PDE5-IN-3

PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC50 of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC50 of 5.827 μM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC50=1286.96 ng/mL) . PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity[1].

Product Specifications

CAS Number

[2538149-57-2]

UNSPSC

12352005

Target

Apoptosis; EGFR; Phosphodiesterase (PDE) ; Wnt

Type

Reference compound

Related Pathways

Apoptosis; JAK/STAT Signaling; Metabolic Enzyme/Protease; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pde5-in-3.html

Solubility

10 mM in DMSO

Smiles

O=C1C2=C(N(C3=CC=C(Br)C=C3)N=C2)N=C(C4=CC5=CC=CC=C5N=C4OC)N1

Molecular Formula

C21H14BrN5O2

Molecular Weight

448.27

References & Citations

[1]Tarek S Ibrahim, et al. Design and synthesis of novel pyrazolo[3,4-d]pyrimidin-4-one bearing quinoline scaffold as potent dual PDE5 inhibitors and apoptotic inducers for cancer therapy. Bioorg Chem. 2020 Dec;105:104352.