2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. USP25/28-IN-2

USP25/28-IN-2 (compound AZ2) 是一种选择性双重 USP25/USP28 抑制剂，其 USP28 IC50 值为 0.9 μM、USP28 Ka 值为 0.9 μM、USP25 IC50 值为 0.88 μM。USP25/28-IN-2 可调控 USP25 和 USP28 的活性以影响下游通路，调节 c-Myc 癌蛋白的总水平与半衰期，诱导细胞凋亡并降低细胞活力。USP25/28-IN-2 可用于结直肠癌、结直肠腺癌的相关研究。

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USP25/28-IN-2

USP25/28-IN-2 Chemical Structure

CAS No. : 2165322-95-0

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USP25/28-IN-2 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

USP25/28-IN-2 (compound AZ2) is a selectivity dual USP25/USP28 inhibitor with USP28 IC50 values of 0.9 μM, USP28 Ka values of 0.9 μM, and USP25 IC50 values of 0.88 μM. USP25/28-IN-2 modulates USP25 and USP28 activity to affect downstream pathways, modulates c-Myc oncoprotein total levels and half-life, induces apoptosis, reduces cell viability. USP25/28-IN-2 can be used for the research of colorectal carcinoma, colorectal adenocarcinoma[1].

体外研究
(In Vitro)

USP25/28-IN-2 (compound AZ2) (滴定范围) 可在多种荧光底物分析中强效抑制纯化的重组 USP28 酶活性，其 IC50 值范围为 0.9 至 1.3 μM[1]。
USP25/28-IN-2 (AZ2) (titration range; 10 μM) 可在荧光底物分析中强效抑制纯化的重组 USP25 酶活性，其 IC50 为 0.88 μM[1]。
USP25/28-IN-2 (AZ2) (200 μM) 可特异性、可逆地结合纯化的重组 USP28 蛋白，通过 ITC 测得其 Kd 值为 0.9 μM[1]。
USP25/28-IN-2 (AZ2) (titration range) 可特异性结合纯化的重组 USP28 蛋白，通过 MST 检测[1]得到其 Kd 为 10.3 μM。
USP25/28-IN-2 (AZ2) (0.01-60 μM; 2 h) 可与 HCT116 细胞中的内源性 USP28 结合，通过 Ub-VS 探针竞争实验测得其 EC50 为 18.2 μM[1]。
USP25/28-IN-2 (AZ2) (0.01-60 μM; 2 h) 可与 HCT116 细胞中的内源性 USP25 结合，通过 Ub-VS 探针竞争实验测得其 EC50 为 11.5 μM[1]。
USP25/28-IN-2 (AZ2) (0-100 μM; 3 h) 可呈剂量依赖性降低 HCT116 细胞中内源性总 c-Myc 蛋白水平[1]。
USP25/28-IN-2 (AZ2) (0-100 μM; 3 h) 经 3 小时处理后可剂量依赖性地诱导 HCT116 细胞发生凋亡，该效应通过 PARP 切割实验检测[1]。
USP25/28-IN-2 (AZ2) (0-100 μM; 72 h) 在处理 72 h 后，在多种癌细胞系 (包括 HCT116、HT29 和 SW480) 及组织匹配的正常细胞系中发挥剂量依赖性的抗增殖作用，其中癌细胞的 EC50 值集中在 20 μM 左右，正常细胞的 EC50 值为 28 μM[1]。

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

USP25/28-IN-2 相关抗体:

Western Blot Analysis[1]

Cell Line: HCT116 colon carcinoma cells
Concentration: 0-100 μM
Incubation Time: 3 h
Result: Dose-dependently reduced endogenous total c-Myc protein levels, with complete reduction observed at the highest concentrations tested.
Left USP28 protein levels unchanged (confirming no general protein degradation).

Apoptosis Analysis[1]

Cell Line: HCT116 colon carcinoma cells
Concentration: 0-100 μM
Incubation Time: 3 h
Result: Dose-dependently induced PARP cleavage, with cleavage most pronounced following complete down-regulation of c-Myc.
Showed no PARP cleavage at lower concentrations where c-Myc levels were not fully reduced.

Cell Viability Assay[1]

Cell Line: HCT116 colon carcinoma cells, HT29 colorectal adenocarcinoma cells, SW480 colorectal adenocarcinoma cells, 21 cancer cell line panel, 7 tissue-matched normal cell line panel
Concentration: 0-100 μM (in ½ log unit increments)
Incubation Time: 72 h
Result: Reduced cell viability in HCT116 cells with an EC50 in the 18.0-20.0 μM range.
Exhibited similar dose-dependent anti-proliferative activity in HT29 and SW480 cells.
Reduced cell viability across the 21 cancer cell line panel with EC50 values clustered around 20 μM.
Reduced cell viability across the 7 normal cell line panel with EC50 values clustered around 28 μM, showing a minimal therapeutic window.
分子量

420.23

Formula

C17H17BrF3NO3
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

USP25/28-IN-2 相关分类

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  • 稀释计算器

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  • 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:

USP25/28-IN-22165322-95-0DeubiquitinaseDUBscolorectal carcinomaSW480 cellsc-Myc oncoproteinHT29 cellscolorectal adenocarcinomaUSP25deubiquitinasesapoptosisUSP28HCT116 cellsInhibitorinhibitorinhibit

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