1. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  2. Phosphodiesterase (PDE) EGFR Wnt Apoptosis
  3. 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.

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PDE5-IN-3 Chemical Structure

PDE5-IN-3 Chemical Structure

CAS No. : 2538149-57-2

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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].

IC50 & Target[1]

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].

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

Molecular Weight

448.27

Formula

C21H14BrN5O2

CAS No.
SMILES

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

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PDE5-IN-3
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HY-131710
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