2. PI3K/Akt/mTOR Apoptosis
  3. PI3K mTOR Apoptosis Bcl-2 Family MDM-2/p53 Caspase
  4. PI3K/mTOR-IN-17

PI3K/mTOR-IN-17 是一种 PI3K 和 mTOR 双重抑制剂，对 PI3K 和 mTOR 的 IC50 值分别为 1.21 μM 和 0.21 μM。PI3K/mTOR-IN-17 通过将细胞生长阻滞在 G1 期，诱导细胞发生 caspase 介导的细胞凋亡 (apoptosis)。PI3K/mTOR-IN-17 上调 caspases-3、7、8 和 9 的水平、p53 的表达以及 Bax/Bcl-2 比值。PI3K/mTOR-IN-17 抑制 PI3K/mTOR 信号通路。PI3K/mTOR-IN-17 可用于癌症研究，如非小细胞肺癌 (NSCLC)。

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PI3K/mTOR-IN-17 Chemical Structure

PI3K/mTOR-IN-17 Chemical Structure

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Customer Review

PI3K/mTOR-IN-17 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 mTOR 亚型特异性产品:

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mTOR mTORC1 mTORC2

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3K/mTOR-IN-17 is a dual PI3K and mTOR inhibitor with IC50 values of 1.21 μM (PI3K), and 0.21 μM (mTOR). PI3K/mTOR-IN-17 induces cells caspase-mediated apoptosis by arresting their growth in the G1-phase. PI3K/mTOR-IN-17 upregulates the levels of caspases-3, 7, 8, and 9, p53 expression and Bax/Bcl-2 ratio. PI3K/mTOR-IN-17 suppresses the PI3K/mTOR signaling pathway. PI3K/mTOR-IN-17 can be used for research of cancer, such as non-small cell lung cancer (NSCLC)[1].

IC50 & Target

PI3K

1.21 μM (IC50)

mTOR

0.21 μM (IC50)

Caspase 3

 

Caspase-7

 

Caspase-8

 

Caspase-9

 

Bax

 

Bcl-2

 

体外研究
(In Vitro)

PI3K/mTOR-IN-17 (Compound 8) 显示出优异的细胞毒性，对肺成纤维细胞 WI-38 的 IC50 值为 21.13 μM，对 A549 细胞的 IC50 值为 1.39 μM，选择性指数为 15.32[1]。

PI3K/mTOR-IN-17 (1.39 μM, 48 h) 可上调 A549 细胞中 p53 和 Bax 的水平，并下调 Bcl-2、EGFR、PI3K 和 mTOR 的水平[1]。

PI3K/mTOR-IN-17 (1.39 μM, 48 h) 可上调 A549 细胞中启动型 caspase-8 和 9 的水平，以及执行型 caspase-3 和 7 的水平[1]。

PI3K/mTOR-IN-17 (1.39 μM, 48 h) 通过将 A549 细胞生长阻滞在 G1 期，显著诱导细胞凋亡[1]。

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

PI3K/mTOR-IN-17 相关抗体:

Real Time qPCR[1]

Cell Line: A549 lung cancer cells
Concentration: 1.39 μM
Incubation Time: 48 h
Result: Significantly increased the expression of p53 by 8.38 folds Bax by 9.88 fold and downregulated the leves of Bcl-2 by 0.45 fold.
Suppressed gene expression of EGFR by 0.42 fold, PI3K by 0.45 fold, and mTOR by 0.58 fold.

Apoptosis Analysis[1]

Cell Line: A549 lung cancer cells
Concentration: 1.39 μM
Incubation Time: 48 h
Result: Significantly induced, increasing the overall death rate by 21 fold.
Total apoptosis reached 25.03% (19.38% late apoptosis, 5.65% early apoptosis) compared to 1.19% in the untreated control group.
Markedly increased the cell population in the G1-phase to 80.2% compared to 57.3% in the control,and reduced the proportions of cells in the S and G2/M phases.

ELISA Assay[1]

Cell Line: A549 lung cancer cells
Concentration: 1.39 μM
Incubation Time: 48 h
Result: Upregulated the initiator caspase-8 and 9 levels by almost 2.2 and 1.03 fold and the executioner caspases-3 and 7 by 1.73 and 1.34 fold.
分子量

618.68

Formula

C36H34N4O6
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

PI3K/mTOR-IN-17 相关分类

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  • 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:

PI3K/mTOR-IN-17PI3KmTORApoptosisBcl-2 FamilyMDM-2/p53CaspasePhosphoinositide 3-kinaseMammalian target of RapamycinCaspasesBax/Bcl-2P53Non-small cell lung cancer (NSCLC)A549 cellslung fibroblasts WI-38Inhibitorinhibitorinhibit

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