1. Metabolic Enzyme/Protease Cytoskeleton
  2. E1/E2/E3 Enzyme Cadherin
  3. Hakin-1

Hakin-1 是一种 E3 泛素连接酶 Hakai 抑制剂。Hakin-1 可阻断 Hakai 介导的总体泛素化及 E-钙黏蛋白的特异性泛素化,并抑制上皮间质转化 (EMT) 进程。Hakan-1 可抑制肿瘤进展和癌症转移。Hakin-1 可用于研究结直肠癌等癌症。

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Hakin-1

Hakin-1 Chemical Structure

CAS No. : 346660-34-2

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Hakin-1 is a E3 Ubiquitin-Ligase Hakai inhibitor. Hakin-1 blocks Hakai-mediated global ubiquitination and specific ubiquitination of E-cadherin and inhibits epithelial-mesenchymal transition (EMT) progression. Hakan-1 inhibits tumor progression and cancer metastasis. Hakin-1 can be used for the study of carcinoma such as colorectal cancer[1].

体外研究
(In Vitro)

Hakin-1 (10-3000 μM) 对 HT-29、LoVo、MDCK、HaKai-MDCK (clone-4) 和 HaKai-MDCK (clone-11) 细胞活力表现出剂量依赖性抑制作用,IC50 分别为 289.2、159.1、265.6、176.3 和 165.4 μM[1]
Hakin-1 (50-100 μM) 促进 E-cadherin 和 Cortactin 的上调,并下调 Vimentin,但在 HT-29 细胞中 mRNA 水平没有变化[1]
Hakin-1 (50-100 μM,21-28 天) 显著减少 HT-29 和 HaKai-MDCK 细胞癌细胞团块的形成[1]
Hakin-1 (50-100 μM,48 小时) 可降低 HT-29、LoVo 和 HaKai-MDCK 细胞中的细胞侵袭和细胞迁移[1]

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

Cell Migration Assay [1]

Cell Line: HT-29, LoVo and HaKai-MDCK cells
Concentration: 50 and 100 μM
Incubation Time: 24 h
Result: Strongly inhibits the migratory ability of HT-29 cells.

Cell Invasion Assay[1]

Cell Line: HT-29, LoVo and HaKai-MDCK cells
Concentration: 50 and 100 μM
Incubation Time: 24 h
Result: Strongly inhibits the invasive ability of LoVo cells.
体内研究
(In Vivo)

Hakin-1 (5 mg/kg,腹腔注射,每周 3 次,持续 20 天) 可降低 Hakai-MDCK 肿瘤异种移植瘤中的肿瘤生长,该肿瘤移植瘤上 E-钙粘蛋白不表达,并且这种作用伴随着 N-钙粘蛋白间充质标志物表达的降低和肺微转移形成减少[1]

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

Animal Model: Hakai-MDCK induced xenografts model established in six weeks old athymic nu/nu mice[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection (i.p.), 3 times a week for 20 days
Result: Inhibited tumor growth and promoted tumor differentiation.
Significantly reduced the number of Ki67-positive cells, which are markers of tumor proliferation, and the mitotic index.
Significantly reduced the density of blood vessels within the tumor (as indicated by CD31 labeling).
Reduced the level of N-cadherin and increased Cortactin.
Significantly reduced pulmonary micrometastases.
No obvious systemic toxicity.
分子量

385.35

Formula

C16H11N5O5S

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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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.

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Hakin-1
目录号:
HY-176861
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