2. PI3K/Akt/mTOR Apoptosis Cell Cycle/DNA Damage Epigenetics Stem Cell/Wnt
  3. Akt Apoptosis Caspase PARP β-catenin
  4. AKT-IN-28

AKT-IN-28 是一种 Akt 变构抑制剂，是 Shikonin (HY-N0822) 的衍生物。AKT-IN-28 通过疏水和氢键相互作用有效结合 Akt 的变构位点，Kd 值为 2.07 μM。AKT-IN-28 显著抑制 Akt 活性，诱导 KRAS 突变型结直肠癌细胞中的细胞凋亡 (apoptosis)，将细胞周期阻滞于 G2/M 期，并抑制细胞增殖、迁移和代谢。

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AKT-IN-28 Chemical Structure

AKT-IN-28 Chemical Structure

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AKT-IN-28 相关抗体

Top Publications Citing Use of Products

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

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

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AKT-IN-28 is an Akt allosteric inhibitor, a derivative of Shikonin (HY-N0822). AKT-IN-28 effectively binds to the allosteric site of Akt through hydrophobic and hydrogen interactions with Kd of 2.07 μM. AKT-IN-28 significantly inhibits Akt activity, induces cell apoptosis, arrests cell cycle in G2/M phase, and suppresses proliferation, migration and metabolism of KRAS mutant colorectal cancer cells[1].

IC50 & Target

Caspase 3

 

PARP

 

Akt

2.07 μM (Kd)

体外研究
(In Vitro)

AKT-IN-28 (Compound L8) 具有强效的抗增殖活性 (对 HCT-8、HCT-116、PC-3、MDA-MB-231 和 HeLa 细胞的 IC50 分别为 4.51、4.57、5.07、8.94 和 6.59 μM)，对正常细胞的细胞毒性较低 (对 MCF-10A 和 HCoEpiC 细胞的 IC50 分别为 > 100  和 67 μM) [1]。
AKT-IN-28 (1-4 μM，24 小时) 剂量依赖性地降低 HCT-8 和 HCT-116 细胞中 Akt 酶活性，并显著抑制总 Akt、p-Akt、PARP 和 β-catenin 的蛋白表达、细胞增殖活性和迁移，但是增加 cleaved-PARP 蛋白水平[1]。
AKT-IN-28 (0.25-1 μM，7 天) 显著抑制结肠癌细胞活力，减少 HCT-116 细胞集落形成[1]。
AKT-IN-28 (2-8 μM，24 小时) 有效诱导 HCT-116 和 HCT-8 细胞中的细胞凋亡，并将细胞周期停滞在 G2/M 期 (8 μM)，降低周期相关蛋白 CDH1、CDK1 和 CDC20，并升高 caspase3 活性[1]。
AKT-IN-28 (2-8 μM，2-24 小时) 显著降低 HCT-116 细胞中的葡萄糖消耗、乳酸生成和 ATP 水平[1]。

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

AKT-IN-28 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCT-116 cells
Concentration: 1, 2, 4 μM
Incubation Time: 24 h
Result: Significantly reduced the percentage of EdU-positive cells.

Cell Migration Assay [1]

Cell Line: HCT-8 cells, HCT-116 cells
Concentration: 1, 2, 4 μM
Incubation Time: 3, 6, 12, 24 h
Result: Significantly reduced the number of metastasis colon cancer cells and enlarged the space area of migrating cells.

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 1, 2, 4 μM
Incubation Time: 24 h
Result: Significantly inhibited the total Akt, p-Akt, PARP and β-catenin protein expression but increased cleaved-PARP protein level.
Obviously decreased the expression levels of cycle-related proteins CDH1, CDK1, and CDC20.

Cell Cycle Analysis[1]

Cell Line: HCT-8 cells, HCT-116 cells
Concentration: 2, 4, 8 μM
Incubation Time: 24 h
Result: Arrested the cell cycle at G2/M phase at 8 μM in HCT-8 and HCT-116 cells.

Apoptosis Analysis[1]

Cell Line: HCT-8 cells, HCT-116 cells
Concentration: 2, 4, 8 μM
Incubation Time: 24 h
Result: Effectively induced cell apoptosis in HCT-8 and HCT-116 cells.
分子量

573.57

Formula

C32H28FNO8
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

AKT-IN-28 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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× = ×
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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:

AKT-IN-28AktApoptosisCaspasePARPβ-cateninPKBProtein kinase Bpoly ADP ribose polymerase Beta cateninAllosteric inhibitorAnticancerShikoninHCT-8 cellsHCT-116 cellsInhibitorinhibitorinhibit

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