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).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 3112325-99-9
- Formel: C21H24N4O4S
- Molecular Weight:428.50
-
Speicherung:
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]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
|
BRD4 7.90 nM (IC50) |
CDK4 |
Bcl-2 |
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.
-
Cell Line:HCT-116 cells
-
Concentration:1.25 μM, 2.5 μM, 5.0 μM
-
Incubation Time:24 h
-
Result:Downregulated the expression of c-MYC, CDK4 and BCL-2 proteins.
Upregulated p21 levels in a dose-dependent manner.
-
Cell Line:HCT-116 cells
-
Concentration:10 μM
-
Incubation Time:72 h
-
Result:Showed 92% inhibition rate against HCT-116 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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].
-
Dosage:25 mg/kg or 50 mg/kg
-
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
-
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.
Chemical Information
-
CAS. Nr. 3112325-99-9
-
Molecular Weight 428.50
-
Formel C21H24N4O4S
-
SMILES
CCS(=O)(NC1=CC(C2=CN(C(C(NC)=C2)=O)C)=C(C=C1)OC3=CN=CC=C3C)=O
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BRD4-IN-12 Related Classifications
HY-181505 Related Classifications
Powered by Bioz