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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3052223-40-9
- 分子式: C30H28ClN3O3S
- 分子量:546.08
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
DNA Methyltransferase アイソフォーム固有の製品をすべて表示
More
生物活性
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.
-
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.
-
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.
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.
化学情報
-
CAS 番号 3052223-40-9
-
分子量 546.08
-
分子式 C30H28ClN3O3S
-
SMILES
CC1(C2C(N(C(C21)=O)CC3=CC4=C(C(C5=CC(Cl)=C6C=CC=CC6=C5OC7CCNCC7)=CC=N4)S3)=O)C
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Powered by Bioz