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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PFKFB4-IN-1 Related Antibodies

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

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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.
SMILES

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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PFKFB4-IN-1 Related Classifications

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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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