2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. Phosphodiesterase (PDE) EGFR Wnt Apoptosis
  4. PDE5-IN-3

PDE5-IN-3 (compound 11j) 是一种有效的 PDE5 抑制剂，IC50 为 1.57 nM。PDE5-IN-3 对 EGFR 显示中度抑制作用，IC50 为 5.827 µM。PDE5-IN-3 显着抑制 Wnt/β-catenin 通路 (IC50=1286.96 ng/mL)。PDE5-IN-3 在 HepG2 细胞中诱导内在的凋亡线粒体途径。PDE5-IN-3 具有很强的抗肿瘤活性。

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PDE5-IN-3 Chemical Structure

PDE5-IN-3 Chemical Structure

CAS No. : 2538149-57-2

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PDE5-IN-3 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

查看所有亚型
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

查看 EGFR 亚型特异性产品:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(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].

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

PDE5-IN-3 相关抗体:
分子量

448.27

Formula

C21H14BrN5O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PDE5-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

PDE5-IN-32538149-57-2Phosphodiesterase (PDE)EGFRWntApoptosisEpidermal growth factor receptorErbB-1HER1PDE5Wnt/β-cateninmitochondrialHepG2 cellsantitumorBcl-2Baxp53cytochrome ccaspase-9caspase-3Inhibitorinhibitorinhibit

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