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

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].

For research use only. We do not sell to patients.

USP7-IN-18 Chemical Structure

USP7-IN-18 Chemical Structure

CAS No. : 3052223-40-9

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USP7-IN-18 Related Antibodies

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DNA Methyltransferase DNMT1 DNMT3 MGMT

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Description

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].

In Vitro

USP7-IN-18 (Compound X21) (1.95-2000 nM, 3 min) binds to the catalytic domain of USP7 with a KD value of 4.9 μM, as determined by SPR analysis[1].

USP7-IN-18 (0.25-1 μM, 24 h) acts as a novel USP7 inhibitor by directly inhibiting enzymatic activity and regulating downstream pathways, including the first-reported target PCLAF[1].

USP7-IN-18 (0.01-100 μM, 72 h) significantly inhibits proliferation of leukemia (RS4;11) and colon cancer (MC38/CT26.WT) cells[1].

USP7-IN-18 (2.5 μM, 0.5 h) exhibits high selectivity for USP7 over eight other deubiquitinases, including USP47 (the most homologous to USP7)[1].

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

USP7-IN-18 Related Antibodies

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.
In Vivo

USP7-IN-18 (Compound X21) (5 mg/kg, 10 mg/kg, i.p., daily for 16 days) shows potent antitumor activity in the MC38 tumor-bearing C57BL/6J mice[1].

MedChemExpress (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.
Molecular Weight

546.08

Formula

C30H28ClN3O3S
CAS No.
SMILES

CC1(C2C(N(C(C21)=O)CC3=CC4=C(C(C5=CC(Cl)=C6C=CC=CC6=C5OC7CCNCC7)=CC=N4)S3)=O)C
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Storage

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Purity & Documentation
References
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USP7-IN-18 Related Classifications

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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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