1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. Huib32

Huib32 是一种高效的小分子 USP32 抑制剂 (IC50 = 21.2 nM),相较于其他密切相关的去泛素化酶 (DUBs) (例如 USP8/10/16、UCHL1 和 OTUB2) 具有高选择性。Huib32 通过可逆地共价结合活性位点 Cys743 来抑制 USP32,从而增强底物的泛素化水平、改变内体形态,并模拟 USP32 敲除的表型。Huib32 可用于乳腺癌、卵巢癌、肺癌,阿尔茨海默病和帕金森病的相关研究。

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Huib32

Huib32 Chemical Structure

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查看 Deubiquitinase 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

Huib32 is a potent small-molecule inhibitor of USP32 (IC50 = 21.2 nM), exhibiting high selectivity over other closely related deubiquitinating enzymes (DUBs), such as USP8/10/16, UCHL1 and OTUB2. Huib32 reversibly inhibits USP32 by covalently binding to the active site Cys743, which enhances substrate ubiquitination, alters endosomal morphology, and mimics USP32 depletion. Huib32 can be used for breast, ovarian, and lung cancer and Alzheimer's and Parkinson’s diseases research[1].

IC50 & Target[1]

USP32

21.2 nM (IC50)

体外研究
(In Vitro)

Huib32 (BB01CA282) (0-50 μM,6-24 小时) 以剂量依赖的方式选择性抑制 USP32FL 和 USP32CD (从 0.1 μM 开始),对其他 16 种检测到的去泛素化酶 (DUB) 无显著影响[1]
Huib32 (0-50 μM, 24 小时) 在 MelJuSo 细胞中表现出强效、剂量依赖性的内源性 USP32 靶点占位能力 (IC50 ~0.1 μM),证实了其细胞通透性及细胞内靶向活性[1]
Huib32 (10 μM,4-72 小时) 诱导晚期内体分散,并增强 RAB7 和其他底物 (例如 RAB6、RAB32、RAB11A/B、TMEM192) 的泛素化,证实了其在膜转运中的作用,并揭示了 USP32 的新潜在底物[1]
Huib32 (10 μM, 4-72 小时) 显著改变了泛素组修饰谱,在 4 小时和 72 小时富集和消耗独特的 Lys-ε-Gly-Gly 肽,影响包括 RAB11A/B 与 USP32 自身在内的底物,且不改变其总蛋白水平,表明其调控方式为非降解性泛素化[1]
Huib32 (10 μM, 72 小时) 特异性增强了 GFP-RAB7 WT 的泛素化,但对 GFP-RAB7 2KR 突变体无影响,验证了其对已确认的 USP32 底物的靶向作用[1]

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

Western Blot Analysis[1]

Cell Line: MelJuSo cells
Concentration: 0, 0.1, 0.5, 1, 5, 10, and 50 μM
Incubation Time: 4, 24 and 72 h
Result: Strongly increased the ubiquitination of RAB7 after 4 h of incubation in MelJuSo cells stably expressing GFP-RAB7, which steadily stayed up to 72 h of incubation.
Approximately 2-fold increase in RAB7 ubiquitination was observed in GFP-RAB7 WT, but not in the ubiquitination-deficient mutant GFP-RAB7 2KR.

Immunofluorescence[1]

Cell Line: MelJuSo cells
Concentration: 0, 5 and 10 μM
Incubation Time: 72 h
Result: Induced dispersion and swelling of the late endosomal compartments, a phenotype consistent with USP32 depletion.
分子量

381.45

Formula

C16H23N5O4S

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
  • 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)

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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.

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产品名称:
Huib32
目录号:
HY-178124
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