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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- CAS. Nr.: 2538149-57-2
- Formel: C21H14BrN5O2
- Molecular Weight:448.27
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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PDE5 1.57 nM (IC50) |
EGFR 5.827 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
8.72 μM
Compound: 68
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Anticancer activity against human HeLa cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
Anticancer activity against human HeLa cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
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[PMID: 34438126] |
| HeLa | IC50 |
8.72 μM/L
Compound: 68
|
Anticancer activity against human HeLa cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
Anticancer activity against human HeLa cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
|
[PMID: 34438126] |
| MCF7 | IC50 |
6.56 μM
Compound: 68
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Anticancer activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
Anticancer activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
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[PMID: 34438126] |
| MCF7 | IC50 |
6.56 μM/L
Compound: 68
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Anticancer activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
Anticancer activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
|
[PMID: 34438126] |
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.
Chemical Information
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CAS. Nr. 2538149-57-2
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Molecular Weight 448.27
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Formel C21H14BrN5O2
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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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PDE5-IN-3 Related Classifications
HY-131710 Related Classifications
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