasts (NHDF), immortalized pancreatic ductal epithelial cells (HPDE), human PDAC cell lines (PANC-1, MIA PaCa-2, Suit2, AsPC1, PaCa3, Hs776T)
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Concentration:1, 10, 25 and 50 μM
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Incubation Time:48 h
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Result:Showed no cytotoxicity in NHDF cells at concentrations up to 50 μM.
Showed minimal cytotoxicity in HPDE cells.
Induced dose-dependent cytotoxicity across all PDAC cell lines, with IC50 values ranging from 15 to 30 μM depending on the cell line.
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Cell Line:PANC-1, MIA PaCa-2 PDAC cell lines
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Concentration:25 μM
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Incubation Time:15 min, 1, 2, 3, or 4 h
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Result:Impaired long-term cell viability significantly in both cell lines after a 1 h incubation.
Increased cytotoxic effects with longer incubation times.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:2 days post-fertilization embryos[1]
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Dosage:7 μM
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Administration:immersion in fish water; daily; 48 h
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Result:Reduced fluorescence intensity statistically significantly at T2 compared to controls in MIA PaCa-2 xenografts.
Reduced fluorescence intensity statistically significantly at both T1 and T2 compared to controls in PANC-1 xenografts, with more pronounced and significant reduction at T2.
Chemical Information
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Molecular Weight 506.00
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Formula C27H28ClN5O3
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SMILES
C/C=C\C(N1C=C(C2=CC(OC3=CC=C(C=C3)NC([C@@H]4CCCN4)=O)=CC=C21)C5=CN(N=C5)C)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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