2. PI3K/Akt/mTOR Apoptosis Cell Cycle/DNA Damage Cytoskeleton
  3. Akt Apoptosis mTOR PI3K Microtubule/Tubulin
  4. PI3K/Akt/mTOR-IN-4

PI3K/Akt/mTOR-IN-4 (compound 4r) 是一种有效的 PI3K/Akt/mTOR 和微管蛋白聚合 (tubulin polymerization) 抑制剂。PI3K/Akt/mTOR-IN-4 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G2/M 期。PI3K/Akt/mTOR-IN-4 会降低p-PI3K、p-Akt、p-mTOR 和 β-微管蛋白的表达。

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PI3K/Akt/mTOR-IN-4

PI3K/Akt/mTOR-IN-4 Chemical Structure

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PI3K/Akt/mTOR-IN-4 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3K/Akt/mTOR-IN-4 (compound 4r) is a potent PI3K/Akt/mTOR and tubulin polymerization inhibitor. PI3K/Akt/mTOR-IN-4 induce apoptosis and cell cycle arrest at G2/M phase. PI3K/Akt/mTOR-IN-4 decreases the expression of p-PI3K, p-Akt, and p-mTOR, β-tubulin[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Ca-Ski IC50
7.24 μM
Compound: 4r
Antiproliferative activity against human Ca-Ski cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human Ca-Ski cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 38636129]
HEK-293T IC50
23.96 μM
Compound: 4r
Cytotoxicity against human HEK293T cells assessed as cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HEK293T cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 38636129]
HeLa IC50
5.03 μM
Compound: 4r
Antiproliferative activity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 38636129]
L02 IC50
21.08 μM
Compound: 4r
Cytotoxicity against human L02 cells assessed as cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 38636129]
SiHa IC50
3.38 μM
Compound: 4r
Antiproliferative activity against human SiHa cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human SiHa cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 38636129]
体外研究
(In Vitro)

PI3K/Akt/mTOR-IN-4 (compound 4r) (0-100 µM; 48 h) 显示出抗增殖活性，对 SiHa、HeLa、Ca Ski、LO2、HEK-293t 细胞的 IC50 值分别为 3.38、5.03、7.24、21.08、23.96 µM[1]。
PI3K/Akt/mTOR-IN-4 (0-16 µM; 24 h) 诱导细胞凋亡和细胞周期停滞在 G2/M 期[1]。
PI3K/Akt/mTOR-IN-4 (4, 8,16 µM；24 h) 以剂量依赖性方式降低 p-PI3K、p-Akt、p-mTOR 和 β-微管蛋白的表达[1]。

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

PI3K/Akt/mTOR-IN-4 相关抗体:

Cell Proliferation Assay[1]

Cell Line: SiHa, HeLa, Ca Ski, LO2, HEK-293t cells
Concentration: 0-100 µM
Incubation Time: 48 h
Result: Inhibited cell proliferative with IC50s of 3.38, 5.03, 7.24, 21.08, 23.96 µM for SiHa, HeLa, Ca Ski, LO2, HEK-293t cells, respectively.

Cell Cycle Analysis[1]

Cell Line: SiHa cells
Concentration: 0-16 µM
Incubation Time: 24 h
Result: Induced cell cycle arrest at G2/M phase with G2/M phase cells accumulating from 5.24 % (Ctrl) to 28.37 % (16 μM).

Apoptosis Analysis[1]

Cell Line: SiHa cells
Concentration: 0-16 µM
Incubation Time: 24 h
Result: Induced apoptosis the percentage of apoptotic cells were increased from 11.62 % (Ctrl) to 98.56 % (16 μM).

Western Blot Analysis[1]

Cell Line: SiHa cells
Concentration: 4, 8, 16 μM
Incubation Time: 24 h
Result: Decreased the expression of phosphorylation of PI3K, Akt, and mTOR, β-tubulin in a dose-dependent manner.
体内研究
(In Vivo)

PI3K/Akt/mTOR-IN-4 (0-400 μM; 0-96 h) 对斑马鱼胚胎没有毒性[1]。

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

Animal Model: zebrafish embryos[1]
Dosage: 0, 12.5, 25, 50, 100, 200, 400 μM
Administration: 0-96 h
Result: Showed no toxicity for zebrafish embryos.
分子量

500.56

Formula

C29H29FN4O3
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/Akt/mTOR-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

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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/Akt/mTOR-IN-4AktApoptosismTORPI3KMicrotubule/TubulinPKBProtein kinase BMammalian target of RapamycinPhosphoinositide 3-kinasetubulin polymerizationapoptosisG2/Mp-PI3Kp-Aktand p-mTORzebrafish embryosInhibitorinhibitorinhibit

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