PFKFB4-IN-1
Based on 1 Customer Validation
PFKFB4-IN-1 is a potent and selective ATP-competitive PFKFB4 inhibitor (IC50 = 4.50 μM) that reduces intracellular PFKFB4 protein levels. PFKFB4-IN-1 exhibits >12-fold selectivity over PFKFB1/4 and PFKFB3/4. PFKFB4-IN-1 inhibits cancer cell proliferation, induces apoptosis, and inhibits cell migration. PFKFB4-IN-1 inhibits tumor growth in the MDA-MB-231 xenograft mouse model. PFKFB4-IN-1 can be used for breast, lung and liver cancer research.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 2664831-55-2
- Formula: C11H6N6O6
- Molecular Weight:318.20
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Epigenetics Compound Library
HY-L005
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Phosphatase Inhibitor Library
HY-L081
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Anti-Cancer Metabolism Compound Library
HY-L083
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Anti-Liver Cancer Compound Library
HY-L101
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Anti-Ovarian Cancer Compound Library
HY-L173
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
All Caspase Isoforms
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Biological Activity
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PFKFB4 4.50 μM (IC50) |
PFKFB4-IN-1 (compound 2v) (2-100 μM, 72 h) demonstrates broad-spectrum anticancer activity, with IC50 values of 4.02 μM (MCF-7), 11.07 μM (HepG2), and 11.2 μM (A549), while showing significantly lower cytotoxicity toward normal human liver cells (HL7702, IC50 > 50 μM)[1].
PFKFB4-IN-1 (0-48 h) inhibits proliferation of MCF-7 breast cancer cells in both time- and concentration-dependent manner[1].
PFKFB4-IN-1 (6-18 μM, 24 h) inhibits both migration and colony formation, and induces apoptosis in MCF-7 breast cancer cells through the canonical caspase-3 activation and PARP cleavage pathway[1].
PFKFB4-IN-1 (0-25 μM, 24 h) suppresses PFKFB4 protein levels and suppresses glycolytic metabolism in MCF-7 cells, with markedly reduced intracellular ATP and NADP+/NADPH levels[1].
PFKFB4-IN-1 stably binds within the ATP-binding pocket of PFKFB4, forming key hydrogen bonds with residues Asn168, Gly51, and Tyr428.
PFKFB4-IN-1 shows no significant increase in ROS levels and DNA damage in MCF-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7 cells
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Concentration:6, 12, and 18 μM
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Incubation Time:0, 1, 2, 4, 8 and 24 h
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Result:Progressively increased levels of cleaved PARP and cleaved caspase-3.
Did not accelerate PFKFB4 protein degradation in MCF-7 cells.
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Cell Line:MCF7 cells
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Concentration:6, 12, and 18 μM
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Incubation Time:0 and 24 h
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Result:Significantly inhibited the migration of MCF-7 cells into the wounded area, with a significant reduction in the number of migrating cells compared to the control group.
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Cell Line:MCF7 cells
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Concentration:6, 12, and 18 μM
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Incubation Time:7 days
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Result:Markedly inhibited colony formation in MCF-7 cells even at low concentrations.
Completely prevented colony growth at 18 μM.
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Cell Line:MCF7 cells
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Concentration:6, 12, and 18 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a concentration-dependent manner, with the apoptotic rate of MCF-7 cells increasing from 5.61% to 6.55% and 9.68%, respectively.
PFKFB4-IN-1 (5 μM, a single dose at 24 h post-fertilization for 72 h) shows a favorable acute safety profile in the zebrafish developmental toxicity model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c-nu nude mice subcutaneously injected with MDA-MB-231 cells[1]
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Dosage:30 mg/kg
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Administration:i.p., q.d. for 14 days
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Result:Exerted a notable inhibitory effect on tumor growth with the tumor growth inhibition (TGI) of 71.9%.
Induced pronounced nuclear shrinkage in tumor tissues, suggesting that its antitumor effect may be attributed to the induction of apoptosis.
Showed no significant body weight fluctuations and no damages in organ tissues.
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Animal Model:Zebrafish embryos[1]
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Dosage:5 μM
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Administration:a single dose at 24 h post-fertilization for 72 h
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Result:Resulted in only negligible embryonic mortality and minimal morphological deformities during the early stages of development.
Chemical Information
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CAS No. 2664831-55-2
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Appearance Solid
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Molecular Weight 318.20
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Formula C11H6N6O6
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Color reddish brown
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SMILES
O=[N+](C1=CC=C(O1)/C=N\NC2=CC=C(C3=NON=C23)[N+]([O-])=O)[O-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 20 mg/mL (62.85 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1427 mL | 15.7134 mL | 31.4268 mL | 78.5669 mL |
| 5 mM | 0.6285 mL | 3.1427 mL | 6.2854 mL | 15.7134 mL | |
| 10 mM | 0.3143 mL | 1.5713 mL | 3.1427 mL | 7.8567 mL | |
| 15 mM | 0.2095 mL | 1.0476 mL | 2.0951 mL | 5.2378 mL | |
| 20 mM | 0.1571 mL | 0.7857 mL | 1.5713 mL | 3.9283 mL | |
| 25 mM | 0.1257 mL | 0.6285 mL | 1.2571 mL | 3.1427 mL | |
| 30 mM | 0.1048 mL | 0.5238 mL | 1.0476 mL | 2.6189 mL | |
| 40 mM | 0.0786 mL | 0.3928 mL | 0.7857 mL | 1.9642 mL | |
| 50 mM | 0.0629 mL | 0.3143 mL | 0.6285 mL | 1.5713 mL | |
| 60 mM | 0.0524 mL | 0.2619 mL | 0.5238 mL | 1.3094 mL |
PFKFB4-IN-1 Related Classifications
HY-178367 Related Classifications
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