PADI4-IN-1
PADI4-IN-1 is a potent peptidylarginine deiminase isoform 4 (PADI4) inhibitor with an IC50 of 1.5 μM and SI (PADI1/PADI4) of 52.1. PADI4-IN-1 can inhibit cellular citrullination events. PADI4-IN-1 can be used for the research of inflammation, such as rheumatoid arthritis.
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。
- 分子式: C21H23NO3
- 分子量:337.41
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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
製品説明
IC50 & Target
[1]|
PADI4 1.5 μM (IC50) |
体外実験
PADI4-IN-1 (Compound 7) (10-100 μM, 50 mins) decreases total cellular citrullination events and histone H3 citrullination mediated by PADI4 in HL-60 cell lysates[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60 cells
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Concentration:10 and 100 μM
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Incubation Time:50 mins
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Result:Decreased total HL-60 cellular citrullination events and histone H3 citrullination mediated by PADI4.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Collagen type II antibody/LPS (HY-D1056) induced rheumatoid arthritis mice models[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneally injection
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Result:Decreased the arthritis score of the mice by 66 % treated at days 4, 5, 6, and 7.
Decreased the arthritis score of the mice by 100 % treated at days 3 and 4.
Reduced the expression of IL-6, IL-1β, IFN-γ, RANKL, IL-17A, CXCL15, ANXA2, HIF-1α, iNOS, and TNF-αtreated at days 3 and 4.
Reduced inflammatory cell influx, pannus formation, cartilage destruction, cartilage remnant, edema, and accumulation of inflammatory cells (mononuclear cells and neutrophil).
Reduced the erosion of cartilage and bone.
Reduced the levels of citrullinated antigens.
化学情報
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分子量 337.41
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分子式 C21H23NO3
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SMILES
COC1=CC2=C(C(OC)=C1)OC3(N(C4=CC=CC=C4C3(C)C)C)C=C2
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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)