2. Epigenetics Apoptosis Cytoskeleton Cell Cycle/DNA Damage
  3. Epigenetic Reader Domain c-Myc Bcl-2 Family PAK Apoptosis
  4. 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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BRD4-IN-12

BRD4-IN-12 Chemical Structure

CAS No. : 3112325-99-9

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BRD4-IN-12 Related Antibodies

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Description

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)[1].

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.

BRD4-IN-12 Related Antibodies

Western Blot Analysis[1]

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 Viability Assay[1]

Cell Line: HCT-116 cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Showed 92% inhibition rate against HCT-116 cells.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-inf CL Vz F
Mice[1] 2 mg/kg i.v. 0.29 h - h - ng/mL 456 ng·h/mL 458 ng·h/mL 73.8 mL/min/kg 1.20 L/kg - %
Mice[1] 25 mg/kg p.o. 1.49 h 0.333 h 81.3 ng/mL 86.0 ng·h/mL 95.9 ng·h/mL - mL/min/kg - L/kg 1.51 %
In Vivo

BRD4-IN-12 (H5) (25 mg/kg or 50 mg/kg; p.o.; once a day; for 18 days) exhibits 52% and 82% tumor growth inhibition (TGI) at 25 mg/kg and 50 mg/kg, respectively, in male BALB/c nude mice bearing HCT-116 colorectal cancer xenografts; maintains stable body weight and causes no significant pathological damage to major organs (heart, liver, spleen, lung, kidney); and downregulates the expression of c-MYC and BCL-2 in tumor tissues; induces increased cell spacing, smaller and rounded nuclei in tumor tissues of male BALB/c nude mice with HCT-116 colorectal cancer xenografts[1].

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.
Molecular Weight

428.50

Formula

C21H24N4O4S
CAS No.
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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Purity & Documentation
References
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BRD4-IN-12 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BRD4-IN-123112325-99-9Epigenetic Reader Domainc-MycBcl-2 FamilyPAKApoptosisMycp21 activated kinasesBRD4 inhibitorantitumor efficacydownregulates c-MYC/BCL-2/CDK4upregulates p21HCT-116 cellsBALB/c nude miceHCT-116 xenograft modelcolorectal cancer (CRC)Inhibitorinhibitorinhibit

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