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)

细胞效力
(Cellular Effect)
Cell Line 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]
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]
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

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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