2538149-57-2

2538149-57-2 structure

Name: PDE5-IN-3
Chemical Name: PDE5-IN-3
CAS Number: 2538149-57-2
Molecular Formula: C₂₁H₁₄BrN₅O₂
Molecular Weight: 448.27
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2022-08-22 08:00:57
Modify Date: 2024-01-05 19:53:49
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].

Name	PDE5-IN-3

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.

Molecular Formula	C₂₁H₁₄BrN₅O₂
Molecular Weight	448.27