2. Metabolic Enzyme/Protease Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. Phosphatase Apoptosis Caspase PARP
  4. PFKFB4-IN-1

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.

PFKFB4-IN-1

PFKFB4-IN-1 Chemical Structure

CAS No. : 2664831-55-2

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Based on 1 publication(s) in Google Scholar

PFKFB4-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Caspase Isoform Specific Products:

View All Isoforms
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

View All PARP Isoform Specific Products:

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

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Description

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[1].

IC50 & Target[1]

PFKFB4

4.50 μM (IC50)

In Vitro

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.

PFKFB4-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF7 cells
Concentration: 6, 12, and 18 μM
Incubation Time: 0, 1, 2, 4, 8 and 24 h
Result: Progressively increased levels of cleaved PARP and cleaved caspase-3.
Did not accelerate PFKFB4 protein degradation in MCF-7 cells.

Cell Migration Assay [1]

Cell Line: MCF7 cells
Concentration: 6, 12, and 18 μM
Incubation Time: 0 and 24 h
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.

Cell Proliferation Assay[1]

Cell Line: MCF7 cells
Concentration: 6, 12, and 18 μM
Incubation Time: 7 days
Result: Markedly inhibited colony formation in MCF-7 cells even at low concentrations.
Completely prevented colony growth at 18 μM.

Apoptosis Analysis[1]

Cell Line: MCF7 cells
Concentration: 6, 12, and 18 μM
Incubation Time: 24 h
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.
In Vivo

PFKFB4-IN-1 (30 mg/kg, i.p., q.d. for 14 days) inhibits tumor growth in MDA-MB-231 xenograft mouse model[1].
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.

Animal Model: Female BALB/c-nu nude mice subcutaneously injected with MDA-MB-231 cells[1]
Dosage: 30 mg/kg
Administration: i.p., q.d. for 14 days
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.
Animal Model: Zebrafish embryos[1]
Dosage: 5 μM
Administration: a single dose at 24 h post-fertilization for 72 h
Result: Resulted in only negligible embryonic mortality and minimal morphological deformities during the early stages of development.
Molecular Weight

318.20

Formula

C11H6N6O6
CAS No.
Appearance

Solid

Color

reddish brown

SMILES

O=[N+](C1=CC=C(O1)/C=N\NC2=CC=C(C3=NON=C23)[N+]([O-])=O)[O-]
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1427 mL 15.7134 mL 31.4268 mL
5 mM 0.6285 mL 3.1427 mL 6.2854 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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
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PFKFB4-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PFKFB4-IN-12664831-55-2PhosphataseApoptosisCaspasePARPpoly ADP ribose polymeraseATP-competitivePFKFB4MDA-MB-231A549MCF-7HepG2breast cancerlung cancerliver cancerzebrafishInhibitorinhibitorinhibit

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