ZSW
ZSW is a hexokinase 2 (HK2) inhibitor with human HK2 IC50 of 0.48 μM, human HK2 Ka of 252.00 μM, and selectivity over HK3 and GCK. ZSW binds directly to HK2, inhibits its enzymatic activity, modulates macrophage phenotypes through glycolysis inhibition, and inhibits NF-κB nuclear translocation by preventing IκBα phosphorylation and degradation. ZSW alleviates inflammatory bowel disease (IBD) and improves the intestinal inflammatory state of IBD mice. ZSW can be used for the research of inflammatory bowel disease.
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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: 3124329-46-7
- 分子式: C26H22N4O6S
- 分子量:518.54
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
ZSW (0.5-1 μM; 24 h) dose-dependently inhibits LPS-induced pro-inflammatory cytokine IL-1β and IL-6 gene expression in RAW264.7 mouse macrophages after 24 h co-treatment with 0.5 or 1 μM ZSW[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-stimulated RAW264.7 mouse macrophages
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Concentration:0.5-1 μM
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Incubation Time:24 h
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Result:Significantly reduced LPS-induced upregulation of IL-1β mRNA levels in a dose-dependent manner.
Significantly reduced LPS-induced upregulation of IL-6 mRNA levels in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 7 weeks old, 20-25 g, DSS-induced acute colitis)[1]
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Dosage:10 mg/kg; 20 mg/kg; 30 mg/kg
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Administration:i.p.; daily; 9 days
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Result:Maintained higher body weights than the DSS-only group at study end.
Increased colon length compared to the DSS-only group, with partial restoration toward control levels.
Reduced disease activity index (DAI) scores compared to the DSS-only group.
Improved colonic epithelial integrity, reduced ulceration, preserved goblet cells, and restored organized crypt structure relative to the DSS-only group.
Downregulated splenic iNOS mRNA expression compared to the DSS-only group, with the 20 mg/kg dose showing the strongest reduction.
Suppressed colonic pro-inflammatory IL-1β mRNA expression and upregulated anti-inflammatory IL-10 and Arg-1 mRNA expression compared to the DSS-only group.
Showed no significant differences in spleen, kidney, or liver indices relative to controls, with no obvious liver or kidney toxicity observed via H&E staining.
化学情報
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CAS 番号 3124329-46-7
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分子量 518.54
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分子式 C26H22N4O6S
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SMILES
O=C(C1=CN=CC=C1)/C=C/C2=CN(C3=CC=C(C=C23)N4CCOCC4)S(=O)(C5=CC=CC=C5[N+]([O-])=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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)