BRD4 Inhibitor-38
BRD4 Inhibitor-38 (Compound 25) is an orally active inhibitor of BRD4 with IC50 values of 3.64 μM and 0.12 μM against BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-38 also exhibits anti-inflammatory activity, with an IC50 value of 1.98 μM for inhibiting nitric oxide (NO) production.
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- 分子式: C19H18N2O4
- 分子量:338.36
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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BRD4 BD1 3.64 μM (IC50) |
BRD4 BD2 0.12 μM (IC50) |
BRD4 Inhibitor-38 (Compound 25) (2.5-20 μM; 2 h) exhibits anti-inflammatory activity in Raw 264.7 and THP-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Raw 264.7, THP-1
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Concentration:2.5, 5, 10, 20 μM
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Incubation Time:2 h (stimulated with LPS (1 μg/mL) and LPS (100 ng/mL) + IFN-γ (20 ng/mL) for 6 h. note: Compound 25 were pre-treated for 2 h before stimulating with LPS for 6 h.)
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Result:Inhibited the mRNA expression of LPS-induced IL-6 and TNF-α in a dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS-induced mouse model of acute inflammation[1].
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Dosage:25, 50, 100 mg/kg
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Administration:Oral administration (p.o.)，single dose. After LPS treatment (10mg/kg; Single dose)
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Result:Significantly inhibited the increase of inflammatory genes IL-6 and TNF-α at doses of 50 and 100 mg/kg. Alleviated lung tissue edema, damage, and lung hemorrhage. Mitigated kidney damage, significantly increased the proportion of normal renal tubules, improved the internal brush border structure, reduced renal interstitial inflammatory cell infiltration, and decreased the number of interstitial vacuoles at a dose of 100 mg/kg.
化学情報
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分子量 338.36
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分子式 C19H18N2O4
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SMILES
COC1=C2C(N=C(/C=C/C3=CC=C(OC)C=C3)NC2=O)=CC(OC)=C1
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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)
BRD4 Inhibitor-38 関連分類
HY-170686 関連分類
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