BRD4-IN-11
BRD4-IN-11 is an orally active and selective BRD4 inhibitor (IC50 = 26.35 nM (BD1), IC50 = 72.81 nM (BD2)). BRD4-IN-11 is approximately 3- to 18-fold more potent against BRD4 than againstBRD2, BRD3, and BRDT. BRD4-IN-11 enhances H2S release and inhibits the upregulation of fibrotic markers (α-SMA and fibronectin), c-Myc, and CDC25B. BRD4-IN-11 reduces apoptosis in LO2 hepatocytes. BRD4-IN-11 significantly improves liver and lung function in a hepatopulmonary fibrosis model and can be used to study hepatopulmonary fibrosis.
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- 화학식: C40H37ClN4O5S3
- 분자량:785.39
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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BRD4 (BD1) 26.35 nM (IC50) |
BRD4 (BD2) 72.81 nM (IC50) |
BRD4-IN-11 (Compound 11r) exhibits inhibition of LX-2 cells[1].
BRD4-IN-11 (0.5-2.0 μM, 48 h) reduces the apoptosis rate, inhibits the expression of CDC25B, α-SMA, and c-Myc, and fibronectin in Carbon tetrachloride (CCl4) (HY-Y0298)-treated LO2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BRD4-IN-11 (15-30 mg/kg, p.o., once a day, 15 days) prevents lung fibrosis in Bleomycin (BLM) (HY-108345) induced pulmonary fibrosis (PF) model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CCl4-induced (1 mg/kg, i.p.) male C57BL/6J mice (6-7weeks old) hepatic fibrosis model[1]
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Dosage:15 mg/kg, 30 mg/kg
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Administration:p.o., once a day, 3 days
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Result:Alleviated CCl4-induced liver fibrosis, reduced collagen deposition in liver tissue and the increased expression of fibrosis biomarkers (type I collagen and α-SMA) in CCl4-treated mice, and alleviated CCl4-induced massive hepatocyte apoptosis.
Reduced liver weight coefficient and AST, ALT and TG levels at 30 mg/kg.
Had a safer and more effective ameliorative effect on CCl4-induced organ toxicity than JQ-1 (HY-78695), and that high dose is more effective than low dose.
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Animal Model:BLM-induced (2 mg/kg, injected into the trachea) male C57BL/6J mice (6-7weeks old) PF model[1]
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Dosage:15 mg/kg, 30 mg/kg
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Administration:p.o., once a day, 15 days
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Result:Reduced lung coefficient (lung weight/body weight ratio) and hydroxyproline content (a specific marker of collagen deposition and fibrosis severity), indicating effective attenuation of fibrosis at the molecular level.
Reduced inflammatory cell infiltration, decreased collagen deposition in lung tissue, and suppressed the expression of key fibrosis markers (i.e., collagen I and α-SMA) in BLM-injured lung tissue.
Chemical Information
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분자량 785.39
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화학식 C40H37ClN4O5S3
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SMILES
CC1=NN=C2[C@@H](N=C(C3=C(N12)SC(C)=C3C)C4=CC=C(C=C4)Cl)CC(OC5=CC=C(C=C5)OCCCCCCOC6=CC=C(C=C6)C7=CC(SS7)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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