1. PI3K/Akt/mTOR Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  2. Akt Microtubule/Tubulin Apoptosis
  3. AKT1-IN-11

AKT1-IN-11 是 Podophyllotoxin (HY-15552) 的衍生物,是一种 AKT1/tubulin双重抑制剂。AKT1-IN-11 会下调肿瘤细胞中 AKT 激酶的磷酸化水平,干扰细胞增殖,导致 G2/M 期阻滞并诱导细胞凋亡 (apoptosis)。AKT1-IN-11 还能促进微管蛋白解聚。AKT1-IN-11 可用于结直肠癌的研究。

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AKT1-IN-11

AKT1-IN-11 Chemical Structure

CAS No. : 3087064-94-3

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查看 Akt 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AKT1-IN-11, a Podophyllotoxin (HY-15552) derivative, is a AKT1/tubulin dual inhibitor. AKT1-IN-11 down-regulates the phosphorylation level of AKT kinase in tumor cells, disrupting cell proliferation, causeing G2/M phase arrest and inducing apoptosis. AKT1-IN-11 also promotes tubulin depolymerization. AKT1-IN-11 can be used for the research of colorectal cancer[1].

体外研究
(In Vitro)

AKT1-IN-11 (48 h) 抑制 HCT-116, HT-29, HCT-8, 和 NCM460 细胞增殖,其 IC50 值分别为 0.77, 0.48, 1.68 和 52.28 μM[1]
AKT1-IN-11 (0.2 μM, 12-24 h) 在 HCT-116 细胞中诱导凋亡[1]
AKT1-IN-11 (0.1-0.2 μM; 24 h) 抑制 HCT-116 细胞迁移并逆转细胞中的上皮间质转化过程[1]
AKT1-IN-11 (0.1-0.2 μML; 2-8 h) 诱导 HCT-116 细胞 G2/M 期阻滞,并下调 Cyclin B1 和 CDK4 表达[1]
AKT1-IN-11 (0.1 μM; 12 h) 促进 HCT-116 细胞中的微管解聚[1]
AKT1-IN-11 (0.1-0.2 μM, 24 h) 浓度依赖性下调 HCT-116 细胞 p-AKT 表达,抑制 AKT 通路激活[1]

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

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.1, 0.2 μM
Incubation Time: 2, 4, 8 and 24 h
Result: Downregulated the expression of phosphorylated AKT1 (p-AKT) in a concentration-dependent manner.
Downregulated the expression of Cyclin B1 and CDK4.
Reduced the levels of E-cadherin and increased the levels of N-cadherin.

Immunofluorescence[1]

Cell Line: HCT-116 cells
Concentration: 0.1 μM
Incubation Time: 12 h
Result: Disrupted microtubule structure.
体内研究
(In Vivo)

AKT1-IN-11 (1-2 mg/kg;腹腔注射;每隔一天一次;共6次) 显著抑制了小鼠 HCT-116 异种移植模型中的肿瘤生长[1]

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

Animal Model: Mice (Male, BALB/c-nu/nu, 6-8 weeks) with subcutaneous injection of HCT-116 cells[1]
Dosage: 1, 2 mg/kg
Administration: Intraperitoneally injection; once every two days; 6 doses
Result: Reduced tumor volumes without causing a significant decrease in body weight.
Reduced the tumor weight-to-body weight ratio.
Reduced the Ki67-positive rate and increased the TUNEL-positive rate.
分子量

692.69

Formula

C33H32N4O11S

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
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  • 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.

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产品名称:
AKT1-IN-11
目录号:
HY-179516
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