BRD4-IN-12
BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC50 of 7.9 nM. BRD4-IN-12 downregulates the expression of c-MYC, BCL-2, CDK4 and upregulates p21. BRD4-IN-12 inhibits tumor cell proliferation and promotes apoptosis. BRD4-IN-12 exhibits excellent antitumor effects in the HCT-116 colorectal cancer xenograft model. BRD4-IN-12 can be used for the study of colorectal cancer (CRC).
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- No. CAS: 3112325-99-9
- Fòrmula: C21H24N4O4S
- Peso molecular:428.50
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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- Pureza y Documentación
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
BRD4 7.90 nM (IC50) |
CDK4 |
Bcl-2 |
In Vitro
BRD4-IN-12 (H5) (72 h) shows cytotoxicity against HCT-116 colorectal cancer cells with an IC50 value of 0.84 μM, the cytotoxicity of BRD4-IN-12 induced in HCT-116 cells is BRD4-dependent[1].
BRD4-IN-12 (1.25-5.0 μM; 24 h) downregulates the protein expression of c-MYC, CDK4 and BCL-2, and dose-dependently upregulates the protein expression of p21 in HCT-116 cells[1].
BRD4-IN-12 (20 μM; 3 h) stabilizes BRD4 protein in HCT-116 cell lysates, confirming its intracellular binding to BRD4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 cells
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Concentration:1.25 μM, 2.5 μM, 5.0 μM
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Incubation Time:24 h
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Result:Downregulated the expression of c-MYC, CDK4 and BCL-2 proteins.
Upregulated p21 levels in a dose-dependent manner.
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Cell Line:HCT-116 cells
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Concentration:10 μM
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Incubation Time:72 h
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Result:Showed 92% inhibition rate against HCT-116 cells.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c nude mice (4-6 weeks old, 18-22 g) were subcutaneously inoculated with HCT-116 cells (5 × 106 cells/mL)[1].
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Dosage:25 mg/kg or 50 mg/kg
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Administration:Dissolved in vehicle containing 5% ethanol, 40% PEG 400, 5% Tween 80, and 50% water; Oral (p.o.) administration; once daily; for 18 days
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Result:Both doses maintained stable body weight and caused no obvious pathological damage to major organs (heart, liver, spleen, lung, kidney).
Both doses downregulated the expression of c-MYC and BCL-2 in tumor tissues and induced increased cell spacing, smaller and rounded nuclei in tumor tissues (H&E staining).
The 25 mg/kg dose exhibited 52% tumor growth inhibition (TGI) without significant body weight loss.
The 50 mg/kg dose achieved 82% tumor growth inhibition (TGI) and downregulated the expression of c-MYC and BCL-2 in tumor tissues.
- RNA extraction experimental
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- MTT Cell Proliferation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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No. CAS 3112325-99-9
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Peso molecular 428.50
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Fòrmula C21H24N4O4S
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SMILES
CCS(=O)(NC1=CC(C2=CN(C(C(NC)=C2)=O)C)=C(C=C1)OC3=CN=CC=C3C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BRD4-IN-12 Related Classifications
HY-181505 Related Classifications
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