PDE5-IN-3

Modify Date: 2024-01-05 19:53:49

PDE5-IN-3 Structure
PDE5-IN-3 structure
Common Name PDE5-IN-3
CAS Number 2538149-57-2 Molecular Weight 448.27
Density N/A Boiling Point N/A
Molecular Formula C21H14BrN5O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name PDE5-IN-3

 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
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