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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2538149-57-2
- 分子式: C21H14BrN5O2
- 分子量:448.27
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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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
|
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] |
| 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
|
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] |
| MCF7 | IC50 |
6.56 μM/L
Compound: 68
|
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.
化学情報
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CAS 番号 2538149-57-2
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分子量 448.27
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)