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[1].

Product Specifications

CAS Number

[2664831-55-2]

UNSPSC

12352005

Target

Apoptosis; Caspase; PARP; Phosphatase

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

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

Molecular Formula

C11H6N6O6

Molecular Weight

318.20

References & Citations

[1]Chen Y, et al. Structure-guided discovery of nitrobenzo-2-oxa-1,3-diazole (NBD) scaffold-based PFKFB4 inhibitors for cancer therapy. Eur J Med Chem. 2025 Dec 15;300:118109.