2. Cell Cycle/DNA Damage Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Deubiquitinase Ferroptosis Reactive Oxygen Species (ROS) Glutathione Peroxidase
  4. USP30-IN-20

USP30-IN-20 是一种具有口服活性的 USP30 抑制剂 (Kd = 1.61 μM，IC50 = 12.8 μM)。USP30-IN-20 通过促进 GPX4 的泛素化介导降解诱导铁死亡 (ferroptosis)。USP30-IN-20 抑制前列腺癌细胞的增殖、迁移、侵袭能力。USP30-IN-20 诱导前列腺癌细胞的 G0/G1 期阻滞并升高 ROS 水平。USP30-IN-20 在小鼠 PC3 细胞皮下异种移植模型中显示出显著抗肿瘤活性。USP30-IN-20 可用于晚期前列腺癌研究。

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USP30-IN-20

USP30-IN-20 Chemical Structure

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USP30-IN-20 相关抗体

Top Publications Citing Use of Products

查看 Deubiquitinase 亚型特异性产品:

查看所有亚型
USP1 USP2 USP7 USP8 USP10 USP30 UCHL1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

USP30-IN-20 is an orally active USP30 inhibitor (Kd = 1.61 μM, IC50 = 12.8 μM). USP30-IN-20 induces ferroptosis by promoting ubiquitination-mediated degradation of GPX4. USP30-IN-20 inhibits the proliferation, migration, invasion, and stemness of prostate cancer cells. USP30-IN-20 induces G0/G1 cell cycle arrest and ROS levels in prostate cancer cells. USP30-IN-20 exhibits significant anti-tumor efficacy in PC3 cell subcutaneous xenografts in mice. USP30-IN-20 can be used for the study of advanced prostate cancer[1].

IC50 & Target[1]

USP30

1.61 μM (Kd)

USP30

12.8 μM (IC50)

体外研究
(In Vitro)

USP30-IN-20 (Compound 8m) 对 PC3、DU145 前列腺癌细胞及 CD24-CD44+ 前列腺癌干样细胞表现出显著抗增殖活性，IC50 分别为 4.87 μM、5.44 μM 和 5.94 μM[1]。
USP30-IN-20 (2.5-5 μM, 14 days) 显著减少 PC3 和 DU145 细胞的恶性克隆数量[1]。
USP30-IN-20 (2.5-5 μM, 24-48 h) 诱导 PC3 和 DU145 细胞 G0/G1 期阻滞，抑制迁移并降低侵袭能力[1]。
USP30-IN-20 (2.5-5 μM, 72 h) 干扰肿瘤球形成，显著减少 PC3 和 DU145 细胞的球体数量[1]。
USP30-IN-20 (2.5-5 μM, 24 h) 显著上调 PC3 和 DU145 细胞内 ROS 及脂质 ROS 水平，增加丙二醛 (MDA) 含量并降低谷胱甘肽 (GSH) 水平[1]。
USP30-IN-20 (5 μM, 24 h) 使 PC3 细胞线粒体缩小，线粒体嵴和膜结构消失，并破坏线粒体膜电位，但不影响细胞凋亡[1]。
USP30-IN-20 (2.5-5 μM; 24 h) 以剂量依赖方式下调 PC3 和 DU145 细胞中 GPX4 蛋白表达[1]。

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

USP30-IN-20 相关抗体:

Cell Invasion Assay[1]

Cell Line: PC3 and DU145 cells
Concentration: 2.5, 5 μM
Incubation Time: 24 h
Result: Suppressed the invasion capacity of PC3 and DU145 cells.
体内研究
(In Vivo)

USP30-IN-20 (Compound 8m) (25-50 mg/kg, 口服, 每日一次，连续 18 天) 显著抑制裸鼠体内 PC3 前列腺癌异种移植瘤的增殖[1]。

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

Animal Model: PC3 prostate cancer cells (1 × 107 cells) were subcutaneously implanted into the flanks of 6-8-week-old male athymic nude mice (BALB/c strain)[1]
Dosage: 25, 50 mg/kg
Administration: p.o., daily, 18 days
Result: Achieved significant tumor growth inhibition in male athymic nude mice.
Showed no significant changes in body weight.
分子量

353.70

Formula

C16H15ClO2Se
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

USP30-IN-20 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

USP30-IN-20DeubiquitinaseFerroptosisReactive Oxygen Species (ROS)Glutathione PeroxidaseDUBsprostate cancerROSUSP30GPX4ferroptosisInhibitorinhibitorinhibit

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