2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. Skp2-IN-4

Skp2-IN-4 是一种 Skp2 抑制剂，对 Skp2-Cks1 结合的 IC50 为 0.38 μM。Skp2-IN-4 增强抗肿瘤活性，通过靶向 Skp2，抑制肿瘤增殖并诱导 S 期细胞阻滞。Skp2-IN-4 通过抑制肿瘤细胞干性，显著增强 NCl-H1299 异种移植小鼠模型中对 Cisplatin (HY-17394) 的化疗敏感性，具有肺癌和食道癌研究潜力。

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Skp2-IN-4 Chemical Structure

Skp2-IN-4 Chemical Structure

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Skp2-IN-4 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Skp2-IN-4 is an Skp2 inhibitor with a IC50 of 0.38  μM for Skp2-Cks1 binding. Skp2-IN-4 improves anti-tumor activity, inhibits the proliferation and induces S phase arrest by targeting Skp2. Skp2-IN-4 significantly enhances Cisplatin (HY-17394) chemosensitivity by suppressing the tumor cell stemness in NCl-H1299 xenograft mice model, promising for lung cancer and esophageal cancer research[1].

体外研究
(In Vitro)

Skp2-IN-4 (Compound 10 h) 可有效抑制肿瘤活性，对肺癌细胞 NCl-H1299 和食管癌细胞 KYSE-510 的 IC50 分别为 11.24 μM 和 10.32 μM[1]。
Skp2-IN-4 (4 h) 在 57-68 °C 的温度范围内提高了对 Skp2 蛋白的稳定性，并干扰 KYSE-510 和 NCl-H1299 细胞中 Skp2 和 Cks1 的结合[1]。
Skp2-IN-4 (2.5-10 μM，1-10 天) 以剂量依赖性方式抑制 KYSE-510 和 NCl-H1299 细胞中的细胞集落形成和 DNA 合成[1]。
Skp2-IN-4 (5-15 μM，48 小时) 以剂量依赖性方式降低 KYSE-510 和 NCl-H1299 细胞中 Skp2 表达，诱导其底物 (p21 和 p27) 在细胞中积累，并将细胞周期停滞于 S 期，且在 10 μM 浓度下效果更显著[1]。
Skp2-IN-4 (10 μM，48 小时) 与 Cisplatin 联合使用，可显著抑制 NCl-H1299 细胞中的球体形成和细胞克隆形成，诱导 G2/M 期细胞停滞和细胞凋亡，并抑制 CD44、Nanog、OCT4 和 SOX2 (肿瘤干性标志物) 的蛋白水平[1]。

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

Skp2-IN-4 相关抗体:

Immunofluorescence[1]

Cell Line: KYSE-510 cells, NCl-H1299 cells
Concentration: 5, 10, 15 μM
Incubation Time: 48 h
Result: Significantly downregulated the expression of Skp2 in a dose-dependent manner in KYSE-510 and NCl-H1299 cells.
Increased the intracellular levels of p21 and p27 (substrates) in a dose-dependent manner in KYSE-510 and NCl-H1299 cells.

Western Blot Analysis[1]

Cell Line: KYSE-510 cells, NCl-H1299 cells
Concentration: 5, 10, 15 μM
Incubation Time: 48 h
Result: Dose-dependently decreased the protein level of Skp2 but significantly increased the p21 and p27 expression in KYSE-510 and NCl-H1299 cells.

Cell Cycle Analysis[1]

Cell Line: KYSE-510 cells, NCl-H1299 cells
Concentration: 5, 10, 15 μM or 12.5 μg/mL Cisplatin
Incubation Time: 48 h
Result: Induced a dose-dependent S phase arrest in KYSE-510 and NCl-H1299 cells.
Caused in a substantial cell cycle blockade with the S phase cell population from 17.51% to 41.92% in KYSE-510 cells as well as similar result in NCl-H1299 cells.
Significantly induced G2/M-phase cell cycle arrest at 10 μM with combination of Cisplatin in NCl-H1299 cells.

Cell Proliferation Assay[1]

Cell Line: KYSE-510 cells, NCl-H1299 cells
Concentration: 2, 5, 10 μM
Incubation Time: 7 days
Result: Effectively inhibited cell colony formation in a concentration-dependently manner.
体内研究
(In Vivo)

Skp2-IN-4 (Compound 10 h) (25 mg/kg，口服，每 2 天一次，持续 20 天) 可增强 NCl-H1299 异种移植小鼠模型中 NCl-H1299 细胞对 Cisplatin 的化学敏感性，并有效抑制肿瘤生长[1]。

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

Animal Model: NOD-SCID mice (6 weeks old) were injected into the right axilla with NCl-H1299 cells (1 × 107 cells/mouse)[1].
Dosage: 25  mg/kg or Cisplatin (5 mg/kg)
Administration: Oral gavage (p.o.), Cisplatin (i.p.), every 2 day for 20 days and then collected tumors and major organ tissues.
Result: Significantly inhibited tumor growth, and reduced tumor volume and weight with combination of Cisplatin in NCl-H1299 xenograft mice model.
Induced no obvious toxicity with combination of Cisplatin in NCl-H1299 xenograft mice model.
分子量

377.44

Formula

C24H19N5
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

Skp2-IN-4 相关分类

  • 摩尔计算器

  • 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.

Keywords:

Skp2-IN-4E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseS-phase kinase-associated protein 2Skp2ChemosensitivityNCl-H1299 cellsKYSE-510 cellsNCl-H1299 xenograft mice modelInhibitorinhibitorinhibit

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