2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Deubiquitinase DNA Methyltransferase MDM-2/p53
  4. USP7-IN-18

USP7-IN-18 (Compound X21) (0.25-1 μM, 24 h) 作为新型USP7抑制剂，通过直接抑制酶活性和调控下游通路 (包括首次报道的PCLAF靶点)。
USP7-IN-18 (0.01-100 μM, 72 h) 显著抑制白血病 (RS4;11) 和结肠癌 (MC38/CT26.WT) 细胞增殖。
USP7-IN-18 (2.5 μM, 0.5 h) 对 USP7 表现出较高的选择性，优于其他 8 种去泛素化酶。USP7-IN-18 (1.95-2000 nM, 3 min) 经过SPR 分析发现与 USP7 的催化结构域结合，KD值为4.9 μM。

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USP7-IN-18

USP7-IN-18 Chemical Structure

CAS No. : 3052223-40-9

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USP7-IN-18 相关抗体

Top Publications Citing Use of Products

查看 Deubiquitinase 亚型特异性产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

USP7-IN-18 is a naphthalene derivative. USP7-IN-18 is a selective USP7 inhibitor (IC50 : 130.9 nM), with no or very weak inhibition of the other 8 DUBs including USP47. USP7-IN-18 specifically binds to the catalytic domain of USP7, blocking its deubiquitinase activity. USP7-IN-18 causes degradation of the oncogenic proteins MDM2 and DNMT1, and also degrades the novel target PCLAF. USP7-IN-18 activates the p53-p21 pathway. USP7-IN-18 exerts anti-tumor effects in colon cancer animal models and reshapes the tumor immune microenvironment. USP7-IN-18 achieves both direct cytotoxic and immune-synergistic anti-tumor actions[1].

体外研究
(In Vitro)

USP7-IN-18 (1.95-2000 nM, 3 min) 经过 SPR 分析发现与 USP7 的催化结构域结合，KD值为4.9 μM[1]。

USP7-IN-18 (Compound X21) (0.25-1 μM, 24 h) 作为新型 USP7 抑制剂，通过直接抑制酶活性和调控下游通路 (包括首次报道的 PCLAF 靶点)[1]。

USP7-IN-18 (0.01-100 μM, 72 h) 显著抑制白血病 (RS4;11) 和结肠癌 (MC38/CT26.WT) 细胞增殖[1]。

USP7-IN-18 (2.5 μM, 0.5 h) 对 USP7 表现出较高的选择性，优于其他 8 种去泛素化酶[1]。

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

USP7-IN-18 相关抗体:

Cell Viability Assay[1]

Cell Line: RS4; 11 cells, MC38 cells, CT26.WT cells
Concentration: 0.01-100 μM in RS4; 11 cells, 0.5-100 μM in MC38 cells and CT26.WT cells
Incubation Time: 72 h
Result: Demonstrated antiproliferative activity against the human leukemia RS4; 11 cell line with an IC50 value of 0.65 μM.
Exhibited antiproliferative activity against MC38 and CT26.WT mouse colon cancer cell lines with IC50 values of 2.93 μM and 2.89 μM, respectively.

Western Blot Analysis[1]

Cell Line: RS4; 11 cells
Concentration: 0.25 μM, 0.5 μM, 1 μM
Incubation Time: 24 h
Result: Demonstrated downregulation of DNMT1, UHRF1, MDM2, TRIM27, and PCLAF, with concurrent upregulation of p53 and p21.
Significantly reduced PCLAF protein levels.
Slightly reduced USP7 protein levels.
体内研究
(In Vivo)

USP7-IN-18 (Compound X21) (5 mg/kg, 10 mg/kg, i.p., 每日一次, 持续16天) 在携带 MC38 肿瘤的 C57BL/6J 小鼠模型中显著抑制肿瘤生长[1]。

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

Animal Model: MC38 tumor-bearing C57BL/6J female mice (8 weeks)[1].
Dosage: 5 mg/kg, 10 mg/kg
Administration: Daily intraperitoneal injection (i.p.), at the corresponding doses for 16 days.
Result: Demonstrated significant tumor growth inhibition (TGI = 58.2%) at 10 mg/kg on day 16, while showing weaker efficacy at 5 mg/kg, indicating dose-dependent antitumor activity.
Significantly reduced tumor mass in immunocompetent mice, confirming effective tumor growth suppression.
Caused transient body weight loss due to initial stress response, with subsequent recovery observed in later stages.
Animal Model: MC38 tumor-bearing BALB/c female mice (8 weeks)[1].
Dosage: 10 mg/kg
Administration: Daily intraperitoneal injection (i.p.), at the corresponding doses for 16 days.
Result: Demonstrated 19.24% tumor growth inhibition (TGI) without statistical significance and caused no body weight changes in mice.
Exhibited significantly attenuated antitumor efficacy in immunodeficient mice, suggesting immune microenvironment-dependent therapeutic activity.
Demonstrated significantly increased proportions of CD8+ T cells and elevated CD8+/CD4+ ratios, while exhibiting upward trends in NK cell proportions with unchanged Tregs/MDSCs ratios, collectively indicating tumor immune microenvironment remodeling.
分子量

546.08

Formula

C30H28ClN3O3S
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

USP7-IN-18 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:

USP7-IN-183052223-40-9DeubiquitinaseDNA MethyltransferaseMDM-2/p53DUBsDNMTsDNA MTasesUSP7Colon CancerAcute LeukemiaPCLAFC57BL/6J miceBALB/c nude miceRS4;11 cellsMC38 cellsCT26.WT cellsAntiproliferative activityInhibitorinhibitorinhibit

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