PDE5-IN-3

Names

[ CAS No. ]:
2538149-57-2

[ Name ]:
PDE5-IN-3

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Signaling Pathways >> Stem Cell/Wnt >> Wnt
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

PDE5:1.57 nM (IC50)

EGFR:5.827 μM (IC50)


[In Vitro]

PDE5-IN-3 lowers the expression levels of the anti-apoptotic Bcl-2 protein, and causes the high expression of the pro-apoptotic protein Bax, p53, cytochrome c and up-regulates active caspase-9 and caspase-3 levels[1].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H14BrN5O2

[ Molecular Weight ]:
448.27

Related Compounds