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  3. BRD4 Inhibitor-20

BRD4 Inhibitor-20 

Cat. No.: HY-146208
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BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer.

For research use only. We do not sell to patients.

BRD4 Inhibitor-20 Chemical Structure

BRD4 Inhibitor-20 Chemical Structure

CAS No. : 2490311-14-1

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Description

BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer[1].

IC50 & Target[1]

BRD4 BD1

19 nM (IC50)

BRD4 BD2

28 nM (IC50)

BRD2 (BD1)

24 nM (IC50)

BRD2 (BD2)

18 nM (IC50)

In Vitro

BRD4 Inhibitor-20 (compound 12j) exhibits excellent BRD4 inhibitory activities (BD1, IC50=19 nM; BD2, IC50=28 nM) and inhibitory activities against BRD2 (BD1, IC50=24 nM; BD2, IC50=18 nM)[1].
BRD4 Inhibitor-20 (0.5, 2.5, 5.0 μM; 24 h) reduces the expression of c-Myc[1].
BRD4 Inhibitor-20 (72 h) has anti-proliferation potency with IC50 values of 4.75 μM, 1.35 μM and 44.07 μM in HT-29, HL-60 and WI-38 cells, respectively[1].
BRD4 Inhibitor-20 (2.5, 5.0, 10.0 μM; 24 h) can arrest the cell-cycle progression of HT-29 cells into the G1 phase[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HT-29 cells
Concentration: 0.5, 2.5, 5.0 μM
Incubation Time: 24 h
Result: Displayed profound inhibitory effects on c-Myc protein expression.

Cell Proliferation Assay[1]

Cell Line: HT-29, HL-60 and WI-38 cells
Concentration:
Incubation Time: 72 h
Result: Possessed strong anti-proliferative activity and weak toxicity.

Cell Cycle Analysis[1]

Cell Line: HT-29 cell lines
Concentration: 2.5, 5.0, 10.0 μM
Incubation Time: 24 h
Result: Arrested the cell-cycle progression of the cell line into the G1 phases and the percentage of cells in G1 phase after treatment under concentrations of 2.5, 5.0 and 10.0 μM were 85.98%, 86.49% and 86.05%, respectively.
In Vivo

BRD4 Inhibitor-20 (compound 12j) (i.v., 5 mg/kg; p.o, 15mg/kg) exhibits favorable oral pharmacokinetic propertie[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: rats[1]
Dosage: 5 mg/kg, 15 mg/kg
Administration: intravenous dosing (iv) or oral dosing (po)
Result:
PK Parameters iv (5 mg/kg) po (15 mg/kg)
Cmax(μg/L) - 2175
Tmax(h) - 1.00
t1/2(h) 1.56 3.59
CLz/F (L/h/kg) 0.68 1.03
AUC0−t(μg/L*h) 7296 14384
AUC0−∞(μg/L*h) 7340 14600
F (%) - 66%
Molecular Weight

358.41

Formula

C18H18N2O4S

CAS No.
SMILES

O=C1NC2=CC=C(C=C2/C1=C(C)\C)NS(=O)(C3=C(C=CC=C3)OC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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BRD4 Inhibitor-20
Cat. No.:
HY-146208
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