2. Metabolic Enzyme/Protease
  3. Phosphatase
  4. 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.

PFKFB3-IN-3

PFKFB3-IN-3 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PFKFB3-IN-3 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

In Vitro

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.

PFKFB3-IN-3 Related Antibodies

Cell Viability Assay[1]

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)
Concentration: 1, 10, 25 and 50 μM
Incubation Time: 48 h
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.

Cell Viability Assay[1]

Cell Line: PANC-1, MIA PaCa-2 PDAC cell lines
Concentration: 25 μM
Incubation Time: 15 min, 1, 2, 3, or 4 h
Result: Impaired long-term cell viability significantly in both cell lines after a 1 h incubation.
Increased cytotoxic effects with longer incubation times.
In Vivo

PFKFB3-IN-3 (Compound 6) (7 μM; waterborne exposure; 48 h) exerts statistically significant anti-tumor effects in a zebrafish PDAC xenograft model, and its ability to reduce signals from fluorescently labeled tumor cells is superior to the baseline clearance level[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 2 days post-fertilization embryos[1]
Dosage: 7 μM
Administration: immersion in fish water; daily; 48 h
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.
Molecular Weight

506.00

Formula

C27H28ClN5O3
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PFKFB3-IN-3 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

PFKFB3-IN-3PhosphatasePFKFB3Cys154PFKFB2MIA PaCa-2glycolytic fluxPANC-1pancreatic ductal adenocarcinomaPFKFB1PFKFB4PDAC cell linesInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PFKFB3-IN-3
Cat. No.:
HY-184148
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.