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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

448.27

C₂₁H₁₄BrN₅O₂

2538149-57-2

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]